LATS1
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Also known as WARTS
Summary
LATS1 (large tumor suppressor kinase 1, HGNC:6514) is a protein-coding gene on chromosome 6q25.1, encoding Serine/threonine-protein kinase LATS1 (O95835). Negative regulator of YAP1 in the Hippo signaling pathway that plays a pivotal role in organ size control and tumor suppression by restricting proliferation and promoting apoptosis.
The protein encoded by this gene is a putative serine/threonine kinase that localizes to the mitotic apparatus and complexes with cell cycle controller CDC2 kinase in early mitosis. The protein is phosphorylated in a cell-cycle dependent manner, with late prophase phosphorylation remaining through metaphase. The N-terminal region of the protein binds CDC2 to form a complex showing reduced H1 histone kinase activity, indicating a role as a negative regulator of CDC2/cyclin A. In addition, the C-terminal kinase domain binds to its own N-terminal region, suggesting potential negative regulation through interference with complex formation via intramolecular binding. Biochemical and genetic data suggest a role as a tumor suppressor. This is supported by studies in knockout mice showing development of soft-tissue sarcomas, ovarian stromal cell tumors and a high sensitivity to carcinogenic treatments.
Source: NCBI Gene 9113 — RefSeq curated summary.
At a glance
- GWAS associations: 4
- Clinical variants (ClinVar): 131 total — 1 pathogenic, 2 likely-pathogenic
- Druggable target: yes — 32 molecules with ChEMBL bioactivity
- Cancer driver (intOGen): loss-of-function (tumor-suppressor-like) across 6 cancer types
- MANE Select transcript:
NM_004690
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:6514 |
| Approved symbol | LATS1 |
| Name | large tumor suppressor kinase 1 |
| Location | 6q25.1 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | WARTS |
| Ensembl gene | ENSG00000131023 |
| Ensembl biotype | protein_coding |
| OMIM | 603473 |
| Entrez | 9113 |
Gene structure
Transcript identifiers
Ensembl transcripts: 11 — 8 protein_coding, 2 nonsense_mediated_decay, 1 protein_coding_CDS_not_defined
ENST00000253339, ENST00000392273, ENST00000441107, ENST00000458696, ENST00000542720, ENST00000542747, ENST00000543571, ENST00000852165, ENST00000852166, ENST00000916254, ENST00000916255
RefSeq mRNA: 5 — MANE Select: NM_004690
NM_001270519, NM_001350339, NM_001350340, NM_001350392, NM_004690
CCDS: CCDS34551, CCDS59040
Canonical transcript exons
ENST00000543571 — 8 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001338727 | 149701779 | 149702266 |
| ENSE00002281518 | 149658153 | 149662238 |
| ENSE00002314788 | 149717849 | 149718101 |
| ENSE00003487293 | 149695074 | 149695221 |
| ENSE00003535606 | 149679875 | 149680457 |
| ENSE00003559966 | 149683079 | 149684592 |
| ENSE00003643935 | 149676260 | 149676366 |
| ENSE00003683657 | 149676555 | 149676737 |
Expression profiles
Bgee: expression breadth ubiquitous, 263 present calls, max score 95.24.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 13.6257 / max 172.8738, expressed in 1777 samples.
FANTOM5 promoters (3 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 76139 | 13.0281 | 1775 |
| 76140 | 0.5335 | 293 |
| 76138 | 0.0641 | 21 |
Top tissues by expression
287 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| germinal epithelium of ovary | UBERON:0001304 | 95.24 | gold quality |
| tibia | UBERON:0000979 | 95.22 | gold quality |
| mucosa of paranasal sinus | UBERON:0005030 | 93.20 | gold quality |
| gingival epithelium | UBERON:0001949 | 91.27 | gold quality |
| epithelium of nasopharynx | UBERON:0001951 | 91.23 | gold quality |
| nasopharynx | UBERON:0001728 | 91.21 | gold quality |
| parietal pleura | UBERON:0002400 | 90.97 | gold quality |
| visceral pleura | UBERON:0002401 | 90.76 | gold quality |
| seminal vesicle | UBERON:0000998 | 90.75 | gold quality |
| pigmented layer of retina | UBERON:0001782 | 90.20 | gold quality |
| palpebral conjunctiva | UBERON:0001812 | 90.18 | gold quality |
| eye | UBERON:0000970 | 90.17 | gold quality |
| pleura | UBERON:0000977 | 89.82 | gold quality |
| gingiva | UBERON:0001828 | 89.59 | gold quality |
| mammary duct | UBERON:0001765 | 89.39 | gold quality |
| amniotic fluid | UBERON:0000173 | 89.34 | gold quality |
| cortical plate | UBERON:0005343 | 89.08 | gold quality |
| jejunal mucosa | UBERON:0000399 | 89.01 | gold quality |
| skin of hip | UBERON:0001554 | 88.61 | gold quality |
| superficial temporal artery | UBERON:0001614 | 87.85 | gold quality |
| esophagus squamous epithelium | UBERON:0006920 | 87.80 | gold quality |
| ventricular zone | UBERON:0003053 | 87.58 | gold quality |
| caput epididymis | UBERON:0004358 | 87.54 | gold quality |
| adrenal tissue | UBERON:0018303 | 87.44 | gold quality |
| ganglionic eminence | UBERON:0004023 | 87.27 | gold quality |
| cauda epididymis | UBERON:0004360 | 86.90 | gold quality |
| jejunum | UBERON:0002115 | 86.81 | gold quality |
| mammalian vulva | UBERON:0000997 | 86.78 | gold quality |
| oral cavity | UBERON:0000167 | 86.70 | gold quality |
| corpus epididymis | UBERON:0004359 | 86.39 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | yes | 7.60 |
Regulation
Is transcription factor: yes
Downstream targets (CollecTRI)
1 targets.
| Target | Regulation |
|---|---|
| VEPH1 | Repression |
Upstream regulators (CollecTRI, top): CUX1, FOXC1, FOXL2, VEPH1, ZBED1
miRNA regulators (miRDB)
276 targeting LATS1, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-MIR-3613-3P | 100.00 | 76.36 | 7965 |
| HSA-MIR-3163 | 100.00 | 77.23 | 8605 |
| HSA-LET-7A-3P | 100.00 | 74.03 | 3932 |
| HSA-LET-7B-3P | 100.00 | 74.08 | 3913 |
| HSA-LET-7F-1-3P | 100.00 | 74.02 | 3928 |
| HSA-MIR-4262 | 100.00 | 73.26 | 3931 |
| HSA-MIR-98-3P | 100.00 | 74.08 | 3907 |
| HSA-MIR-3646 | 100.00 | 73.56 | 5283 |
| HSA-MIR-5692A | 100.00 | 74.40 | 6850 |
| HSA-MIR-340-5P | 100.00 | 72.50 | 4437 |
| HSA-MIR-200B-3P | 100.00 | 73.31 | 2693 |
| HSA-MIR-200C-3P | 100.00 | 73.35 | 2685 |
| HSA-MIR-429 | 100.00 | 73.44 | 2698 |
| HSA-MIR-4747-5P | 100.00 | 67.90 | 2681 |
| HSA-MIR-5196-5P | 100.00 | 67.98 | 2761 |
| HSA-MIR-5692B | 100.00 | 71.32 | 2622 |
| HSA-MIR-5692C | 100.00 | 71.32 | 2622 |
| HSA-MIR-450A-1-3P | 100.00 | 69.33 | 1837 |
| HSA-MIR-5011-5P | 100.00 | 83.46 | 5820 |
| HSA-MIR-4282 | 99.99 | 75.36 | 6408 |
| HSA-MIR-181A-5P | 99.99 | 72.96 | 2995 |
| HSA-MIR-181B-5P | 99.99 | 72.97 | 2996 |
| HSA-MIR-181C-5P | 99.99 | 72.95 | 2996 |
| HSA-MIR-181D-5P | 99.99 | 73.04 | 2997 |
| HSA-MIR-371B-5P | 99.99 | 75.34 | 4759 |
| HSA-MIR-3662 | 99.99 | 73.82 | 5684 |
| HSA-MIR-186-5P | 99.99 | 70.83 | 3707 |
| HSA-MIR-548AW | 99.99 | 72.57 | 3559 |
| HSA-MIR-548N | 99.98 | 71.94 | 4170 |
| HSA-MIR-4775 | 99.98 | 75.00 | 6394 |
Literature-anchored findings (GeneRIF, showing 40)
- regulation of function on the mitosis apparatus by Cdc/cyclin B (PMID:12372621)
- molecular alterations found in soft tissue sarcoma (PMID:12379777)
- kpm negatively regulates cell growth by inducing G(2)/M arrest and apoptotic cell death through its kinase activity (PMID:12624101)
- WARTS plays a critical role in maintenance of ploidy through its actions in both mitotic progression and the G(1) tetraploidy checkpoint (PMID:15122335)
- LATS1 is a novel cytoskeleton regulator that affects cytokinesis by regulating actin polymerization through negative modulation of LIMK1. (PMID:15220930)
- Mst2, a STE20-family member and purported Hpo ortholog, phosphorylates and activates both Lats1 and Lats2 (PMID:15688006)
- Hypermethylation of the promoter region of LATS1 likely plays an important role in the down-regulation of LATS1 mRNA level in breast cancers, and breast cancers with a decreased expression of LATS1 mRNA level have a biologically aggressive phenotype. (PMID:15746036)
- Activation of Omi / HtrA2-mediated cell death is a potential mechanism for the tumor suppressive activity of WARTS. (PMID:16007220)
- Moderate overexpression of human LATS1 in cells exposed to microtubule poisons facilitated mitotic exit, and this activity required MOB1A. (PMID:16061636)
- LATS1 and LATS2 mRNA was down-regulated in astrocytoma by hypermethylation of the promoter (PMID:17049657)
- LATS1 inactivates YAP oncogenic function by suppressing its transcription regulation of cellular genes via sequestration of YAP in the cytoplasm after phosphorylation of YAP. (PMID:18158288)
- Expression profiling of genes induced by ectopic expression of YAP or by knockdown of LATS1 reveals a subset of the potential Drosophila Hippo pathway targets implicated in epithelial-to-mesenchymal transition. (PMID:18413746)
- Overexpression of YAP2 in cells promoted apoptosis, whereas the Mst2/Lats1-induced phosphorylation of YAP partially rescued the cells from apoptotic death. (PMID:18640976)
- collection of genes identified suggests that LATS1/2 function through diverse mechanisms and multiple signaling pathways including the Hippo signaling pathway, as well as the p53, Ras-ERK, or WNT networks, to inhibit tumor progression (PMID:19799973)
- YAP is phosphorylated by Lats on all of the five consensus HXRXXS motifs (PMID:20048001)
- ubiquitin E3 ligase ITCH physically and functionally associates with LATS1 (PMID:21212414)
- KIBRA associates with and activates Lats (large tumor suppressor) 1 and 2 kinases by stimulating their phosphorylation on the hydrophobic motif (PMID:21233212)
- study identifies E3 ubiquitin ligase Itch as a unique negative regulator of LATS1 and presents a possibility of targeting LATS1/Itch interaction as a therapeutic strategy in cancer. (PMID:21383157)
- LATS1 phosphorylates a phosphatase as does the yeast Dbf2 and demonstrate a novel role of LATS1 in controlling PLK1 at the G2 DNA damage checkpoint. (PMID:22641346)
- These results indicate that LATS1 is an important candidate tumor suppressor and its downregulated expression may contribute to glioma progression (PMID:22909338)
- In conclusion, N-terminally truncated Lats1 induced Lats2 downregulation and Yap protein accumulation, leading to chromosomal instability and tumorigenesis. (PMID:23230145)
- LATS1 is critical in mediating WWP1-induced increased cell proliferation in breast cancer cells. (PMID:23573293)
- Decreased expression of LATS1 in CRC is associated with promoter hypermethylation, but not microsatellite instability status (PMID:23885148)
- LATS1 and LATS2 mutations from cancers can lead to loss or reduction of their growth-inhibitory activity (PMID:24026096)
- Data indicate that the phosphorylation of Amot130 by LATS1/2 is found to be a key feature that enables it to inhibit Yes-associated protein (YAP) dependent signaling and cell growth. (PMID:24101513)
- Thus AMOT is a direct substrate of Lats1/2 mediating functions of the Hippo pathway in endothelial cell migration and angiogenesis. (PMID:24106267)
- These results collectively suggest that the Hippo pathway negatively regulates the actin-binding activity of Amot family members through direct phosphorylation. (PMID:24225952)
- These results indicate that LATS1 may play an important role in NSCLC, and may serve as a novel therapeutic target of non-small-cell lung cancer (NSCLC). (PMID:24682895)
- overexpression of Kibra rescues the increased cell migration and aberrant three-dimensional morphogenesis induced by knockdown of PTPN14, and this rescue is mediated through the activation of the upstream LATS1 kinase (PMID:25023289)
- NF2 loss-driven derepressed CRL4(DCAF1) promotes activation of YAP by inhibiting hippo pathwat kinases Lats1 and 2 in the nucleus. (PMID:25026211)
- ivation of MSH4 in germ cells may have played a role in the acquisition of additional TP53 and LATS1 germline mutations in a Li-Fraumeni family (PMID:25041856)
- LATS1 and LATS2 kinases play an important role in the regulation of NS5A function through site-specific post-translational modification and that phosphorylation of Ser/Thr71 is essential for optimal viral genome replication. (PMID:25044019)
- Cyclic stretch is associated with a JNK-dependent increase in binding of a LATS inhibitor, LIMD1, to the LATS1 kinase and that reduction of LIMD1 expression suppresses the activation of YAP by cyclic stretch. (PMID:25127217)
- Data indicate that tumour suppressor RASSF1A triggers large tumor suppressor kinase 1 (LATS)-CDK2 interaction and restricts CDK2 kinase activity towards BRCA2. (PMID:25218637)
- both LATS1 demethylation and overexpression of LATS1 downregulated the expression of Yes-associated protein (YAP), inhibited cell proliferation, induced cell apoptosis and cell cycle G1 arrest in 786-O cells (PMID:25270913)
- Findings suggest that polyomavirus middle T-antigen (PyMT) activates the Hippo pathway tumor suppressor Lats in a Src-dependent manner. (PMID:25362852)
- The control of LATS activation by angiotensin II and subsequent YAP localization is important for podocyte homeostasis and survival. (PMID:25393475)
- results reported here further support that LATS1/2 act normally as tumor suppressors and loss of their functions contributes to human cancer development (PMID:25482410)
- ITCH up-regulation and LATS1 down-regulation were closely associated with tumorigenesis and progression of SCC (PMID:25618271)
- These results demonstrated that as an inhibitor of YAP, LATS1 was decreased via downregulation of YAP using RNAi. This therefore indicated that the change in YAP levels in hepatocellular carcinoma cells may regulate LATS1 in a feedback manner. (PMID:25625370)
Cross-species orthologs
6 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | lats1 | ENSDARG00000003751 |
| mus_musculus | Lats1 | ENSMUSG00000040021 |
| rattus_norvegicus | Lats1 | ENSRNOG00000014916 |
| drosophila_melanogaster | wts | FBGN0011739 |
| caenorhabditis_elegans | wts-1 | WBGENE00007047 |
| caenorhabditis_elegans | WBGENE00011992 |
Paralogs (13): MAST4 (ENSG00000069020), MAST2 (ENSG00000086015), MAST3 (ENSG00000099308), SGK2 (ENSG00000101049), SGK3 (ENSG00000104205), DMPK (ENSG00000104936), MAST1 (ENSG00000105613), SGK1 (ENSG00000118515), MASTL (ENSG00000120539), LATS2 (ENSG00000150457), STK32B (ENSG00000152953), STK32C (ENSG00000165752), STK32A (ENSG00000169302)
Protein
Protein identifiers
Serine/threonine-protein kinase LATS1 — O95835 (reviewed: O95835)
Alternative names: Large tumor suppressor homolog 1, WARTS protein kinase
All UniProt accessions (3): O95835, H0YG09, Q6PJG3
UniProt curated annotations — full annotation on UniProt →
Function. Negative regulator of YAP1 in the Hippo signaling pathway that plays a pivotal role in organ size control and tumor suppression by restricting proliferation and promoting apoptosis. The core of this pathway is composed of a kinase cascade wherein STK3/MST2 and STK4/MST1, in complex with its regulatory protein SAV1, phosphorylates and activates LATS1/2 in complex with its regulatory protein MOB1, which in turn phosphorylates and inactivates YAP1 oncoprotein and WWTR1/TAZ. Phosphorylation of YAP1 by LATS1 inhibits its translocation into the nucleus to regulate cellular genes important for cell proliferation, cell death, and cell migration. Acts as a tumor suppressor which plays a critical role in maintenance of ploidy through its actions in both mitotic progression and the G1 tetraploidy checkpoint. Negatively regulates G2/M transition by down-regulating CDK1 kinase activity. Involved in the control of p53 expression. Affects cytokinesis by regulating actin polymerization through negative modulation of LIMK1. May also play a role in endocrine function. Plays a role in mammary gland epithelial cell differentiation, both through the Hippo signaling pathway and the intracellular estrogen receptor signaling pathway by promoting the degradation of ESR1. Acts as an activator of the NLRP3 inflammasome by mediating phosphorylation of ‘Ser-265’ of NLRP3 following NLRP3 palmitoylation, promoting NLRP3 activation by NEK7.
Subunit / interactions. Complexes with CDK1 in early mitosis. LATS1-associated CDK1 has no mitotic cyclin partner and no apparent kinase activity. Binds phosphorylated ZYX, locating this protein to the mitotic spindle and suggesting a role for actin regulatory proteins during mitosis. Binds to and colocalizes with LIMK1 at the actomyosin contractile ring during cytokinesis. Interacts (via PPxY motif 2) with YAP1 (via WW domains). Interacts with MOB1A and MOB1B. Interacts with LIMD1, WTIP and AJUBA. Interacts with ESR1, DCAF1 and DCAF13; probably recruits DCAF1 and DCAF13 to ESR1 to promote ESR1 ubiquitination and ubiquitin-mediated proteasomal degradation. Interacts with STK3/MST2; this interaction is inhibited in the presence of DLG5. Interacts with SCRIB in the presence of DLG5. Interacts with WWTR1/TAZ. Interacts with WWC1, WWC2 and WWC3 (via their WW domains).
Subcellular location. Cytoplasm. Cytoskeleton. Microtubule organizing center. Centrosome. Spindle. Midbody. Spindle pole body.
Tissue specificity. Expressed in all adult tissues examined except for lung and kidney.
Post-translational modifications. Autophosphorylated and phosphorylated during M-phase of the cell cycle. Phosphorylated by STK3/MST2 at Ser-909 and Thr-1079, which results in its activation. Phosphorylated by MAP4Ks; in parallel to STK3/MST2 and resulting to its activation. Phosphorylation at Ser-464 by NUAK1 and NUAK2 leads to decreased protein level and is required to regulate cellular senescence and cellular ploidy.
Similarity. Belongs to the protein kinase superfamily. AGC Ser/Thr protein kinase family.
Isoforms (2)
| UniProt ID | Names | Canonical? |
|---|---|---|
| O95835-1 | 1 | yes |
| O95835-2 | 2 |
RefSeq proteins (5): NP_001257448, NP_001337268, NP_001337269, NP_001337321, NP_004681* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000719 | Prot_kinase_dom | Domain |
| IPR000961 | AGC-kinase_C | Domain |
| IPR008271 | Ser/Thr_kinase_AS | Active_site |
| IPR009060 | UBA-like_sf | Homologous_superfamily |
| IPR011009 | Kinase-like_dom_sf | Homologous_superfamily |
| IPR015940 | UBA | Domain |
| IPR017892 | Pkinase_C | Domain |
| IPR042706 | LATS1_STKc | Domain |
| IPR049761 | LATS1-like_MobB | Domain |
| IPR050236 | Ser_Thr_kinase_AGC | Family |
Pfam: PF00069, PF00433, PF00627
Catalyzed reactions (Rhea), 2 shown:
- L-seryl-[protein] + ATP = O-phospho-L-seryl-[protein] + ADP + H(+) (RHEA:17989)
- L-threonyl-[protein] + ATP = O-phospho-L-threonyl-[protein] + ADP + H(+) (RHEA:46608)
UniProt features (54 total): compositionally biased region 11, sequence variant 9, region of interest 8, modified residue 7, helix 5, domain 3, mutagenesis site 3, short sequence motif 2, binding site 2, splice variant 2, chain 1, active site 1
Structure
Experimental structures (PDB)
4 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 7LWH | X-RAY DIFFRACTION | 1.61 |
| 5BRK | X-RAY DIFFRACTION | 2.3 |
| 4ZRK | X-RAY DIFFRACTION | 2.32 |
| 5B5W | X-RAY DIFFRACTION | 2.96 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-O95835-F1 | 55.88 | 0.16 |
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Catalytic / active sites (1): 828 (proton acceptor)
Ligand- & substrate-binding residues (2): 711–719; 734
Post-translational modifications (7): 246, 278, 464, 613, 674, 909, 1079
Mutagenesis-validated functional residues (3):
| Position | Phenotype |
|---|---|
| 464 | abolishes phosphorylation by nuak1 and nuak2. |
| 559 | loss of interaction with yap1. |
| 734 | loss of kinase activity, autophosphorylation, increased ploidy, prolonged duration of mitosis and lack of p53 expression |
Function
Pathways and Gene Ontology
Reactome pathways
2 pathways
| ID | Pathway |
|---|---|
| R-HSA-2028269 | Signaling by Hippo |
| R-HSA-162582 | Signal Transduction |
MSigDB gene sets: 379 (showing top):
GSE45365_NK_CELL_VS_CD8A_DC_MCMV_INFECTION_DN, GOBP_CHROMOSOME_ORGANIZATION, GOBP_REGULATION_OF_CELLULAR_RESPONSE_TO_GROWTH_FACTOR_STIMULUS, GOBP_EMBRYO_DEVELOPMENT_ENDING_IN_BIRTH_OR_EGG_HATCHING, GOBP_EPITHELIUM_DEVELOPMENT, GOBP_REGULATION_OF_PROTEIN_POLYMERIZATION, GOBP_REGULATION_OF_PHOSPHORYLATION, GOBP_NEGATIVE_REGULATION_OF_KINASE_ACTIVITY, GOBP_INFLAMMATORY_RESPONSE, GOBP_SYNAPSE_ASSEMBLY, GOBP_CELLULAR_RESPONSE_TO_LIPID, GOBP_REGULATION_OF_DEVELOPMENTAL_GROWTH, GOBP_MAMMARY_GLAND_EPITHELIUM_DEVELOPMENT, GOBP_CELL_CYCLE_PHASE_TRANSITION, GOBP_GROWTH
GO Biological Process (27): G1/S transition of mitotic cell cycle (GO:0000082), G2/M transition of mitotic cell cycle (GO:0000086), sister chromatid segregation (GO:0000819), inner cell mass cell fate commitment (GO:0001827), inner cell mass cellular morphogenesis (GO:0001828), protein phosphorylation (GO:0006468), intracellular protein localization (GO:0008104), hormone-mediated signaling pathway (GO:0009755), regulation of transforming growth factor beta receptor signaling pathway (GO:0017015), keratinocyte differentiation (GO:0030216), regulation of actin filament polymerization (GO:0030833), regulation of intracellular estrogen receptor signaling pathway (GO:0033146), hippo signaling (GO:0035329), positive regulation of apoptotic process (GO:0043065), regulation of protein-containing complex assembly (GO:0043254), negative regulation of cyclin-dependent protein serine/threonine kinase activity (GO:0045736), regulation of organ growth (GO:0046620), cell division (GO:0051301), mammary gland epithelial cell differentiation (GO:0060644), negative regulation of canonical Wnt signaling pathway (GO:0090090), regulation of postsynaptic density assembly (GO:0099151), negative regulation of protein localization to nucleus (GO:1900181), positive regulation of NLRP3 inflammasome complex assembly (GO:1900227), regulation of ubiquitin-dependent protein catabolic process (GO:2000058), positive regulation of hippo signaling (GO:0035332), NLRP3 inflammasome complex assembly (GO:0044546), mitotic cell cycle phase transition (GO:0044772)
GO Molecular Function (12): magnesium ion binding (GO:0000287), protein serine/threonine kinase activity (GO:0004674), ATP binding (GO:0005524), protein kinase binding (GO:0019901), nuclear estrogen receptor binding (GO:0030331), protein serine kinase activity (GO:0106310), nucleotide binding (GO:0000166), protein kinase activity (GO:0004672), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740), metal ion binding (GO:0046872)
GO Cellular Component (11): spindle pole (GO:0000922), nucleus (GO:0005634), cytoplasm (GO:0005737), centrosome (GO:0005813), microtubule organizing center (GO:0005815), cytosol (GO:0005829), midbody (GO:0030496), postsynapse (GO:0098794), glutamatergic synapse (GO:0098978), spindle (GO:0005819), cytoskeleton (GO:0005856)
Reactome top-level categories
Rollup of top-1 pathways:
| Category | Pathways |
|---|---|
| Signal Transduction | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| cellular anatomical structure | 6 |
| mitotic cell cycle | 2 |
| mitotic cell cycle phase transition | 2 |
| inner cell mass cell differentiation | 2 |
| protein kinase activity | 2 |
| microtubule cytoskeleton | 2 |
| synapse | 2 |
| intracellular membraneless organelle | 2 |
| cell cycle G1/S phase transition | 1 |
| cell cycle G2/M phase transition | 1 |
| chromosome organization | 1 |
| nuclear chromosome segregation | 1 |
| cell fate commitment | 1 |
| cell morphogenesis | 1 |
| embryonic morphogenesis | 1 |
| phosphorylation | 1 |
| protein modification process | 1 |
| macromolecule localization | 1 |
| signal transduction | 1 |
| cellular response to hormone stimulus | 1 |
| transforming growth factor beta receptor signaling pathway | 1 |
| regulation of transmembrane receptor protein serine/threonine kinase signaling pathway | 1 |
| regulation of cellular response to transforming growth factor beta stimulus | 1 |
| epidermal cell differentiation | 1 |
| skin development | 1 |
| regulation of actin polymerization or depolymerization | 1 |
| actin filament polymerization | 1 |
| regulation of protein polymerization | 1 |
| estrogen receptor signaling pathway | 1 |
| regulation of intracellular steroid hormone receptor signaling pathway | 1 |
| intracellular signal transduction | 1 |
| apoptotic process | 1 |
| regulation of apoptotic process | 1 |
| positive regulation of programmed cell death | 1 |
| regulation of cellular component biogenesis | 1 |
| regulation of cellular component organization | 1 |
| protein-containing complex assembly | 1 |
| regulation of cyclin-dependent protein serine/threonine kinase activity | 1 |
| cyclin-dependent protein serine/threonine kinase activity | 1 |
| negative regulation of cell cycle | 1 |
Protein interactions and networks
STRING
1850 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| LATS1 | SAV1 | Q9H4B6 | 998 |
| LATS1 | MOB1A | Q9H8S9 | 994 |
| LATS1 | MOB1B | Q7L9L4 | 993 |
| LATS1 | YAP1 | P46937 | 974 |
| LATS1 | NF2 | P35240 | 909 |
| LATS1 | LIMD1 | Q9UGP4 | 860 |
| LATS1 | SCRIB | Q14160 | 855 |
| LATS1 | AMOT | Q4VCS5 | 852 |
| LATS1 | TEAD1 | P28347 | 802 |
| LATS1 | ZYX | Q15942 | 795 |
| LATS1 | WWC1 | Q8IX03 | 794 |
| LATS1 | RASSF1 | Q9NS23 | 777 |
| LATS1 | WWTR1 | Q9GZV5 | 759 |
| LATS1 | CCN1 | O00622 | 753 |
| LATS1 | CCN2 | P29279 | 741 |
IntAct
150 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| YAP1 | LATS1 | psi-mi:“MI:0407”(direct interaction) | 0.880 |
| LATS1 | YAP1 | psi-mi:“MI:0217”(phosphorylation reaction) | 0.880 |
| LATS1 | YAP1 | psi-mi:“MI:0407”(direct interaction) | 0.880 |
| MOB1B | LATS1 | psi-mi:“MI:0914”(association) | 0.840 |
| MOB1B | LATS1 | psi-mi:“MI:0915”(physical association) | 0.840 |
| LATS1 | MOB1B | psi-mi:“MI:0915”(physical association) | 0.840 |
| YAP1 | MPDZ | psi-mi:“MI:0914”(association) | 0.780 |
| LATS1 | MOB1A | psi-mi:“MI:0915”(physical association) | 0.670 |
| LATS1 | YWHAH | psi-mi:“MI:0914”(association) | 0.670 |
| MOB1A | LATS1 | psi-mi:“MI:0914”(association) | 0.670 |
| YWHAG | BLTP3B | psi-mi:“MI:2364”(proximity) | 0.640 |
| WWTR1 | LATS1 | psi-mi:“MI:0914”(association) | 0.640 |
| LATS1 | WWTR1 | psi-mi:“MI:0915”(physical association) | 0.640 |
| LATS1 | CDK1 | psi-mi:“MI:0914”(association) | 0.630 |
| CDK1 | LATS1 | psi-mi:“MI:0915”(physical association) | 0.630 |
| LATS1 | CDK1 | psi-mi:“MI:0915”(physical association) | 0.630 |
BioGRID (732): LATS1 (Two-hybrid), LATS1 (Two-hybrid), LATS1 (Two-hybrid), LDOC1 (Two-hybrid), TFIP11 (Two-hybrid), MOAP1 (Two-hybrid), CEP76 (Two-hybrid), SSX2IP (Two-hybrid), FSD2 (Two-hybrid), SPERT (Two-hybrid), WWTR1 (Biochemical Activity), WWTR1 (Affinity Capture-Western), YAP1 (Protein-peptide), TAZ (Protein-peptide), ITCH (Protein-peptide)
ESM2 similar proteins: A0A0K3AV08, A7J1T0, A7J1T2, A7KAX9, A8X775, A8XU52, A9SY39, B4K6T8, G5EBZ8, G5ECQ3, G5EDE9, G5EEK3, G5EEW9, G5EGK6, O01700, O13839, O17862, O43283, O44757, O45797, O61366, O62090, O95835, P03949, P83510, Q03345, Q09314, Q09446, Q09994, Q11100, Q11181, Q17353, Q21341, Q3LRZ3, Q5R8X7, Q60JJ0, Q60LV7, Q61DP2, Q6E3D4, Q6GPD0
Diamond homologs: A2VDV2, A8WVU9, A8XJL7, E9PSL7, F4HPN2, F4HYG2, F4J6F6, M3TYT0, O01583, O13310, O14578, O15021, O45797, O54874, O60307, O75116, O77819, O94487, O95835, P00517, P05131, P05383, P0C1B1, P12688, P17612, P18961, P22204, P22694, P25321, P27791, P31034, P32328, P36887, P38679, P38938, P49025, P53894, P54265, P54644, P68180
SIGNOR signaling
41 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| STK3 | up-regulates | LATS1 | phosphorylation |
| STK4 | up-regulates | LATS1 | phosphorylation |
| NUAK1 | down-regulates | LATS1 | phosphorylation |
| NUAK2 | down-regulates | LATS1 | phosphorylation |
| MOB1A | up-regulates | LATS1 | binding |
| MOB1B | up-regulates | LATS1 | binding |
| LATS1 | down-regulates | WWTR1 | phosphorylation |
| LATS1 | “down-regulates quantity by repression” | VEPH1 | “transcriptional regulation” |
| VEPH1 | “down-regulates quantity by repression” | LATS1 | “transcriptional regulation” |
| F2R | down-regulates | LATS1 | |
| LATS1 | down-regulates | YAP1 | phosphorylation |
| “sphingosine 1-phosphate” | down-regulates | LATS1 | |
| (R)-adrenaline | up-regulates | LATS1 | |
| GCG | up-regulates | LATS1 | |
| F-actin_assembly | down-regulates | LATS1 | |
| NF2 | up-regulates | LATS1 | binding |
| CyclinB/CDK1 | up-regulates | LATS1 | phosphorylation |
| LATS1 | “down-regulates quantity by destabilization” | YAP1 | phosphorylation |
| Mob1 | up-regulates | LATS1 | binding |
| STK3/4 | up-regulates | LATS1 | phosphorylation |
| DCAF1 | “down-regulates quantity by destabilization” | LATS1 | binding |
| Cullin4-RBX1-DDB1 | “down-regulates quantity by destabilization” | LATS1 | ubiquitination |
| PPM1F | “down-regulates activity” | LATS1 | dephosphorylation |
| GNA13 | “down-regulates activity” | LATS1 | phosphorylation |
| ITCH | “down-regulates quantity” | LATS1 | destabilization |
| LATS1 | “up-regulates activity” | PPP1R12A | phosphorylation |
Enriched among interaction partners
Reactome pathways and GO biological processes over-represented among this gene’s 84 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.
Reactome pathways:
| Pathway | Partners | Fold | FDR |
|---|---|---|---|
| Activation of BAD and translocation to mitochondria | 8 | 95.2× | 7e-13 |
| Signaling by Hippo | 10 | 85.0× | 3e-15 |
| Chk1/Chk2(Cds1) mediated inactivation of Cyclin B:Cdk1 complex | 8 | 84.0× | 2e-12 |
| SARS-CoV-1 targets host intracellular signalling and regulatory pathways | 8 | 84.0× | 2e-12 |
| Activation of BH3-only proteins | 8 | 62.1× | 2e-11 |
| FOXO-mediated transcription | 8 | 42.0× | 7e-10 |
| RHO GTPases activate PKNs | 8 | 39.6× | 1e-09 |
| Intrinsic Pathway for Apoptosis | 8 | 36.6× | 2e-09 |
GO biological processes:
| GO term | Partners | Fold | FDR |
|---|---|---|---|
| hippo signaling | 9 | 85.6× | 4e-13 |
| positive regulation of protein localization to nucleus | 5 | 25.4× | 3e-04 |
| protein targeting | 5 | 23.8× | 4e-04 |
| ERK1 and ERK2 cascade | 5 | 20.6× | 5e-04 |
| positive regulation of stress fiber assembly | 5 | 20.3× | 5e-04 |
| intracellular protein localization | 12 | 16.3× | 4e-09 |
| G1/S transition of mitotic cell cycle | 5 | 13.0× | 3e-03 |
| regulation of cell migration | 5 | 10.2× | 6e-03 |
Disease & clinical
Cancer significance
From intOGen — cancer-driver classification: loss-of-function (tumor-suppressor-like) across 6 cancer types — BCC, BRCA, CEAD, CESC, OVT, PAAD.
Clinical variants and AI predictions
ClinVar
131 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 1 |
| Likely pathogenic | 2 |
| Uncertain significance | 101 |
| Likely benign | 4 |
| Benign | 1 |
Top pathogenic / likely-pathogenic (3)
| Variant ID | HGVS | Classification |
|---|---|---|
| 1801795 | NM_004690.4(LATS1):c.375A>T (p.Lys125Asn) | Pathogenic |
| 619199 | NM_004690.4(LATS1):c.2636G>A (p.Trp879Ter) | Likely pathogenic |
| 800329 | NM_004690.4(LATS1):c.2449G>A (p.Glu817Lys) | Likely pathogenic |
SpliceAI
1885 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 6:149664573:T:A | donor_gain | 1.0000 |
| 6:149676549:CTTTA:C | donor_loss | 1.0000 |
| 6:149676550:TTTA:T | donor_loss | 1.0000 |
| 6:149676551:TTA:T | donor_loss | 1.0000 |
| 6:149676552:TAC:T | donor_loss | 1.0000 |
| 6:149676553:A:AC | donor_gain | 1.0000 |
| 6:149676554:C:CC | donor_gain | 1.0000 |
| 6:149676733:GTCAC:G | acceptor_gain | 1.0000 |
| 6:149676734:TCAC:T | acceptor_gain | 1.0000 |
| 6:149676735:CAC:C | acceptor_gain | 1.0000 |
| 6:149676735:CACC:C | acceptor_gain | 1.0000 |
| 6:149676736:AC:A | acceptor_gain | 1.0000 |
| 6:149676737:CC:C | acceptor_gain | 1.0000 |
| 6:149676738:C:CC | acceptor_gain | 1.0000 |
| 6:149676741:C:CT | acceptor_gain | 1.0000 |
| 6:149676744:A:T | acceptor_gain | 1.0000 |
| 6:149676746:C:CT | acceptor_gain | 1.0000 |
| 6:149676747:A:T | acceptor_gain | 1.0000 |
| 6:149679874:CCACT:C | donor_gain | 1.0000 |
| 6:149695070:TCAC:T | donor_loss | 1.0000 |
| 6:149695071:CACC:C | donor_loss | 1.0000 |
| 6:149695072:A:AG | donor_loss | 1.0000 |
| 6:149695073:C:CG | donor_loss | 1.0000 |
| 6:149695218:TATC:T | acceptor_gain | 1.0000 |
| 6:149695220:TC:T | acceptor_gain | 1.0000 |
| 6:149695221:CCTGA:C | acceptor_gain | 1.0000 |
| 6:149695225:A:AC | acceptor_gain | 1.0000 |
| 6:149695225:A:C | acceptor_gain | 1.0000 |
| 6:149695227:A:AC | acceptor_gain | 1.0000 |
| 6:149695227:A:C | acceptor_gain | 1.0000 |
AlphaMissense
7482 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 6:149661873:A:C | F1083L | 1.000 |
| 6:149661873:A:T | F1083L | 1.000 |
| 6:149661875:A:G | F1083L | 1.000 |
| 6:149661882:G:C | F1080L | 1.000 |
| 6:149661882:G:T | F1080L | 1.000 |
| 6:149661884:A:G | F1080L | 1.000 |
| 6:149661888:A:C | F1078L | 1.000 |
| 6:149661888:A:T | F1078L | 1.000 |
| 6:149661889:A:G | F1078S | 1.000 |
| 6:149661890:A:G | F1078L | 1.000 |
| 6:149661897:G:C | F1075L | 1.000 |
| 6:149661897:G:T | F1075L | 1.000 |
| 6:149661899:A:G | F1075L | 1.000 |
| 6:149662005:A:C | F1039L | 1.000 |
| 6:149662005:A:T | F1039L | 1.000 |
| 6:149662006:A:C | F1039C | 1.000 |
| 6:149662006:A:G | F1039S | 1.000 |
| 6:149662007:A:G | F1039L | 1.000 |
| 6:149662139:G:T | R995S | 1.000 |
| 6:149676333:C:T | G937D | 1.000 |
| 6:149676334:C:G | G937R | 1.000 |
| 6:149676338:A:C | S935R | 1.000 |
| 6:149676338:A:T | S935R | 1.000 |
| 6:149676340:T:G | S935R | 1.000 |
| 6:149676341:C:A | W934C | 1.000 |
| 6:149676341:C:G | W934C | 1.000 |
| 6:149676343:A:G | W934R | 1.000 |
| 6:149676343:A:T | W934R | 1.000 |
| 6:149676346:A:G | W933R | 1.000 |
| 6:149676346:A:T | W933R | 1.000 |
dbSNP variants (sampled 300 via entrez): RS1000058495 (6:149672025 A>G), RS1000101403 (6:149667329 G>A), RS1000132521 (6:149667645 T>C,G), RS1000146642 (6:149711066 C>A), RS1000260189 (6:149704972 C>T), RS1000394368 (6:149669529 G>A), RS1000405432 (6:149673922 G>A), RS1000449314 (6:149712640 C>A), RS1000463203 (6:149699760 T>C), RS1000465498 (6:149699004 T>A), RS1000536802 (6:149712575 T>G), RS1000592690 (6:149706381 G>A,C), RS1000603346 (6:149711270 C>A), RS1000647682 (6:149660538 C>A,G), RS1000693065 (6:149699763 A>T)
Disease associations
OMIM: gene MIM:603473 | disease phenotypes: MIM:254500
GenCC curated gene-disease
Mondo (5): myoepithelial tumor (MONDO:0002380), teratoma (MONDO:0002601), ependymoma (MONDO:0016698), malignant peritoneal mesothelioma (MONDO:0005512), plasma cell myeloma (MONDO:0009693)
Orphanet (4): Ependymoma (Orphanet:251636), Malignant peritoneal mesothelioma (Orphanet:168811), Multiple myeloma (Orphanet:29073), AL amyloidosis (Orphanet:85443)
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
4 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST004635_15 | Testicular germ cell tumor | 2.000000e-09 |
| GCST006631_15 | Nicotine dependence and major depression (severity of comorbidity) | 4.000000e-06 |
| GCST010702_29 | Subcortical volume (MOSTest) | 7.000000e-11 |
| GCST010703_317 | Brain morphology (MOSTest) | 7.000000e-22 |
EFO canonical traits (3, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0007006 | depressive symptom measurement |
| EFO:0009262 | nicotine dependence symptom count |
| EFO:0004346 | neuroimaging measurement |
MeSH disease descriptors (4)
| Descriptor | Name | Tree numbers |
|---|---|---|
| D004806 | Ependymoma | C04.557.465.625.600.380.290; C04.557.470.670.380.290; C04.557.580.625.600.380.290 |
| D009101 | Multiple Myeloma | C04.557.595.500; C14.907.454.460; C15.378.147.780.650; C15.378.463.515.460; C20.683.515.845; C20.683.780.650 |
| D009208 | Myoepithelioma | C04.557.435.585 |
| D013724 | Teratoma | C04.557.465.910 |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (2): CHEMBL4523992 (PROTEIN FAMILY), CHEMBL6167 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
32 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 144,779 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).
| Molecule | Name | Phase | Patents |
|---|---|---|---|
| CHEMBL1873475 | IBRUTINIB | 4 | 7,994 |
| CHEMBL2103830 | FOSTAMATINIB | 4 | 3,841 |
| CHEMBL2325741 | CAPIVASERTIB | 4 | 2,157 |
| CHEMBL3301622 | GILTERITINIB | 4 | 2,395 |
| CHEMBL502835 | NINTEDANIB | 4 | 8,545 |
| CHEMBL535 | SUNITINIB | 4 | 79,020 |
| CHEMBL608533 | MIDOSTAURIN | 4 | 7,259 |
| CHEMBL1091644 | LINSITINIB | 3 | 1,446 |
| CHEMBL2105728 | CRENOLANIB | 3 | 2,167 |
| CHEMBL223360 | LINIFANIB | 3 | 3,925 |
| CHEMBL274654 | ORANTINIB | 3 | 3,596 |
| CHEMBL3137331 | DEFACTINIB | 3 | 1,229 |
| CHEMBL38380 | FASUDIL | 3 | 11,953 |
| CHEMBL522892 | DOVITINIB | 3 | 4,944 |
| CHEMBL603469 | LESTAURTINIB | 3 | |
| CHEMBL91829 | RUBOXISTAURIN | 3 | 77 |
| CHEMBL1721885 | SU-014813 | 2 | 363 |
| CHEMBL230011 | TG100-115 | 2 | 1,504 |
| CHEMBL2386889 | SCH-900776 | 2 | 740 |
| CHEMBL3137336 | UPROSERTIB | 2 | 1,624 |
| CHEMBL495727 | AT-9283 | 2 | |
| CHEMBL564829 | MILCICLIB | 2 | |
| CHEMBL572878 | TOZASERTIB | 2 | |
| CHEMBL1908397 | KW-2449 | 1 | |
| CHEMBL3128043 | PF-03758309 | 1 | |
| CHEMBL3544960 | AT-13148 | 1 | |
| CHEMBL3545328 | XL-019 | 1 | |
| CHEMBL4289017 | PF-03814735 | 1 | |
| CHEMBL482967 | CYC-116 | 1 | |
| CHEMBL494089 | GSK-690693 | 1 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: enzyme — NDR family
Most potent curated ligand interactions (14 total), top 14:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| TRULI | Inhibition | 9.7 | pIC50 |
| example 320 [WO2018198077A2] | Inhibition | 9.15 | pIC50 |
| lestaurtinib | Inhibition | 7.52 | pKd |
| staurosporine | Inhibition | 7.38 | pKd |
| K-252a | Inhibition | 7.17 | pKd |
| PF-3758309 | Inhibition | 6.8 | pKd |
| Lpi-1 | Binding | 6.61 | pKd |
| AST-487 | Inhibition | 6.33 | pKd |
| BI-847325 | Inhibition | 6.2 | pKd |
| sunitinib | Inhibition | 6.2 | pKd |
| A-674563 | Inhibition | 5.96 | pKd |
| midostaurin | Inhibition | 5.96 | pKd |
| defactinib | Inhibition | 5.04 | pKd |
| nintedanib | Inhibition | 4.97 | pKd |
Binding affinities (BindingDB)
12 measured of 12 human assays (12 total across all organisms); most potent 12 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| Staurosporine | KD | 1.7 nM | |
| 2-(3-methylpyrazolidin-4-yl)-N-[(1R)-1-phenylethyl]pyrido[3,4-d]pyrimidin-4-amine | IC50 | 28 nM | US-11458138: 6-6 fused bicyclic heteroaryl compounds and their use as LATS inhibitors |
| 2-(3-methylpyrazolidin-4-yl)-N-(1-pyridin-4-ylethyl)pyrido[3,4-d]pyrimidin-4-amine | IC50 | 99 nM | US-11458138: 6-6 fused bicyclic heteroaryl compounds and their use as LATS inhibitors |
| N-[(1R)-1-phenylethyl]-2-pyrazolidin-4-ylpyrido[3,4-d]pyrimidin-4-amine | IC50 | 143 nM | US-11458138: 6-6 fused bicyclic heteroaryl compounds and their use as LATS inhibitors |
| PKC-412 | KD | 190 nM | |
| (3Z)-4-amino-5-fluoro-3-[5-(4-methylpiperazino)-1,3-dihydrobenzimidazol-2-ylidene]carbostyril | KD | 520 nM | |
| (18S)-18-[(dimethylamino)methyl]-17-oxa-4,14,21-triazahexacyclo[19.6.1.1^{7,14}.0^{2,6}.0^{8,13}.0^{22,27}]nonacosa-1(28),2(6),7(29),8(13),9,11,22(27),23,25-nonaene-3,5-dione | KD | 700 nM | |
| 2-pyrazolidin-4-yl-N-(1-pyridin-4-ylethyl)pyrido[3,4-d]pyrimidin-4-amine | IC50 | 797 nM | US-11458138: 6-6 fused bicyclic heteroaryl compounds and their use as LATS inhibitors |
| N-[4-({4-[(3-methyl-1H-pyrazol-5-yl)amino]-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl}sulfanyl)phenyl]cyclopropanecarboxamide | KD | 1100 nM | |
| 1-[4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-3-[4-[[6-(methylamino)-4-pyrimidinyl]oxy]phenyl]urea | KD | 1400 nM | |
| 5-[(Z)-(5-fluoranyl-2-oxidanylidene-1H-indol-3-ylidene)methyl]-2,4-dimethyl-N-[(2S)-3-morpholin-4-yl-2-oxidanyl-propyl]-1H-pyrrole-3-carboxamide | KD | 2600 nM | |
| N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide | KD | 3500 nM |
ChEMBL bioactivities
866 potent at pChembl≥5 of 933 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
PubChem BioAssay actives
62 with measured affinity, of 499 total; 44 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| 4-methyl-3-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide | 2148641: Binding affinity to human LATS1 incubated for 45 mins by Kinobead based pull down assay | kd | 0.0015 | uM |
| (2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-16-one | 1531743: Inhibition of human LATS1 using KKRNRRLSVA as substrate by [gamma-33P]-ATP assay | ic50 | 0.0128 | uM |
| 1-[6-(3,5-dichloro-4-hydroxyphenyl)-4-[[4-[(dimethylamino)methyl]cyclohexyl]amino]-1,5-naphthyridin-3-yl]ethanone | 1425033: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.0140 | uM |
| (15S,16S,18R)-16-hydroxy-16-(hydroxymethyl)-15-methyl-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8,10,12,20,22,24,26-nonaen-3-one | 1425033: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.0250 | uM |
| (1S)-2-amino-1-(4-chlorophenyl)-1-[4-(1H-pyrazol-4-yl)phenyl]ethanol | 1425033: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.0270 | uM |
| 1-cyclopropyl-3-[5-[6-(morpholin-4-ylmethyl)-1H-benzimidazol-2-yl]-1H-pyrazol-4-yl]urea | 1425033: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.0450 | uM |
| 6-(3-methylimidazol-4-yl)-4-(7H-purin-6-yl)-2,3-dihydro-1,4-thiazine | 2019964: Inhibition of LATS1 (unknown origin) | ic50 | 0.0640 | uM |
| 4-methyl-5-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]-1,3-thiazol-2-amine | 1425033: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.0660 | uM |
| methyl (15S,16R,18R)-16-hydroxy-15-methyl-3-oxo-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8,10,12,20,22,24,26-nonaene-16-carboxylate | 1425033: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.0670 | uM |
| 4-methyl-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide | 2148641: Binding affinity to human LATS1 incubated for 45 mins by Kinobead based pull down assay | kd | 0.0692 | uM |
| 4-[2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[[(3S)-piperidin-3-yl]methoxy]imidazo[4,5-c]pyridin-4-yl]-2-methylbut-3-yn-2-ol | 1425033: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.0740 | uM |
| N-[(1S)-2-(dimethylamino)-1-phenylethyl]-6,6-dimethyl-3-[(2-methylthieno[3,2-d]pyrimidin-4-yl)amino]-1,4-dihydropyrrolo[3,4-d]pyrazole-5-carboxamide | 1425033: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.1570 | uM |
| 3-[8-amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl]-1-methylcyclobutan-1-ol | 1425033: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.1950 | uM |
| Gilteritinib | 1425033: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.2210 | uM |
| 4-(cyclopropylamino)-2-[4-(4-ethylsulfonylpiperazin-1-yl)anilino]pyrimidine-5-carboxamide;hydrochloride | 1425033: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.2610 | uM |
| 2-amino-2-cyclohexyl-N-[2-(1-methylpyrazol-4-yl)-9-oxo-3,10,11-triazatricyclo[6.4.1.04,13]trideca-1,4,6,8(13),11-pentaen-6-yl]acetamide | 1425033: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.3630 | uM |
| N-[2-[4-[[4-(cyclobutylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]-11-azatricyclo[6.2.1.02,7]undeca-2(7),3,5-trien-11-yl]-2-oxoethyl]acetamide | 1425033: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.4060 | uM |
| methyl 2-hydroxy-3-[N-[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]phenyl]-C-phenylcarbonimidoyl]-1H-indole-6-carboxylate | 624963: Binding constant for LATS1 kinase domain | kd | 0.4200 | uM |
| 1-[4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[4-[6-(methylamino)pyrimidin-4-yl]oxyphenyl]urea | 435529: Binding constant for LATS1 kinase domain | kd | 0.4700 | uM |
| Sunitinib | 435529: Binding constant for LATS1 kinase domain | kd | 0.6300 | uM |
| 3-[3-[N-[4-[(dimethylamino)methyl]phenyl]-C-phenylcarbonimidoyl]-2-hydroxy-1H-indol-6-yl]-N-ethylprop-2-ynamide | 1425033: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.6350 | uM |
| N,1,4,4-tetramethyl-8-[4-(4-methylpiperazin-1-yl)anilino]-5H-pyrazolo[4,5-h]quinazoline-3-carboxamide | 1425033: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.6810 | uM |
| 5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide | 435529: Binding constant for LATS1 kinase domain | kd | 0.8500 | uM |
| 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one | 1425033: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.9550 | uM |
| (2S)-1-[[5-(3-methyl-2H-indazol-5-yl)-3-pyridinyl]oxy]-3-phenylpropan-2-amine | 624963: Binding constant for LATS1 kinase domain | kd | 1.1000 | uM |
| Midostaurin | 435529: Binding constant for LATS1 kinase domain | kd | 1.1000 | uM |
| 5-chloro-2-N-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine | 624963: Binding constant for LATS1 kinase domain | kd | 1.6000 | uM |
| Ibrutinib | 1425033: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 1.8840 | uM |
| 1-[4-(3-amino-1H-indazol-4-yl)phenyl]-3-(2-fluoro-5-methylphenyl)urea | 624963: Binding constant for LATS1 kinase domain | kd | 2.1000 | uM |
| Fostamatinib | 1425033: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 2.1570 | uM |
| (18S)-18-[(dimethylamino)methyl]-17-oxa-4,14,21-triazahexacyclo[19.6.1.17,14.02,6.08,13.022,27]nonacosa-1(28),2(6),7(29),8,10,12,22,24,26-nonaene-3,5-dione | 435529: Binding constant for LATS1 kinase domain | kd | 2.6000 | uM |
| 1-[2-[5-[(3-methyloxetan-3-yl)methoxy]benzimidazol-1-yl]quinolin-8-yl]piperidin-4-amine | 1425033: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 2.7680 | uM |
| 3-[2,4-dimethyl-5-[(Z)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid | 1425033: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 3.0110 | uM |
| 5-cyano-N-[2-(cyclohexen-1-yl)-4-[1-[2-(dimethylamino)acetyl]piperidin-4-yl]phenyl]-1H-imidazole-2-carboxamide;hydrochloride | 624963: Binding constant for LATS1 kinase domain | kd | 3.3000 | uM |
| N-[(2S)-1-amino-3-(3,4-difluorophenyl)propan-2-yl]-5-chloro-4-(4-chloro-1-methylpyrazol-5-yl)furan-2-carboxamide | 1425033: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 3.5920 | uM |
| N-[4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]phenyl]pyrrolidine-2-carboxamide | 1425033: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 3.7900 | uM |
| 7-[3-(azetidin-1-yl)cyclobutyl]-5-(3-phenylmethoxyphenyl)pyrrolo[2,3-d]pyrimidin-4-amine | 1425033: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 3.8790 | uM |
| 5-(1,4-diazepan-1-ylsulfonyl)isoquinoline | 1425033: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 4.1700 | uM |
| 3-[2,4-diamino-7-(3-hydroxyphenyl)pteridin-6-yl]phenol | 624963: Binding constant for LATS1 kinase domain | kd | 4.5000 | uM |
| 6-bromo-3-(1-methylpyrazol-4-yl)-5-[(3R)-piperidin-3-yl]pyrazolo[1,5-a]pyrimidin-7-amine | 1425033: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 4.6160 | uM |
| [4-[(E)-2-(1H-indazol-3-yl)ethenyl]phenyl]-piperazin-1-ylmethanone | 624963: Binding constant for LATS1 kinase domain | kd | 5.0000 | uM |
| N-[4-[4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]sulfanylphenyl]cyclopropanecarboxamide | 435529: Binding constant for LATS1 kinase domain | kd | 5.5000 | uM |
| N-methyl-4-[[4-[[3-[methyl(methylsulfonyl)amino]pyrazin-2-yl]methylamino]-5-(trifluoromethyl)pyrimidin-2-yl]amino]benzamide | 1425033: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 9.0500 | uM |
| Capivasertib | 1425033: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 14.1030 | uM |
CTD chemical–gene interactions
46 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| XMU-MP-1 | increases phosphorylation, decreases phosphorylation, decreases reaction, increases expression | 2 |
| sodium arsenite | affects binding, increases reaction, increases abundance, increases expression | 2 |
| Cadmium Chloride | decreases phosphorylation, decreases expression, increases abundance, decreases activity | 2 |
| aristolochic acid I | decreases expression | 1 |
| caulerpin | increases phosphorylation | 1 |
| 3-((6-(2-methoxyphenyl)pyrimidin-4-yl)amino)phenyl)methane sulfonamide | decreases expression | 1 |
| napabucasin | decreases expression | 1 |
| dicrotophos | increases expression | 1 |
| triphenyl phosphate | affects expression | 1 |
| gingerol | increases expression | 1 |
| mono-(2-ethylhexyl)phthalate | decreases reaction, increases stability | 1 |
| zinc chloride | decreases phosphorylation | 1 |
| manganese chloride | increases abundance, increases expression | 1 |
| coumarin | increases phosphorylation | 1 |
| nitazoxanide | increases expression | 1 |
| N,N,N’,N’-tetrakis(2-pyridylmethyl)ethylenediamine | affects binding, decreases reaction | 1 |
| evodiamine | increases phosphorylation, decreases reaction, increases expression | 1 |
| licochalcone A | decreases expression, increases expression | 1 |
| ginsenoside Rg3 | increases expression | 1 |
| jinfukang | decreases expression | 1 |
| Decitabine | affects methylation, affects expression | 1 |
| Sunitinib | increases expression | 1 |
| Leflunomide | increases expression | 1 |
| Air Pollutants | increases abundance, increases expression | 1 |
| Arsenic | increases abundance, increases expression | 1 |
| Arsenicals | affects response to substance, increases abundance | 1 |
| Benzo(a)pyrene | decreases methylation | 1 |
| Cadmium | decreases expression, increases abundance | 1 |
| Caffeine | affects phosphorylation | 1 |
| Chlorpromazine | increases phosphorylation | 1 |
ChEMBL screening assays
207 unique, capped per target: 207 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL4420664 | Binding | Inhibition of LATS in human HaCaT cells assessed as reduction in YAP phosphorylation level incubated for 2 hrs by HTRF assay | 6-6 Fused Bicyclic Heteroaryl Compounds and their Use as LATS Inhibitors |
Cellosaurus cell lines
15 cell lines: 13 cancer cell line, 1 transformed cell line, 1 induced pluripotent stem cell
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_1430 | MSTO-211H | Cancer cell line | Male |
| CVCL_B1AF | Abcam THP-1 LATS1 KO | Cancer cell line | Male |
| CVCL_B8JK | Abcam HCT 116 LATS1 KO | Cancer cell line | Male |
| CVCL_B8Y8 | Abcam MCF-7 LATS1 KO | Cancer cell line | Female |
| CVCL_B9LU | Abcam A-549 LATS1 KO | Cancer cell line | Male |
| CVCL_D7TF | Ubigene A-549 LATS1 KO | Cancer cell line | Male |
| CVCL_D8P3 | Ubigene HCT 116 LATS1 KO | Cancer cell line | Male |
| CVCL_D9IE | Ubigene HEK293 LATS1 KO | Transformed cell line | Female |
| CVCL_E0GC | Ubigene HeLa LATS1 KO | Cancer cell line | Female |
| CVCL_E0ZC | Ubigene MSTO-211H LDHA KO | Cancer cell line | Male |
Clinical trials (associated diseases)
300 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| NCT00029224 | PHASE4 | COMPLETED | Treatment With Zoledronic Acid in Patients With Breast Cancer, Multiple Myeloma, and Prostate Cancer With Cancer Related Bone Lesions |
| NCT00104104 | PHASE4 | COMPLETED | A Multiple Myeloma Trial in Patients With Bone Metastases |
| NCT00211211 | PHASE4 | COMPLETED | FREE Study - Fracture Reduction Evaluation |
| NCT00242528 | PHASE4 | WITHDRAWN | Open-label Study, to Evaluate the Safety and Tolerability of Zoledronic Acid in Patients With Bone Lesions Secondary to Multiple Myeloma. |
| NCT00257114 | PHASE4 | COMPLETED | Evaluation of VELCADE Given as Retreatment to Multiple Myeloma Patients for Efficacy, Safety and Tolerability |
| NCT00352703 | PHASE4 | COMPLETED | PROMPT - Palifermin in Reduction of Oral Mucositis in PBSC Transplantation |
| NCT00361140 | PHASE4 | COMPLETED | Busulfan Safety/Efficacy as Conditioning Prior to Hematopoietic Cell Transplantation (HCT) |
| NCT00622505 | PHASE4 | COMPLETED | Zoledronic Acid Treatment (Every 4 or 12 Weeks) to Prevent Skeletal Complications in Advanced Multiple Myeloma Participants |
| NCT00652041 | PHASE4 | COMPLETED | Bortezomib/Adriamycine/Melfalan/Prednisone (VAMP)/Thalidomide/Cyclophosphamide/Dexamethasone (TaCyDex) or Bortezomib/Melfalan/Prednisone (V-MP)/TaCyDex) in Refractary or Relapsed Multiple Myeloma |
| NCT00733538 | PHASE4 | COMPLETED | Stage I Multiple Myeloma Treatment |
| NCT01087008 | PHASE4 | COMPLETED | Zoledronic Acid in Patients With Multiple Myeloma and Asymptomatic Biochemical Relapse |
| NCT01249690 | PHASE4 | UNKNOWN | Efficacy Study of PAD and TAD in Newly Diagnosed Multiple Myeloma |
| NCT01410929 | PHASE4 | WITHDRAWN | Evaluation of Vertebral Compression Fracture Fixation With RF Kyphoplasty in Patients With Multiple Myeloma |
| NCT01731886 | PHASE4 | COMPLETED | Lenalidomide and Dexamethasone With/Without Stem Cell Transplant in Patients With Multiple Myeloma |
| NCT01868828 | PHASE4 | UNKNOWN | A Study of PAD Versus Velcade, Cyclophosphamide and Dexamethasone (VCD) Treatment in Subjects With Multiple Myeloma |
| NCT02268890 | PHASE4 | COMPLETED | A Pharmacokinetic Study of Bortezomib in Taiwanese Participants With Multiple Myeloma |
| NCT02286830 | PHASE4 | COMPLETED | Prolonged Protection From Bone Disease in Multiple Myeloma |
| NCT02559154 | PHASE4 | UNKNOWN | Modified Bortezomib-based Combination Therapy for Multiple Myeloma |
| NCT02577783 | PHASE4 | UNKNOWN | PDD vs PAD to Treat Initially Diagnosed MM |
| NCT02773550 | PHASE4 | TERMINATED | Treatment With a Scheme With Low Doses of Bortezomib / Melphalan / Prednisone (MPV) in Patients With Multiple Myeloma |
| NCT02958969 | PHASE4 | COMPLETED | Apixaban for Primary Prevention of Venous Thromboembolism in Patients With Multiple Myeloma |
| NCT03173092 | PHASE4 | TERMINATED | A Study of Ixazomib (NINLARO®) in Combination With Lenalidomide and Dexamethasone (IRD) for the Treatment of Participants With Multiple Myeloma (MM) |
| NCT03619252 | PHASE4 | COMPLETED | Pneumococcal Vaccination of Multiple Myeloma Patients on Novel Agents |
| NCT03768960 | PHASE4 | COMPLETED | A Study of DARZALEX (Daratumumab) In Indian Participants With Relapsed and Refractory Multiple Myeloma, Whose Prior Therapy Included a Proteasome Inhibitor and an Immunomodulatory Agent |
| NCT03829371 | PHASE4 | ACTIVE_NOT_RECRUITING | STUDY COMPARING TWO STANDARD TREATMENTS IN AUTOLOGOUS STEM CELL TRANSPLANTATION INELIGIBLE POPULATION AFFECTED BY MULTIPLE MYELOMA |
| NCT03908138 | PHASE4 | UNKNOWN | RDD Versus VDD in Newly Diagnosed Patients With Multiple Myeloma |
| NCT04217967 | PHASE4 | COMPLETED | Ixazomib, Lenalidomide, and Combination for Maintenance in NDMM Patients |
| NCT04952766 | PHASE4 | COMPLETED | Study Evaluating SARS-CoV-2 (COVID-19) Humoral Response After BNT162b2 Vaccine in Immunocompromised Adults Compared to Healthy Adults |
| NCT04989140 | PHASE4 | UNKNOWN | Study of Pomalidomide, Oral Dexamethasone and Ixazomib in Patients With Relapsed MM Who Have Received Lenalidomide |
| NCT05183139 | PHASE4 | WITHDRAWN | A Multicenter In-class Transition Study of Ixazomib Combined With Pomalidomide and Dexamethasone or With Lenalidomide and Dexamethasone in Adults With Relapsed/Refractory Multiple Myeloma |
| NCT05201781 | PHASE4 | RECRUITING | A Long-term Study for Participants Previously Treated With Ciltacabtagene Autoleucel |
| NCT05429515 | PHASE4 | NOT_YET_RECRUITING | Effect of HFR-SUPRA in the Treatment of Multiple Myeloma-related Acute Kidney Injury |
| NCT05511428 | PHASE4 | COMPLETED | Home Based Daratumumab Administration for Patients With Multiple Myeloma |
| NCT05545202 | PHASE4 | UNKNOWN | A Randomized, Comparative, Double-blind Trial of Pentaisomaltose and Dimethyl Sulphoxide for Cryoprotection of Hematopoietic Stem Cells in Subjects With Multiple Myeloma or Malignant Lymphoma With a Need for Autologous Transplantation |
| NCT05555329 | PHASE4 | COMPLETED | Alternative Dosing Scheme of Pomalidomide 4 mg Every Other Day Versus Pomalidomide 2 mg and 4 mg Every Day; the POMAlternative Study |
| NCT05722405 | PHASE4 | RECRUITING | Ixazomib Plus Low-dose Lenalidomide Versus Ixazomib Alone for Maintenance Treatment of High Risk Multiple Myeloma |
| NCT05855122 | PHASE4 | UNKNOWN | Safety and ASCT-related Symptom Burden Optimization of Tocilizumab in ASCT Following HD Melphalan Conditioning for Multiple Myeloma Patients |
| NCT05944783 | PHASE4 | NOT_YET_RECRUITING | Bioequivalence Studies of Dasatinib 100 Mg |
| NCT06057402 | PHASE4 | RECRUITING | Elranatamab Post Trial Access Study for Participants With Multiple Myeloma (MM) |
| NCT06251076 | PHASE4 | RECRUITING | Plan Development for Giving Teclistamab in the Outpatient Setting |
Related Atlas pages
- Targeted by drugs: Defactinib, Lestaurtinib, Midostaurin, Nintedanib, Sunitinib
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): ependymoma, malignant peritoneal mesothelioma, teratoma, testicular germ cell tumor