TUBA1B
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Also known as K-ALPHA-1
Summary
TUBA1B (tubulin alpha 1b, HGNC:18809) is a protein-coding gene on chromosome 12q13.12, encoding Tubulin alpha-1B chain (P68363). Tubulin is the major constituent of microtubules, protein filaments consisting of alpha- and beta-tubulin heterodimers. It is a common-essential gene (DepMap: required in 93.0% of cancer cell lines).
Enables several functions, including GTP binding activity; GTPase activity; and ubiquitin protein ligase binding activity. A structural constituent of cytoskeleton. Involved in microtubule cytoskeleton organization. Located in cilium and microtubule. Is active in microtubule cytoskeleton.
Source: NCBI Gene 10376 — RefSeq curated summary.
At a glance
- GWAS associations: 5
- Clinical variants (ClinVar): 23 total
- Druggable target: yes — 21 molecules with ChEMBL bioactivity
- Cancer dependency (DepMap): dependent in 93.0% of screened cell lines (common-essential)
- MANE Select transcript:
NM_006082
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:18809 |
| Approved symbol | TUBA1B |
| Name | tubulin alpha 1b |
| Location | 12q13.12 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | K-ALPHA-1 |
| Ensembl gene | ENSG00000123416 |
| Ensembl biotype | protein_coding |
| OMIM | 602530 |
| Entrez | 10376 |
Gene structure
Transcript identifiers
Ensembl transcripts: 13 — 10 protein_coding, 2 retained_intron, 1 nonsense_mediated_decay
ENST00000332858, ENST00000336023, ENST00000547476, ENST00000547765, ENST00000549870, ENST00000550367, ENST00000551324, ENST00000552984, ENST00000920097, ENST00000920098, ENST00000920099, ENST00000920100, ENST00000920101
RefSeq mRNA: 1 — MANE Select: NM_006082
NM_006082
CCDS: CCDS31792
Canonical transcript exons
ENST00000336023 — 4 exons
| Exon | Start | End |
|---|---|---|
| ENSE00002364243 | 49127782 | 49128938 |
| ENSE00003483466 | 49129242 | 49129390 |
| ENSE00003562279 | 49129500 | 49129722 |
| ENSE00003634293 | 49131298 | 49131395 |
Expression profiles
Bgee: expression breadth ubiquitous, 153 present calls, max score 99.95.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 2023.6541 / max 9793.5382, expressed in 1828 samples.
FANTOM5 promoters (8 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 130815 | 2012.6204 | 1828 |
| 130809 | 6.0600 | 1560 |
| 130810 | 2.1437 | 1042 |
| 130812 | 1.7782 | 875 |
| 130813 | 0.6607 | 286 |
| 130811 | 0.2188 | 64 |
| 206687 | 0.1156 | 26 |
| 130814 | 0.0566 | 15 |
Top tissues by expression
153 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| ventricular zone | UBERON:0003053 | 99.95 | gold quality |
| superior frontal gyrus | UBERON:0002661 | 99.90 | gold quality |
| frontal pole | UBERON:0002795 | 99.90 | gold quality |
| prefrontal cortex | UBERON:0000451 | 99.89 | gold quality |
| frontal cortex | UBERON:0001870 | 99.88 | gold quality |
| dorsal plus ventral thalamus | UBERON:0001897 | 99.88 | gold quality |
| right frontal lobe | UBERON:0002810 | 99.86 | gold quality |
| dorsolateral prefrontal cortex | UBERON:0009834 | 99.86 | gold quality |
| anterior cingulate cortex | UBERON:0009835 | 99.86 | gold quality |
| Brodmann (1909) area 9 | UBERON:0013540 | 99.86 | gold quality |
| Brodmann (1909) area 10 | UBERON:0013541 | 99.86 | gold quality |
| cerebral cortex | UBERON:0000956 | 99.84 | gold quality |
| ganglionic eminence | UBERON:0004023 | 99.84 | gold quality |
| primary visual cortex | UBERON:0002436 | 99.80 | gold quality |
| dorsal root ganglion | UBERON:0000044 | 99.79 | gold quality |
| hypothalamus | UBERON:0001898 | 99.79 | gold quality |
| spinal cord | UBERON:0002240 | 99.79 | gold quality |
| C1 segment of cervical spinal cord | UBERON:0006469 | 99.79 | gold quality |
| endometrium epithelium | UBERON:0004811 | 99.77 | gold quality |
| smooth muscle tissue | UBERON:0001135 | 99.74 | gold quality |
| cortical plate | UBERON:0005343 | 99.70 | gold quality |
| temporal lobe | UBERON:0001871 | 99.69 | gold quality |
| amygdala | UBERON:0001876 | 99.68 | gold quality |
| Ammon’s horn | UBERON:0001954 | 99.68 | gold quality |
| substantia nigra | UBERON:0002038 | 99.67 | gold quality |
| islet of Langerhans | UBERON:0000006 | 99.66 | gold quality |
| cerebellum | UBERON:0002037 | 99.66 | gold quality |
| cerebellar cortex | UBERON:0002129 | 99.66 | gold quality |
| cerebellar hemisphere | UBERON:0002245 | 99.66 | gold quality |
| right hemisphere of cerebellum | UBERON:0014890 | 99.65 | gold quality |
Single-cell (SCXA)
Detected in 86 experiment(s), a significant marker in 62.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-CURD-79 | yes | 10163.25 |
| E-GEOD-93593 | yes | 8469.28 |
| E-HCAD-5 | yes | 8004.44 |
| E-MTAB-9435 | yes | 7930.46 |
| E-HCAD-25 | yes | 7630.57 |
| E-MTAB-5061 | yes | 7458.31 |
| E-HCAD-10 | yes | 7367.84 |
| E-CURD-112 | yes | 6004.52 |
| E-GEOD-135922 | yes | 5995.98 |
| E-HCAD-6 | yes | 5977.90 |
| E-HCAD-4 | yes | 5875.48 |
| E-GEOD-114530 | yes | 5448.15 |
| E-MTAB-10662 | yes | 5413.25 |
| E-MTAB-7407 | yes | 5377.63 |
| E-MTAB-10432 | yes | 5200.38 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): PPARA, RORA
miRNA regulators (miRDB)
27 targeting TUBA1B, 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-3134 | 100.00 | 66.43 | 777 |
| HSA-MIR-223-3P | 99.99 | 70.14 | 1140 |
| HSA-MIR-4534 | 99.99 | 66.58 | 1907 |
| HSA-MIR-3148 | 99.97 | 75.06 | 6478 |
| HSA-MIR-3688-3P | 99.97 | 72.02 | 2834 |
| HSA-MIR-570-3P | 99.96 | 72.41 | 4910 |
| HSA-MIR-8082 | 99.95 | 67.27 | 1170 |
| HSA-MIR-6124 | 99.87 | 69.78 | 3551 |
| HSA-MIR-10395-5P | 99.86 | 67.35 | 676 |
| HSA-MIR-3617-5P | 99.75 | 69.41 | 1968 |
| HSA-MIR-641 | 99.75 | 69.35 | 1975 |
| HSA-MIR-4802-3P | 99.72 | 70.13 | 1273 |
| HSA-MIR-6132 | 99.60 | 65.83 | 1554 |
| HSA-MIR-6836-5P | 99.60 | 65.62 | 1538 |
| HSA-MIR-4643 | 99.49 | 67.63 | 1791 |
| HSA-MIR-569 | 99.42 | 66.32 | 1009 |
| HSA-MIR-1272 | 99.34 | 68.79 | 878 |
| HSA-MIR-6797-3P | 99.17 | 66.94 | 668 |
| HSA-MIR-10399-5P | 99.17 | 69.87 | 2610 |
| HSA-MIR-6504-3P | 99.17 | 69.31 | 2891 |
| HSA-MIR-4717-3P | 99.06 | 66.34 | 1072 |
| HSA-MIR-6076 | 98.61 | 65.69 | 637 |
| HSA-MIR-1322 | 97.98 | 68.96 | 625 |
| HSA-MIR-4314 | 97.50 | 67.30 | 1369 |
| HSA-MIR-6895-5P | 97.05 | 64.96 | 522 |
| HSA-MIR-3192-5P | 96.98 | 65.76 | 1926 |
| HSA-MIR-3918 | 96.13 | 64.65 | 1300 |
Functional genomics
DepMap (CRISPR cell-line fitness): dependent in 93.0% of screened cell lines, common-essential.
Literature-anchored findings (GeneRIF, showing 29)
- increased levels in paclitaxel-resistant breast cancer cells (PMID:12054644)
- Candidate gene K-ALPHA-1 expression in malignant and non-malignant prostate tissue samples after microdissection. (PMID:17628775)
- accumulation of alpha-synuclein might contribute to the pathogenesis of PD and other Lewy body diseases by promoting alterations in parkin and tubulin solubility (PMID:18195004)
- N-terminal sequencing and blastx analysis as well as blocking with K-alpha1 tubulin-specific Ab identified the epithelial Ag as K-alpha1 tubulin[K-alpha1 tubulin] (PMID:18354170)
- mitochondrial ribosomal protein S12 3’-UTR interacts specifically with TRAP1 (tumor necrosis factor receptor-associated protein1), hnRNPM4 (heterogeneous nuclear ribonucleoprotein M4), Hsp70 and Hsp60 (heat shock proteins 70 and 60), and alpha-tubulin (PMID:18790094)
- These results imply that MeCP2 is involved in the regulation of neuronal alpha-tubulin and add molecular evidence that reversal of the effects of MeCP2 deficiency is achievable (PMID:19174478)
- Increased expression of centrosomal TUBA1B in atypical ductal hyperplasia and carcinoma of the breast is reported. (PMID:19215229)
- This protein has been found differentially expressed in the Wernicke’s Area from patients with schizophrenia. (PMID:19405953)
- alpha-tubulin interacted with ARL7. (PMID:19409876)
- Data show that 4-oxo-4-HPR inhibited tubulin polymerization and modulated gene expression of spindle aberration associated genes Kif 1C, Kif 2A, Eg5, Tara, tankyrase-1, centractin, and TOGp. (PMID:19996280)
- Confocal microscopic analyses showed co-localization of the TaSP protein with alpha-tubulin and reciprocal immuno-co-precipitation experiments demonstrated an association of TaSP with alpha-tubulin in vivo. (PMID:20162433)
- the ethyl acetate extract of Lactuca sativa induced HL-60 cell death, which correlated with the acetylation of alpha-tubulin. (PMID:20204303)
- This protein has been found differentially expressed in the anterior cingulate cortex from patients with schizophrenia (PMID:20381070)
- TQ induced a concentration- and time-dependent degradation of alpha/beta tubulin in both cancer cell types. (PMID:21881916)
- ARHGAP21 is a Rho-GAP involved in cell-cell junction remodeling that affects migration and EMT through alpha-tubulin interaction and acetylation (PMID:23235160)
- Increased TUBA1B expression is associated with poor overall survival in hepatocellular carcinoma. (PMID:23625295)
- Data indicate that the derivatives exhibited much better potency to inhibit tubulin polymerization but a decreased activity to inhibit Hsp27 chaperone function. (PMID:23767669)
- Results suggest that lithium chloride (LiCl) treatments activate alpha-tubulin N-acetyltransferase 1 (alphaTAT1) by the inhibition of glycogen synthase kinase 3 beta (GSK-3beta) and promote the alpha-tubulin acetylation, and then elongate the primary cilia. (PMID:24760594)
- NAD-dependent regulation of alpha-tubulin acetylation is mediated by SIRT2. (PMID:24814981)
- TUBA1B/ESR1 gene interaction might play pivotal roles in the occurrence and development of Postmenopausal Osteoporosis. (PMID:26676054)
- Taken together our data provide valuable information regarding the interaction of CK1delta and a-tubulin and a novel approach for the development of pharmacological tools to inhibit proliferation of cancer cells. (PMID:26996302)
- Data show that retinal endothelial cells (HREC) treated with low molecular weight fraction of commercial 5% human serum albumin (LMWF5A) exhibit a rapid increase in the amount and distribution of acetylated alpha-tubulin. (PMID:27613088)
- The C-terminal tail from the tubulin beta I isotype, but not the beta III isotype, formed contacts in the putative binding site of a recently discovered antineoplastic peptide that disrupts microtubule formation in glioma cells. (PMID:28290671)
- Structure of spastin bound to a glutamate-rich peptide implies a hand-over-hand mechanism of substrate translocation. (PMID:31767681)
- The Expression and Potential Role of Tubulin Alpha 1b in Wilms’ Tumor. (PMID:32908931)
- Lower levels of tubulin alpha 1b in the frontal pole in schizophrenia supports a role for changed cytoskeletal dynamics in the aetiology of the disorder. (PMID:34274903)
- Dynamic Network Biomarker of Pre-Exhausted CD8(+) T Cells Contributed to T Cell Exhaustion in Colorectal Cancer. (PMID:34434188)
- Integrated regulation of tubulin tyrosination and microtubule stability by human alpha-tubulin isotypes. (PMID:37379209)
- Tubulin Alpha-1b as a Potential Biomarker for Lung Adenocarcinoma Diagnosis and Prognosis. (PMID:37489256)
Cross-species orthologs
4 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| mus_musculus | Tuba1b | ENSMUSG00000023004 |
| rattus_norvegicus | Tuba1b | ENSRNOG00000072536 |
| drosophila_melanogaster | alphaTub84B | FBGN0003884 |
| drosophila_melanogaster | alphaTub84D | FBGN0003885 |
Paralogs (23): TUBG2 (ENSG00000037042), TUBE1 (ENSG00000074935), TUBA3D (ENSG00000075886), TUBB1 (ENSG00000101162), TUBB4A (ENSG00000104833), TUBD1 (ENSG00000108423), TUBA4A (ENSG00000127824), TUBG1 (ENSG00000131462), TUBB2A (ENSG00000137267), TUBB2B (ENSG00000137285), TUBA3E (ENSG00000152086), TUBA1A (ENSG00000167552), TUBA1C (ENSG00000167553), TUBB8B (ENSG00000173213), TUBB6 (ENSG00000176014), TUBAL3 (ENSG00000178462), TUBA8 (ENSG00000183785), TUBB4B (ENSG00000188229), TUBB (ENSG00000196230), TUBA3C (ENSG00000198033), TUBA4B (ENSG00000243910), TUBB3 (ENSG00000258947), TUBB8 (ENSG00000261456)
Protein
Protein identifiers
Tubulin alpha-1B chain — P68363 (reviewed: P68363)
Alternative names: Alpha-tubulin ubiquitous, Tubulin K-alpha-1, Tubulin alpha-ubiquitous chain
All UniProt accessions (6): P68363, F8VRK0, F8VU66, F8VVB9, F8VWV9, F8VX09
UniProt curated annotations — full annotation on UniProt →
Function. Tubulin is the major constituent of microtubules, protein filaments consisting of alpha- and beta-tubulin heterodimers. Microtubules grow by the addition of GTP-tubulin dimers to the microtubule end, where a stabilizing cap forms. Below the cap, tubulin dimers are in GDP-bound state, owing to GTPase activity of alpha-tubulin.
Subunit / interactions. Heterodimer of alpha- and beta-tubulin. A typical microtubule is a hollow water-filled tube with an outer diameter of 25 nm and an inner diameter of 15 nM. Alpha-beta heterodimers associate head-to-tail to form protofilaments running lengthwise along the microtubule wall with the beta-tubulin subunit facing the microtubule plus end conferring a structural polarity. Microtubules usually have 13 protofilaments but different protofilament numbers can be found in some organisms and specialized cells. Interacts with gamma-tubulin; the interaction allows microtubules to nucleate from the gamma-tubulin ring complex (gTuRC). Nascent microtubule interacts (via alpha-tubulin MREC motif) with TTC5/STRAP; this interaction may result in tubulin mRNA-targeted degradation. Component of sperm flagellar doublet microtubules.
Subcellular location. Cytoplasm. Cytoskeleton.
Post-translational modifications. Some glutamate residues at the C-terminus are polyglutamylated, resulting in polyglutamate chains on the gamma-carboxyl group. Polyglutamylation plays a key role in microtubule severing by spastin (SPAST). SPAST preferentially recognizes and acts on microtubules decorated with short polyglutamate tails: severing activity by SPAST increases as the number of glutamates per tubulin rises from one to eight, but decreases beyond this glutamylation threshold. Glutamylation is also involved in cilia motility. Some glutamate residues at the C-terminus are monoglycylated but not polyglycylated due to the absence of functional TTLL10 in human. Monoglycylation is mainly limited to tubulin incorporated into cilia and flagella axonemes, which is required for their stability and maintenance. Flagella glycylation controls sperm motility. Both polyglutamylation and monoglycylation can coexist on the same protein on adjacent residues, and lowering glycylation levels increases polyglutamylation, and reciprocally. Acetylation of alpha chains at Lys-40 is located inside the microtubule lumen. This modification has been correlated with increased microtubule stability, intracellular transport and ciliary assembly. Methylation of alpha chains at Lys-40 is found in mitotic microtubules and is required for normal mitosis and cytokinesis contributing to genomic stability. Nitration of Tyr-451 is irreversible and interferes with normal dynein intracellular distribution. Undergoes a tyrosination/detyrosination cycle, the cyclic removal and re-addition of a C-terminal tyrosine residue by the enzymes tubulin tyrosine carboxypeptidase (MATCAP1/KIAA0895L, VASH1 or VASH2) and tubulin tyrosine ligase (TTL), respectively. Tyrosination promotes microtubule interaction with CAP-Gly domain-containing proteins such as CLIP1, CLIP2 and DCTN1. Tyrosination regulates the initiation of dynein-dynactin motility via interaction with DCTN1, which brings the dynein-dynactin complex into contact with microtubules. In neurons, tyrosinated tubulins mediate the initiation of retrograde vesicle transport. Detyrosination is involved in metaphase plate congression by guiding chromosomes during mitosis: detyrosination promotes interaction with CENPE, promoting pole-proximal transport of chromosomes toward the equator. Detyrosination increases microtubules-dependent mechanotransduction in dystrophic cardiac and skeletal muscle. In cardiomyocytes, detyrosinated microtubules are required to resist to contractile compression during contraction: detyrosination promotes association with desmin (DES) at force-generating sarcomeres, leading to buckled microtubules and mechanical resistance to contraction.
Domain organisation. The MREC motif mediates interaction with TTC5/STRAP and may be critical for tubulin autoregulation.
Induction. Autoregulated by feedback control of mRNA degradation. In excess of soluble tubulin, TTC5/STRAP cofactor triggers cotranslation degradation of tubulin mRNA.
Similarity. Belongs to the tubulin family.
Isoforms (2)
| UniProt ID | Names | Canonical? |
|---|---|---|
| P68363-1 | 1 | yes |
| P68363-2 | 2 |
RefSeq proteins (1): NP_006073* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000217 | Tubulin | Family |
| IPR002452 | Alpha_tubulin | Family |
| IPR003008 | Tubulin_FtsZ_GTPase | Domain |
| IPR008280 | Tub_FtsZ_C | Homologous_superfamily |
| IPR017975 | Tubulin_CS | Conserved_site |
| IPR018316 | Tubulin/FtsZ_2-layer-sand-dom | Domain |
| IPR023123 | Tubulin_C | Homologous_superfamily |
| IPR036525 | Tubulin/FtsZ_GTPase_sf | Homologous_superfamily |
| IPR037103 | Tubulin/FtsZ-like_C | Homologous_superfamily |
Pfam: PF00091, PF03953
Catalyzed reactions (Rhea), 1 shown:
- GTP + H2O = GDP + phosphate + H(+) (RHEA:19669)
UniProt features (95 total): helix 24, strand 21, binding site 18, modified residue 10, turn 6, sequence conflict 4, mutagenesis site 3, chain 2, cross-link 2, region of interest 1, site 1, short sequence motif 1, splice variant 1, active site 1
Structure
Experimental structures (PDB)
39 structures, top 30 by resolution.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 6S8L | X-RAY DIFFRACTION | 1.8 |
| 6J8O | X-RAY DIFFRACTION | 1.85 |
| 7PJF | X-RAY DIFFRACTION | 1.86 |
| 6J4V | X-RAY DIFFRACTION | 2.1 |
| 8VT7 | ELECTRON MICROSCOPY | 2.66 |
| 7Z6S | ELECTRON MICROSCOPY | 2.9 |
| 8V2J | ELECTRON MICROSCOPY | 2.9 |
| 9COC | ELECTRON MICROSCOPY | 2.9 |
| 9BP6 | ELECTRON MICROSCOPY | 3.1 |
| 9CMM | ELECTRON MICROSCOPY | 3.1 |
| 7LXB | ELECTRON MICROSCOPY | 3.26 |
| 9HQ4 | ELECTRON MICROSCOPY | 3.28 |
| 7M18 | ELECTRON MICROSCOPY | 3.38 |
| 6E7B | ELECTRON MICROSCOPY | 3.5 |
| 6I2I | ELECTRON MICROSCOPY | 3.6 |
| 7SJ8 | ELECTRON MICROSCOPY | 3.6 |
| 7ZCW | ELECTRON MICROSCOPY | 3.6 |
| 8T42 | ELECTRON MICROSCOPY | 3.6 |
| 8U3Z | ELECTRON MICROSCOPY | 3.6 |
| 9F3B | ELECTRON MICROSCOPY | 3.6 |
| 6E7C | ELECTRON MICROSCOPY | 3.65 |
| 5IJ9 | ELECTRON MICROSCOPY | 3.7 |
| 6QUS | ELECTRON MICROSCOPY | 3.7 |
| 6QVE | ELECTRON MICROSCOPY | 3.7 |
| 5IJ0 | ELECTRON MICROSCOPY | 3.8 |
| 6QUY | ELECTRON MICROSCOPY | 3.8 |
| 6QVJ | ELECTRON MICROSCOPY | 3.8 |
| 7SJ7 | ELECTRON MICROSCOPY | 3.8 |
| 7SJ9 | ELECTRON MICROSCOPY | 3.8 |
| 7SJA | ELECTRON MICROSCOPY | 3.8 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P68363-F1 | 91.85 | 0.84 |
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 (2): 451 (involved in polymerization); 254
Ligand- & substrate-binding residues (18): 71; 99; 140; 143; 144; 145; 146; 179; 183; 206; 224; 228 …
Post-translational modifications (12): 40, 40, 48, 232, 282, 339, 439, 443, 445, 451, 326, 370
Mutagenesis-validated functional residues (3):
| Position | Phenotype |
|---|---|
| 254 | abolished gtpase activity; microtubules have an expanded lattice with a negative twist and display high binding to micro |
| 254 | promotes microtubule nucleation efficiency and slows gtp hydrolysis. |
| 254 | abolished gtpase activity; microtubules have an expanded lattice with a positive twist and display low binding to microt |
Function
Pathways and Gene Ontology
Reactome pathways
87 pathways
| ID | Pathway |
|---|---|
| R-HSA-1445148 | Translocation of SLC2A4 (GLUT4) to the plasma membrane |
| R-HSA-190840 | Microtubule-dependent trafficking of connexons from Golgi to the plasma membrane |
| R-HSA-190861 | Gap junction assembly |
| R-HSA-2132295 | MHC class II antigen presentation |
| R-HSA-2467813 | Separation of Sister Chromatids |
| R-HSA-2500257 | Resolution of Sister Chromatid Cohesion |
| R-HSA-3371497 | HSP90 chaperone cycle for steroid hormone receptors (SHR) in the presence of ligand |
| R-HSA-380320 | Recruitment of NuMA to mitotic centrosomes |
| R-HSA-389960 | Formation of tubulin folding intermediates by CCT/TriC |
| R-HSA-389977 | Post-chaperonin tubulin folding pathway |
| R-HSA-437239 | Recycling pathway of L1 |
| R-HSA-5610787 | Hedgehog ‘off’ state |
| R-HSA-5620920 | Cargo trafficking to the periciliary membrane |
| R-HSA-5620924 | Intraflagellar transport |
| R-HSA-5626467 | RHO GTPases activate IQGAPs |
| R-HSA-5663220 | RHO GTPases Activate Formins |
| R-HSA-6807878 | COPI-mediated anterograde transport |
| R-HSA-6811434 | COPI-dependent Golgi-to-ER retrograde traffic |
| R-HSA-6811436 | COPI-independent Golgi-to-ER retrograde traffic |
| R-HSA-68877 | Mitotic Prometaphase |
| R-HSA-8852276 | The role of GTSE1 in G2/M progression after G2 checkpoint |
| R-HSA-8955332 | Carboxyterminal post-translational modifications of tubulin |
| R-HSA-9013407 | RHOH GTPase cycle |
| R-HSA-9609690 | HCMV Early Events |
| R-HSA-9609736 | Assembly and cell surface presentation of NMDA receptors |
| R-HSA-9619483 | Activation of AMPK downstream of NMDARs |
| R-HSA-9646399 | Aggrephagy |
| R-HSA-9648025 | EML4 and NUDC in mitotic spindle formation |
| R-HSA-9668328 | Sealing of the nuclear envelope (NE) by ESCRT-III |
| R-HSA-983189 | Kinesins |
MSigDB gene sets: 377 (showing top):
HONMA_DOCETAXEL_RESISTANCE, REACTOME_ADAPTIVE_IMMUNE_SYSTEM, REACTOME_CYTOKINE_SIGNALING_IN_IMMUNE_SYSTEM, GOBP_RESPONSE_TO_INTERLEUKIN_4, GOBP_RESPONSE_TO_PEPTIDE, MORF_UBE2I, MATTIOLI_MGUS_VS_PCL, PID_PRL_SIGNALING_EVENTS_PATHWAY, THEILGAARD_NEUTROPHIL_AT_SKIN_WOUND_DN, WEIGEL_OXIDATIVE_STRESS_BY_TBH_AND_H2O2, GOBP_NEUROGENESIS, REACTOME_MEMBRANE_TRAFFICKING, PUJANA_CHEK2_PCC_NETWORK, SHETH_LIVER_CANCER_VS_TXNIP_LOSS_PAM1, GROSS_ELK3_TARGETS_UP
GO Biological Process (7): microtubule cytoskeleton organization (GO:0000226), mitotic cell cycle (GO:0000278), microtubule-based process (GO:0007017), cytoskeleton-dependent intracellular transport (GO:0030705), cell division (GO:0051301), cellular response to interleukin-4 (GO:0071353), cytoskeleton organization (GO:0007010)
GO Molecular Function (9): double-stranded RNA binding (GO:0003725), GTPase activity (GO:0003924), structural molecule activity (GO:0005198), structural constituent of cytoskeleton (GO:0005200), GTP binding (GO:0005525), ubiquitin protein ligase binding (GO:0031625), nucleotide binding (GO:0000166), protein binding (GO:0005515), hydrolase activity (GO:0016787)
GO Cellular Component (6): cytoplasm (GO:0005737), microtubule (GO:0005874), cytoplasmic microtubule (GO:0005881), cilium (GO:0005929), microtubule cytoskeleton (GO:0015630), cytoskeleton (GO:0005856)
Reactome top-level categories
Rollup of top-16 pathways:
| Category | Pathways |
|---|---|
| Mitotic Prometaphase | 2 |
| Assembly of the 9+0 primary cilium | 2 |
| RHO GTPase Effectors | 2 |
| Golgi-to-ER retrograde transport | 2 |
| Membrane Trafficking | 1 |
| Transport of connexons to the plasma membrane | 1 |
| Gap junction trafficking | 1 |
| Adaptive Immune System | 1 |
| Mitotic Anaphase | 1 |
| Cellular responses to stress | 1 |
| Cooperation of Prefoldin and TriC/CCT in actin and tubulin folding | 1 |
| Protein folding | 1 |
| L1CAM interactions | 1 |
| Signaling by Hedgehog | 1 |
| ER to Golgi Anterograde Transport | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| cytoskeleton organization | 2 |
| cellular process | 2 |
| cytoskeleton | 2 |
| microtubule-based process | 1 |
| cell cycle | 1 |
| mitotic nuclear division | 1 |
| intracellular transport | 1 |
| response to interleukin-4 | 1 |
| cellular response to cytokine stimulus | 1 |
| organelle organization | 1 |
| RNA binding | 1 |
| ribonucleoside triphosphate phosphatase activity | 1 |
| molecular_function | 1 |
| structural molecule activity | 1 |
| guanyl ribonucleotide binding | 1 |
| purine ribonucleoside triphosphate binding | 1 |
| ubiquitin-like protein ligase binding | 1 |
| nucleoside phosphate binding | 1 |
| heterocyclic compound binding | 1 |
| binding | 1 |
| catalytic activity | 1 |
| intracellular anatomical structure | 1 |
| cellular anatomical structure | 1 |
| microtubule cytoskeleton | 1 |
| polymeric cytoskeletal fiber | 1 |
| cytoplasm | 1 |
| microtubule | 1 |
| intraciliary transport particle | 1 |
| membrane-bounded organelle | 1 |
| plasma membrane bounded cell projection | 1 |
| intracellular membraneless organelle | 1 |
Protein interactions and networks
STRING
0 interactions, top by confidence (×1000):
IntAct
215 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| STAG2 | RAD21 | psi-mi:“MI:0914”(association) | 0.970 |
| EHMT2 | WIZ | psi-mi:“MI:0914”(association) | 0.730 |
| MTMR2 | CCDC22 | psi-mi:“MI:0914”(association) | 0.730 |
| CCT2 | TXNDC9 | psi-mi:“MI:0914”(association) | 0.730 |
| CFTR | ESYT2 | psi-mi:“MI:2364”(proximity) | 0.710 |
| TUBB3 | TUBA1B | psi-mi:“MI:0914”(association) | 0.660 |
| TUBA1B | TXNDC9 | psi-mi:“MI:0914”(association) | 0.640 |
| MAPK7 | PFDN6 | psi-mi:“MI:0914”(association) | 0.640 |
| ATXN7L3 | USP27X | psi-mi:“MI:0914”(association) | 0.640 |
| KDM5A | SIN3B | psi-mi:“MI:0914”(association) | 0.640 |
| LIN28A | IGF2BP3 | psi-mi:“MI:0914”(association) | 0.640 |
| NCBP1 | KPNA3 | psi-mi:“MI:0914”(association) | 0.640 |
| CCT3 | TXNDC9 | psi-mi:“MI:0914”(association) | 0.640 |
| CCT5 | TXNDC9 | psi-mi:“MI:0914”(association) | 0.640 |
| THOC1 | DDX39A | psi-mi:“MI:0914”(association) | 0.640 |
| TUBA1B | AGTRAP | psi-mi:“MI:0915”(physical association) | 0.560 |
| AGTRAP | TUBA1B | psi-mi:“MI:0915”(physical association) | 0.560 |
| APP | TUBA1B | psi-mi:“MI:0915”(physical association) | 0.560 |
| SNCA | TUBA1B | psi-mi:“MI:0915”(physical association) | 0.560 |
| MAP2K2 | BAG2 | psi-mi:“MI:0914”(association) | 0.530 |
| KDM6A | KMT2D | psi-mi:“MI:0914”(association) | 0.530 |
| PPP2R2B | DDX3X | psi-mi:“MI:0914”(association) | 0.460 |
BioGRID (644): TUBA1B (Affinity Capture-MS), AGTRAP (Two-hybrid), MTCL1 (Reconstituted Complex), TUBA1B (Affinity Capture-MS), TUBA1B (Affinity Capture-MS), TUBA1B (Affinity Capture-MS), TUBA1B (Affinity Capture-MS), TUBA1B (Affinity Capture-MS), TUBA1B (Affinity Capture-MS), TUBA1B (Reconstituted Complex), TUBA1B (Affinity Capture-MS), TUBA1B (Reconstituted Complex), TUBA1B (Biochemical Activity), TUBA1B (Affinity Capture-MS), TUBA1B (Affinity Capture-MS)
ESM2 similar proteins: A5A6J1, P02550, P02552, P05213, P05214, P06603, P06604, P06605, P08537, P09644, P0DPH7, P0DPH8, P18258, P18288, P30436, P34690, P36220, P41383, P52273, P68360, P68361, P68362, P68363, P68365, P68366, P68367, P68368, P68369, P68370, P68373, P81947, P81948, Q06331, Q28IX8, Q2HJ86, Q2XVP4, Q32KN8, Q3ZCJ7, Q4R538, Q52PV9
Diamond homologs: A0AAL4, A5A6J1, B9DGT7, B9DHQ0, O22347, O22348, O22349, P02550, P02552, P04105, P04106, P05213, P05214, P06603, P06604, P08537, P09204, P09205, P09243, P0DPH7, P0DPH8, P10872, P10873, P11139, P11237, P11480, P11481, P12543, P14640, P14641, P14642, P18258, P18288, P22275, P28268, P28287, P28752, P29511, P30436, P32255
SIGNOR signaling
6 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| NUMA1 | up-regulates | TUBA1B | binding |
| TTL | down-regulates | TUBA1B | tyrosination |
| SETD2 | “up-regulates activity” | TUBA1B | methylation |
| “Elongator complex” | “up-regulates activity” | TUBA1B | acetylation |
| TUBA1B | up-regulates | Neuron_migration | |
| ATAT1 | “up-regulates quantity by stabilization” | TUBA1B | acetylation |
Enriched among interaction partners
Reactome pathways and GO biological processes over-represented among this gene’s 258 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 |
|---|---|---|---|
| Prefoldin mediated transfer of substrate to CCT/TriC | 8 | 18.3× | 8e-06 |
| Formation of tubulin folding intermediates by CCT/TriC | 6 | 14.8× | 1e-03 |
| Cooperation of Prefoldin and TriC/CCT in actin and tubulin folding | 6 | 14.2× | 1e-03 |
| Dengue Virus Genome Translation and Replication | 6 | 11.1× | 3e-03 |
| Chaperonin-mediated protein folding | 6 | 10.5× | 3e-03 |
| Aggrephagy | 7 | 10.1× | 1e-03 |
| FCERI mediated MAPK activation | 5 | 10.1× | 7e-03 |
| Protein folding | 6 | 9.1× | 4e-03 |
GO biological processes:
| GO term | Partners | Fold | FDR |
|---|---|---|---|
| protein folding | 12 | 5.5× | 3e-03 |
Disease & clinical
Clinical variants and AI predictions
ClinVar
23 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 4 |
| Likely benign | 1 |
| Benign | 4 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
376 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 12:49128935:CAGC:C | acceptor_gain | 1.0000 |
| 12:49128937:GC:G | acceptor_gain | 1.0000 |
| 12:49128937:GCCTG:G | acceptor_loss | 1.0000 |
| 12:49128938:CC:C | acceptor_gain | 1.0000 |
| 12:49128938:CCTG:C | acceptor_loss | 1.0000 |
| 12:49128939:C:CC | acceptor_gain | 1.0000 |
| 12:49129236:GCTTA:G | donor_loss | 1.0000 |
| 12:49129237:CTTA:C | donor_loss | 1.0000 |
| 12:49129238:TTAC:T | donor_loss | 1.0000 |
| 12:49129239:TACC:T | donor_loss | 1.0000 |
| 12:49129240:A:AC | donor_gain | 1.0000 |
| 12:49129240:AC:A | donor_gain | 1.0000 |
| 12:49129240:ACCA:A | donor_loss | 1.0000 |
| 12:49129240:ACCAG:A | donor_gain | 1.0000 |
| 12:49129241:C:CG | donor_gain | 1.0000 |
| 12:49129241:CC:C | donor_gain | 1.0000 |
| 12:49129241:CCA:C | donor_gain | 1.0000 |
| 12:49129241:CCAG:C | donor_gain | 1.0000 |
| 12:49129241:CCAGC:C | donor_gain | 1.0000 |
| 12:49129386:TTCAT:T | acceptor_gain | 1.0000 |
| 12:49129387:TCAT:T | acceptor_gain | 1.0000 |
| 12:49129387:TCATC:T | acceptor_gain | 1.0000 |
| 12:49129388:CAT:C | acceptor_gain | 1.0000 |
| 12:49129388:CATC:C | acceptor_gain | 1.0000 |
| 12:49129388:CATCT:C | acceptor_gain | 1.0000 |
| 12:49129389:AT:A | acceptor_gain | 1.0000 |
| 12:49129389:ATCTG:A | acceptor_gain | 1.0000 |
| 12:49129390:TCTGG:T | acceptor_gain | 1.0000 |
| 12:49129391:C:CC | acceptor_gain | 1.0000 |
| 12:49129391:CT:C | acceptor_gain | 1.0000 |
AlphaMissense
2975 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 12:49128023:C:G | D431H | 1.000 |
| 12:49128031:A:G | L428P | 1.000 |
| 12:49128031:A:T | L428H | 1.000 |
| 12:49128035:C:G | A427P | 1.000 |
| 12:49128049:C:G | R422P | 1.000 |
| 12:49128050:G:T | R422S | 1.000 |
| 12:49128052:G:T | A421D | 1.000 |
| 12:49128053:C:G | A421P | 1.000 |
| 12:49128060:A:C | F418L | 1.000 |
| 12:49128060:A:T | F418L | 1.000 |
| 12:49128061:A:C | F418C | 1.000 |
| 12:49128061:A:G | F418S | 1.000 |
| 12:49128062:A:G | F418L | 1.000 |
| 12:49128068:C:G | G416R | 1.000 |
| 12:49128076:A:G | M413T | 1.000 |
| 12:49128080:C:A | G412W | 1.000 |
| 12:49128080:C:G | G412R | 1.000 |
| 12:49128080:C:T | G412R | 1.000 |
| 12:49128095:A:G | W407R | 1.000 |
| 12:49128095:A:T | W407R | 1.000 |
| 12:49128098:G:C | H406D | 1.000 |
| 12:49128100:A:T | V405D | 1.000 |
| 12:49128102:A:C | F404L | 1.000 |
| 12:49128102:A:T | F404L | 1.000 |
| 12:49128103:A:C | F404C | 1.000 |
| 12:49128103:A:G | F404S | 1.000 |
| 12:49128104:A:G | F404L | 1.000 |
| 12:49128104:A:T | F404I | 1.000 |
| 12:49128106:G:T | A403D | 1.000 |
| 12:49128109:C:G | R402P | 1.000 |
dbSNP variants (sampled 300 via entrez): RS1000230147 (12:49129908 G>A,T), RS1001196149 (12:49132527 A>C), RS1001642284 (12:49128994 T>C), RS1003255509 (12:49127524 G>A,C,T), RS1003470056 (12:49132695 G>T), RS1004301572 (12:49127297 T>C), RS1005694818 (12:49130140 G>A), RS1005719741 (12:49130224 C>G), RS1006311457 (12:49131372 A>C,G), RS1007110807 (12:49131199 A>C), RS1007272084 (12:49133080 A>C,G), RS1007660054 (12:49132710 C>A,T), RS1008039303 (12:49127795 GACTTT>G), RS1009254572 (12:49132624 A>G), RS1009303739 (12:49132263 G>A)
Disease associations
OMIM: gene MIM:602530 | disease phenotypes: MIM:135700
GenCC curated gene-disease
Mondo (2): congenital fibrosis of extraocular muscles (MONDO:0007614), neuromuscular disease (MONDO:0019056)
Orphanet (2): Congenital fibrosis of extraocular muscles (Orphanet:45358), Neuromuscular disease (Orphanet:68381)
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
5 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST008103_109 | Bipolar disorder | 4.000000e-06 |
| GCST010703_9 | Brain morphology (MOSTest) | 8.000000e-10 |
| GCST90010427_15 | Left–right brain asymmetry | 1.000000e-11 |
| GCST90013420_4 | Ambidextrousness | 1.000000e-09 |
| GCST90013421_10 | Left-handedness | 2.000000e-10 |
EFO canonical traits (2, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0004346 | neuroimaging measurement |
| EFO:0009902 | handedness |
MeSH disease descriptors (2)
| Descriptor | Name | Tree numbers |
|---|---|---|
| D009468 | Neuromuscular Diseases | C10.668 |
| C580012 | congenital fibrosis of the extraocular muscles (supp.) |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (4): CHEMBL2095182 (PROTEIN COMPLEX GROUP), CHEMBL3797010 (SINGLE PROTEIN), CHEMBL3832941 (PROTEIN FAMILY), CHEMBL6067579 (PROTEIN-PROTEIN INTERACTION)
Molecules with ChEMBL bioactivity
21 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 1,641,397 (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 |
|---|---|---|---|
| CHEMBL107 | COLCHICINE | 4 | 93,932 |
| CHEMBL159 | VINBLASTINE | 4 | 412,636 |
| CHEMBL33 | LEVOFLOXACIN ANHYDROUS | 4 | 43,403 |
| CHEMBL3545252 | DOCETAXEL | 4 | 1,009 |
| CHEMBL364713 | NOSCAPINE | 4 | 14,987 |
| CHEMBL378544 | VINBLASTINE SULFATE | 4 | 32,829 |
| CHEMBL428647 | PACLITAXEL | 4 | 332,542 |
| CHEMBL5315124 | LEVOFLOXACIN | 4 | 189 |
| CHEMBL553025 | VINORELBINE | 4 | 142,159 |
| CHEMBL571546 | TIRBANIBULIN | 4 | 1,192 |
| CHEMBL61 | PODOFILOX | 4 | 37,640 |
| CHEMBL90555 | VINCRISTINE | 4 | 268,031 |
| CHEMBL92 | DOCETAXEL ANHYDROUS | 4 | 196,686 |
| CHEMBL94657 | PATUPILONE | 3 | 14,934 |
| CHEMBL20684 | ABT-751 | 2 | 2,238 |
| CHEMBL292702 | MAYTANSINE | 2 | 9,300 |
| CHEMBL39541 | DOLASTATIN-10 | 2 | 1,380 |
| CHEMBL49642 | INDIBULIN | 2 | 963 |
| CHEMBL528271 | PARBENDAZOLE | 2 | 6,102 |
| CHEMBL9514 | NOCODAZOLE | 2 | 29,245 |
| CHEMBL246600 | COMBRETASTATIN | 1 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
ChEMBL bioactivities
1163 potent at pChembl≥5 of 1314 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
PubChem BioAssay actives
1090 with measured affinity, of 5781 total; 50 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 |
|---|---|---|---|---|
| (Z)-1-[4-bromo-2-(4-fluorophenyl)-1-benzofuran-7-yl]-3-(4-methoxyphenyl)prop-2-en-1-one | 1882651: Inhibition of tubulin polymerization (unknown origin) measured every 3 secs for 1 hr by spectroflourimetric analysis | ic50 | 0.0001 | uM |
| (Z)-1-[4-bromo-2-(4-fluorophenyl)-1-benzofuran-7-yl]-3-[4-(trifluoromethoxy)phenyl]prop-2-en-1-one | 1882651: Inhibition of tubulin polymerization (unknown origin) measured every 3 secs for 1 hr by spectroflourimetric analysis | ic50 | 0.0002 | uM |
| Vinorelbine | 1993632: Inhibition of tubulin polymerization (unknown origin) | ic50 | 0.0003 | uM |
| (2S)-2-[[(2S)-2-(dimethylamino)-3-methylbutanoyl]amino]-N-[(3R,4S,5S)-3-methoxy-1-[(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-[[(1S)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]amino]propyl]pyrrolidin-1-yl]-5-methyl-1-oxoheptan-4-yl]-N,3-dimethylbutanamide | 270819: Inhibition of tubulin polymerization | ic50 | 0.0005 | uM |
| (2S)-2-[[(2S)-2-(dimethylamino)-3-methylbutanoyl]amino]-N-[(3R,4S,5S)-3-methoxy-1-[(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-(2-pyridin-2-ylethylamino)propyl]pyrrolidin-1-yl]-5-methyl-1-oxoheptan-4-yl]-N,3-dimethylbutanamide | 1896115: Binding affinity to tubulin (unknown origin) | ic50 | 0.0012 | uM |
| (3Z,6Z)-3-[(5-tert-butyl-1H-imidazol-4-yl)methylidene]-6-phenacylidenepiperazine-2,5-dione | 1587857: Inhibition of tubulin polymerization (unknown origin) | ic50 | 0.0014 | uM |
| (3Z,6Z)-3-[(5-tert-butyl-1H-imidazol-4-yl)methylidene]-6-[(2,5-difluorophenyl)methylidene]piperazine-2,5-dione | 1587857: Inhibition of tubulin polymerization (unknown origin) | ic50 | 0.0026 | uM |
| 3-hydroxy-2-[N-[2-(methoxymethyl)-1-benzofuran-7-yl]-C-methylcarbonimidoyl]-5-phenylcyclohex-2-en-1-one | 2034736: Displacement of fluorescent probe (R)-(+)-ethyl 5-amino2-methyl-1,2-dihydro-3-phenylpyrido[3,4-b]pyrazin-7-ylcarbamate from tubulin colchicine binding site (unknown origin) assessed as dissociation constant | kd | 0.0030 | uM |
| 2-methoxy-5-[(Z)-2-(3,4,5-trimethoxyphenyl)ethenyl]phenol | 1862628: Inhibition of tubulin polymerization in human HeLa cells assessed as microtubule network polymerization after 30 mins by immunofluorescence analysis | ic50 | 0.0030 | uM |
| Colchicine | 2074087: Inhibition of microtubule polymerization in human K562 cells measured for 60 mins by fluorescence based analysis | ic50 | 0.0030 | uM |
| (1S,3S,7S,10R,11S,12S,16R)-7,11-dihydroxy-8,8,10,12,16-pentamethyl-3-[(E)-1-(2-methyl-1,3-thiazol-4-yl)prop-1-en-2-yl]-4,17-dioxabicyclo[14.1.0]heptadecane-5,9-dione | 1408257: Inhibition of tubulin polymerization in human MCF7 cells assessed as induction of mitotic arrest | ic50 | 0.0035 | uM |
| tert-butyl (3R,4S,5S)-4-[[(2S)-2-[[(2S)-2-(dimethylamino)-3-methylbutanoyl]amino]-3-methylbutanoyl]-methylamino]-3-methoxy-5-methylheptanoate | 1896110: Inhibition of tubulin (unknown origin) polymerization assessed as reduction in microtubule formation measured for 20 mins by spectrophotometric analysis | ic50 | 0.0042 | uM |
| 3-methoxy-6-[4-(3,4,5-trimethoxyphenyl)-1H-pyrazol-5-yl]benzene-1,2-diol | 1929685: Inhibition of tubulin polymerization in human SH-SY5Y cells incubated for 24 hrs by SDS-PAGE based analysis | ic50 | 0.0054 | uM |
| 2-methoxy-5-[1-(3,4,5-trimethoxyphenyl)ethenyl]phenol | 1862628: Inhibition of tubulin polymerization in human HeLa cells assessed as microtubule network polymerization after 30 mins by immunofluorescence analysis | ic50 | 0.0060 | uM |
| (E)-1-[1-(4-chlorophenyl)-5-methyltriazol-4-yl]-3-(3,4-dimethoxyphenyl)prop-2-en-1-one | 1689700: Inhibition of Tubulin in human RPMI-8226 cells incubated for 2 hrs by ELISA | ic50 | 0.0098 | uM |
| N-(1,3-benzodioxol-5-yl)-5-[2-(3,5-dimethoxyphenoxy)-3-pyridinyl]-1H-1,2,4-triazol-3-amine | 256882: Displacement of [3H]colchicine from tubulin | ki | 0.0100 | uM |
| N-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-[2-(pyridin-2-ylmethylamino)phenyl]-1,3-oxazol-2-amine | 261214: Displacement of [3H]colchicine from tubulin at 65 nM | ic50 | 0.0100 | uM |
| [(1S,2R,3S,5R,6S,16E,18E,20R,21S)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.110,14.03,5]hexacosa-10,12,14(26),16,18-pentaen-6-yl] acetate | 2126113: Displacement of fluorescent Maytansine probe from tubulin (unknown origin) assessed as dissociation constant by competitive binding based fluorescence anisotropy | kd | 0.0110 | uM |
| [(1S,2R,3S,5S,6S,16E,18E,20R,21S)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.110,14.03,5]hexacosa-10,12,14(26),16,18-pentaen-6-yl] (2S)-2-[acetyl(methyl)amino]propanoate | 2126113: Displacement of fluorescent Maytansine probe from tubulin (unknown origin) assessed as dissociation constant by competitive binding based fluorescence anisotropy | kd | 0.0140 | uM |
| N-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-[2-(3,5-dimethoxyphenoxy)-3-pyridinyl]-1H-1,2,4-triazol-3-amine | 256882: Displacement of [3H]colchicine from tubulin | ki | 0.0200 | uM |
| methyl (13S,15S,17S)-13-[(1R,9R,10S,11R,12R,19R)-10-(1-diethoxyphosphorylhexylcarbamoyl)-12-ethyl-10,11-dihydroxy-5-methoxy-8-methyl-8,16-diazapentacyclo[10.6.1.01,9.02,7.016,19]nonadeca-2,4,6,13-tetraen-4-yl]-17-ethyl-17-hydroxy-1,11-diazatetracyclo[13.3.1.04,12.05,10]nonadeca-4(12),5,7,9-tetraene-13-carboxylate | 214333: The compound tested for the inhibition of tubulin polymerization. | ic50 | 0.0200 | uM |
| (E)-3-[5-[(2-cyanoquinolin-4-yl)-methylamino]-2-methoxyphenyl]-N-hydroxyprop-2-enamide | 1862628: Inhibition of tubulin polymerization in human HeLa cells assessed as microtubule network polymerization after 30 mins by immunofluorescence analysis | ic50 | 0.0200 | uM |
| [(1S,2R,3S,5R,6S,16E,18E,20R,21S)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.110,14.03,5]hexacosa-10,12,14(26),16,18-pentaen-6-yl] hept-6-ynoate | 2126113: Displacement of fluorescent Maytansine probe from tubulin (unknown origin) assessed as dissociation constant by competitive binding based fluorescence anisotropy | kd | 0.0200 | uM |
| N-(4-methoxyphenyl)-N,5-dimethylfuro[2,3-d]pyrimidin-4-amine | 1635267: Induction of microtubule depolymerization in human A10 cells incubated for 18 hrs by indirect immunofluorescence analysis | ec50 | 0.0240 | uM |
| (2R,3R)-3-ethyl-2-[(E,2R,3S,4R,5S)-2-hydroxy-4-methoxy-3,5-dimethylnon-7-enyl]-2,3-dihydropyran-6-one | 1572465: Inhibition of tubulin alpha in human A2780 cells assessed as reduction in cell growth | ic50 | 0.0260 | uM |
| N-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-[2-(pyridin-3-ylmethylamino)-3-pyridinyl]-1,3,4-oxadiazol-2-amine | 261214: Displacement of [3H]colchicine from tubulin at 65 nM | ic50 | 0.0300 | uM |
| N-(1,3-benzodioxol-5-yl)-5-[2-(pyridin-4-ylmethylamino)-3-pyridinyl]-1,3,4-oxadiazol-2-amine | 261214: Displacement of [3H]colchicine from tubulin at 65 nM | ic50 | 0.0300 | uM |
| N-(1,3-benzodioxol-5-yl)-5-[2-(pyridin-2-ylmethylamino)-3-pyridinyl]-1,3,4-oxadiazol-2-amine | 261214: Displacement of [3H]colchicine from tubulin at 65 nM | ic50 | 0.0300 | uM |
| Paclitaxel | 260235: Effect on induction of mitotic arrest by phosphohistone H3 (pH3) assay | ec50 | 0.0310 | uM |
| 6-(3-chloro-6,11,11-trioxobenzo[b][1,4]benzothiazepin-5-yl)-N-hydroxyhexanamide | 580932: Inhibition of HDAC activity in human NB4 cells assessed as acetylated tubulin after 24 hrs by Western blot analysis | ec50 | 0.0400 | uM |
| N,5-dimethyl-N-(4-methylsulfanylphenyl)furo[2,3-d]pyrimidin-4-amine | 1635267: Induction of microtubule depolymerization in human A10 cells incubated for 18 hrs by indirect immunofluorescence analysis | ec50 | 0.0450 | uM |
| [7-(3-hydroxyprop-1-ynyl)-6-methoxy-2H-indazol-3-yl]-(3,4,5-trimethoxyphenyl)methanone | 280080: Displacement of [3H]colchicine from tubulin in MCF7 cells | ic50 | 0.0460 | uM |
| (3S,10R,13E,16S)-10-[(3-chloro-4-methoxyphenyl)methyl]-6,6-dimethyl-3-(2-methylpropyl)-16-[(1S)-1-[(2R,3S)-3-phenyloxiran-2-yl]ethyl]-1,4-dioxa-8,11-diazacyclohexadec-13-ene-2,5,9,12-tetrone | 2061859: Binding affinity to tubulin (unknown origin) assessed as dissociation constant by SPR analysis | kd | 0.0470 | uM |
| N-hydroxy-6-(3-methoxy-6,11,11-trioxobenzo[b][1,4]benzothiazepin-5-yl)hexanamide | 580932: Inhibition of HDAC activity in human NB4 cells assessed as acetylated tubulin after 24 hrs by Western blot analysis | ec50 | 0.0500 | uM |
| N-hydroxy-6-(6,11,11-trioxobenzo[b][1,4]benzothiazepin-5-yl)hexanamide | 580932: Inhibition of HDAC activity in human NB4 cells assessed as acetylated tubulin after 24 hrs by Western blot analysis | ec50 | 0.0500 | uM |
| 5-[2-(3,5-dimethoxyphenoxy)-3-pyridinyl]-N-(3-methoxyphenyl)-1H-1,2,4-triazol-3-amine | 256882: Displacement of [3H]colchicine from tubulin | ki | 0.0500 | uM |
| [(1S,2R,3S,5R,6S,16E,18E,20R,21S)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.110,14.03,5]hexacosa-10,12,14(26),16,18-pentaen-6-yl] benzoate | 2126113: Displacement of fluorescent Maytansine probe from tubulin (unknown origin) assessed as dissociation constant by competitive binding based fluorescence anisotropy | kd | 0.0510 | uM |
| N-ethyl-N-(4-methoxyphenyl)-5-methylfuro[2,3-d]pyrimidin-4-amine | 1635267: Induction of microtubule depolymerization in human A10 cells incubated for 18 hrs by indirect immunofluorescence analysis | ec50 | 0.0530 | uM |
| 3-[3-(1,3-benzodioxol-5-ylamino)-1H-1,2,4-triazol-5-yl]-N-(3,5-dimethoxyphenyl)pyridin-2-amine | 256882: Displacement of [3H]colchicine from tubulin | ki | 0.0600 | uM |
| Vinblastine | 214333: The compound tested for the inhibition of tubulin polymerization. | ic50 | 0.0700 | uM |
| methyl (13S,15S,17S)-13-[(1R,9R,10S,11R,12R,19R)-10-[(1-diethoxyphosphoryl-2-phenylethyl)carbamoyl]-12-ethyl-10,11-dihydroxy-5-methoxy-8-methyl-8,16-diazapentacyclo[10.6.1.01,9.02,7.016,19]nonadeca-2,4,6,13-tetraen-4-yl]-17-ethyl-17-hydroxy-1,11-diazatetracyclo[13.3.1.04,12.05,10]nonadeca-4(12),5,7,9-tetraene-13-carboxylate | 214333: The compound tested for the inhibition of tubulin polymerization. | ic50 | 0.0700 | uM |
| N-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-[3-(pyridin-2-ylmethylamino)thiophen-2-yl]-1,3,4-oxadiazol-2-amine | 261214: Displacement of [3H]colchicine from tubulin at 65 nM | ic50 | 0.0750 | uM |
| methyl (13S,15S,17S)-13-[(1R,9R,10S,11R,12R,19R)-10-[[(1S)-1-diethoxyphosphorylethyl]carbamoyl]-12-ethyl-10,11-dihydroxy-5-methoxy-8-methyl-8,16-diazapentacyclo[10.6.1.01,9.02,7.016,19]nonadeca-2,4,6,13-tetraen-4-yl]-17-ethyl-17-hydroxy-1,11-diazatetracyclo[13.3.1.04,12.05,10]nonadeca-4(12),5,7,9-tetraene-13-carboxylate | 214333: The compound tested for the inhibition of tubulin polymerization. | ic50 | 0.0800 | uM |
| 4-methoxy-2-[(Z)-2-(3,4,5-trimethoxyphenyl)ethenyl]thiophene | 1267532: Inhibition of Tubulin polymerization in human HeLa cells assessed as decrease in dynamic tyrosinated microtubules after 2 hrs by microplate reader analysis | ec50 | 0.0810 | uM |
| N-[2-[[(E)-(2,4-dihydroxyphenyl)methylideneamino]carbamoyl]phenyl]furan-2-carboxamide | 1882654: Inhibition of tubulin polymerization (unknown origin) | ic50 | 0.0876 | uM |
| N-hydroxy-6-(3-methoxy-6-oxobenzo[b][1,4]benzoxazepin-5-yl)hexanamide | 580932: Inhibition of HDAC activity in human NB4 cells assessed as acetylated tubulin after 24 hrs by Western blot analysis | ec50 | 0.0900 | uM |
| N-(3,5-dimethoxyphenyl)-3-[3-(3-methoxyanilino)-1H-1,2,4-triazol-5-yl]pyridin-2-amine | 256882: Displacement of [3H]colchicine from tubulin | ki | 0.1000 | uM |
| methyl (13S,15S,17S)-13-[(1R,9R,10S,11R,12R,19R)-10-[[(1R)-1-diethoxyphosphoryl-2-(1H-indol-3-yl)ethyl]carbamoyl]-12-ethyl-10,11-dihydroxy-5-methoxy-8-methyl-8,16-diazapentacyclo[10.6.1.01,9.02,7.016,19]nonadeca-2,4,6,13-tetraen-4-yl]-17-ethyl-17-hydroxy-1,11-diazatetracyclo[13.3.1.04,12.05,10]nonadeca-4(12),5,7,9-tetraene-13-carboxylate | 214333: The compound tested for the inhibition of tubulin polymerization. | ic50 | 0.1000 | uM |
| methyl (13S,15S,17S)-13-[(1R,9R,10S,11R,12R,19R)-10-(1-diethoxyphosphorylethylcarbamoyl)-12-ethyl-10,11-dihydroxy-5-methoxy-8-methyl-8,16-diazapentacyclo[10.6.1.01,9.02,7.016,19]nonadeca-2,4,6,13-tetraen-4-yl]-17-ethyl-17-hydroxy-1,11-diazatetracyclo[13.3.1.04,12.05,10]nonadeca-4(12),5,7,9-tetraene-13-carboxylate | 214333: The compound tested for the inhibition of tubulin polymerization. | ic50 | 0.1000 | uM |
| methyl (13S,15S,17S)-13-[(1R,9R,10S,11R,12R,19R)-10-[[(1S)-1-diethoxyphosphoryl-2-(1H-indol-3-yl)ethyl]carbamoyl]-12-ethyl-10,11-dihydroxy-5-methoxy-8-methyl-8,16-diazapentacyclo[10.6.1.01,9.02,7.016,19]nonadeca-2,4,6,13-tetraen-4-yl]-17-ethyl-17-hydroxy-1,11-diazatetracyclo[13.3.1.04,12.05,10]nonadeca-4(12),5,7,9-tetraene-13-carboxylate | 214333: The compound tested for the inhibition of tubulin polymerization. | ic50 | 0.1000 | uM |
CTD chemical–gene interactions
88 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| sodium arsenite | decreases expression, increases expression | 3 |
| bisphenol A | affects expression, affects cotreatment, decreases expression | 2 |
| perfluorooctanoic acid | affects cotreatment, affects expression, decreases expression | 2 |
| Air Pollutants | affects cotreatment, decreases expression, increases abundance, increases expression | 2 |
| Benzo(a)pyrene | affects methylation, increases expression | 2 |
| Copper | affects binding, decreases expression | 2 |
| Hydrogen Peroxide | affects cotreatment, decreases expression | 2 |
| Silicon Dioxide | decreases acetylation, decreases reaction, affects secretion | 2 |
| Tobacco Smoke Pollution | decreases expression, increases metabolic processing | 2 |
| tert-Butylhydroperoxide | decreases expression | 2 |
| GSK-J4 | decreases expression | 1 |
| FR900359 | affects phosphorylation | 1 |
| bisphenol F | affects cotreatment, decreases expression | 1 |
| ammonium 2,3,3,3-tetrafluoro-2-(heptafluoropropoxy)-propanoate | affects expression, affects cotreatment | 1 |
| beauvericin | increases expression, affects cotreatment | 1 |
| alpha-pinene | affects cotreatment, decreases expression, increases abundance | 1 |
| decabromobiphenyl ether | decreases expression | 1 |
| tris(2-butoxyethyl) phosphate | affects expression | 1 |
| arsenite | affects binding, increases reaction | 1 |
| 2,6-dichloro-4-nitrophenol | increases expression | 1 |
| tris(1,3-dichloro-2-propyl)phosphate | decreases expression | 1 |
| zinc chloride | increases expression | 1 |
| zinc chromate | increases abundance, decreases expression | 1 |
| 4-hydroxy-2-nonenal | affects binding | 1 |
| coumarin | increases phosphorylation | 1 |
| methacrylaldehyde | increases abundance, affects cotreatment, decreases expression | 1 |
| diallyl trisulfide | decreases expression | 1 |
| pinosylvin | decreases expression | 1 |
| cordycepin | affects binding, decreases reaction, decreases expression, affects metabolic processing | 1 |
| di-n-butylphosphoric acid | affects expression | 1 |
ChEMBL screening assays
1689 unique, capped per target: 1648 binding, 35 functional, 6 admet
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1009021 | Binding | Inhibition of tubulin polymerization in human MCF7 cells at 1 uM after 2 hrs by SDS-PAGE | A new cytotoxic epothilone from modified polyketide synthases heterologously expressed in Myxococcus xanthus. — J Nat Prod |
| CHEMBL4146506 | ADMET | Inhibition of tubulin polymerization in human HaCaT cells assessed as chromatin condensation at 1 uM after 24 hrs by Hoechst 33258 staining-based fluorescence microscopic analysis | Design, synthesis, and biological evaluation of novel combretastatin A-4 thio derivatives as microtubule targeting agents. — Eur J Med Chem |
| CHEMBL5056161 | Functional | Inhibition of tubulin polymerization (unknown origin) assessed as fluorescence intensity measured for 90 mins by DAPI based microplate reader | Design, synthesis and biological evaluation of indole-based [1,2,4]triazolo[4,3-a] pyridine derivatives as novel microtubule polymerization inhibitors. — Eur J Med Chem |
Clinical trials (associated diseases)
199 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| NCT00331656 | PHASE4 | UNKNOWN | Comparative Study of Non-Invasive Mask Ventilation vs Cuirass Ventilation in Patients With Acute Respiratory Failure. |
| NCT00994552 | PHASE4 | UNKNOWN | Comparison of Pressure Support and Pressure Control Ventilation in Chronic Respiratory Failure |
| NCT00839033 | PHASE3 | TERMINATED | Evaluation of a Mechanical Device During Acute Respiratory Failure in Patients With Neuromuscular Disorders |
| NCT00942227 | PHASE3 | COMPLETED | The Value of Traction in Treatment of Lumbar Radiculopathy |
| NCT00979108 | PHASE3 | COMPLETED | The Value of Traction in the Treatment of Cervical Radiculopathy |
| NCT01826487 | PHASE3 | COMPLETED | Phase 3 Study of Ataluren in Participants With Nonsense Mutation Duchenne Muscular Dystrophy (nmDMD) |
| NCT02090959 | PHASE3 | TERMINATED | An Extension Study of Ataluren (PTC124) in Participants With Nonsense Mutation Dystrophinopathy |
| NCT02436096 | PHASE3 | COMPLETED | A Study to Evaluate eFFIcacy and Safety of Sublingual TNX-102 SL Tablet Taken at Bedtime in Patients With fibRoMyalgia |
| NCT02829814 | PHASE3 | TERMINATED | Repeat of: A Study to Evaluate Efficacy and Safety of Sublingual TNX-102 SL Tablet Taken at Bedtime in Patients With Fibromyalgia |
| NCT03179631 | PHASE3 | COMPLETED | Long-Term Outcomes of Ataluren in Duchenne Muscular Dystrophy |
| NCT05126758 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study of Deramiocel (CAP-1002) in Ambulatory and Non-Ambulatory Patients With Duchenne Muscular Dystrophy |
| NCT05156320 | PHASE3 | COMPLETED | Efficacy and Safety of Apitegromab in Patients With Later-Onset Spinal Muscular Atrophy Treated With Nusinersen or Risdiplam |
| NCT05337553 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study to Evaluate the Efficacy and Safety of Taldefgrobep Alfa in Participants With Spinal Muscular Atrophy |
| NCT05626855 | PHASE3 | ACTIVE_NOT_RECRUITING | Long-Term Safety & Efficacy of Apitegromab in Patients With SMA Who Completed Previous Trials of Apitegromab |
| NCT06672237 | PHASE3 | RECRUITING | A Phase 3 Study of NTLA-2001 in ATTRv-PN |
| NCT01074359 | PHASE2 | TERMINATED | Safety and Efficacy Study of A0001 in Patients With the A3243G Mitochondrial DNA Point Mutation |
| NCT01371149 | PHASE2 | COMPLETED | Patient -Ventilator Interaction in Chronic Respiratory Failure |
| NCT02022072 | PHASE2 | TERMINATED | Evaluation of Vital Capacity |
| NCT03127514 | PHASE2 | COMPLETED | AMX0035 in Patients With Amyotrophic Lateral Sclerosis (ALS) |
| NCT03406780 | PHASE2 | COMPLETED | A Study of CAP-1002 in Ambulatory and Non-Ambulatory Patients With Duchenne Muscular Dystrophy |
| NCT03921528 | PHASE2 | COMPLETED | An Active Treatment Study of SRK-015 in Patients With Type 2 or Type 3 Spinal Muscular Atrophy |
| NCT05479981 | PHASE2 | COMPLETED | Extension of AOC 1001-CS1 (MARINA) Study in Adult Myotonic Dystrophy Type 1 (DM1) Patients |
| NCT06339580 | PHASE2 | RECRUITING | Assessment of Volume-targeted Ventilation in Patients With Neuromuscular Disease |
| NCT07071935 | PHASE2 | NOT_YET_RECRUITING | A Clinical Trial of Early Ventilation in Amyotrophic Lateral Sclerosis (EVENT ALS) |
| NCT07287189 | PHASE2 | RECRUITING | Phase 2 Study of SAT-3247 in Pediatric Ambulatory Patients |
| NCT00252252 | PHASE1 | COMPLETED | AutoVPAP Versus VPAP; Assessment of Sleep and Ventilation |
| NCT01560741 | PHASE1 | UNKNOWN | Telemedicine and Ventilator Titration in Chronic Respiratory Patients Initiating Non-invasive Ventilation |
| NCT01621984 | PHASE1 | COMPLETED | Therapeutic Riding and Neuromuscular Disease |
| NCT01758510 | PHASE1 | COMPLETED | Safety Study of HLA-haplo Matched Allogenic Bone Marrow Derived Stem Cell Treatment in Amyotrophic Lateral Sclerosis |
| NCT03440034 | PHASE1 | COMPLETED | Study of Pioglitazone in Sporadic Inclusion Body Myositis |
| NCT05730842 | PHASE1 | COMPLETED | Absorption, Metabolism, Excretion and Absolute Bioavailability of EDG-5506 in Healthy Volunteers |
| NCT03059420 | Not specified | RECRUITING | Genetic Studies of Strabismus, Congenital Cranial Dysinnervation Disorders (CCDDs), and Their Associated Anomalies |
| NCT03272802 | PHASE2/PHASE3 | UNKNOWN | Treatment Effect of Edaravone in Patients With Amyotrophic Lateral Sclerosis (ALS) |
| NCT00860951 | PHASE1/PHASE2 | COMPLETED | P300 Brain Computer Interface Keyboard to Operate Assistive Technology |
| NCT02362425 | PHASE1/PHASE2 | COMPLETED | Antioxidant Therapy in RYR1-Related Congenital Myopathy |
| NCT00001201 | Not specified | COMPLETED | Evaluation of Neuromuscular Disease |
| NCT00002044 | Not specified | COMPLETED | A Pilot Study To Evaluate the Effect of Retrovir (Zidovudine: AZT) in the Treatment of Human Immunodeficiency Virus (HIV) Associated Dementia and Neuromuscular Diseases |
| NCT00004553 | Not specified | COMPLETED | Electromyography to Diagnose Neuromuscular Disorders |
| NCT00015470 | Not specified | COMPLETED | Diagnostic Evaluation of Patients With Neuromuscular Disease |
| NCT00017745 | Not specified | COMPLETED | Phenotype/Genotype Correlations in Neuromuscular Disorders |
Related Atlas pages
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): congenital fibrosis of extraocular muscles, neuromuscular disease