GRWD1

gene
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Also known as WDR28GRWDRRB1

Summary

GRWD1 (glutamate rich WD repeat containing 1, HGNC:21270) is a protein-coding gene on chromosome 19q13.33, encoding Glutamate-rich WD repeat-containing protein 1 (Q9BQ67). Histone binding-protein that regulates chromatin dynamics and loading of minichromosome maintenance (MCM) complex at replication origins, possibly by promoting chromatin openness. It is a common-essential gene (DepMap: required in 92.5% of cancer cell lines).

This gene encodes a glutamate-rich protein that contains five WD-repeat motifs. The encoded protein may play a critical role in ribosome biogenesis and may also play a role in histone methylation through interactions with CUL4-DDB1 ubiquitin E3 ligase.

Source: NCBI Gene 83743 — RefSeq curated summary.

At a glance

  • Gene–disease (curated): congenital diarrhea (Limited, GenCC)
  • Clinical variants (ClinVar): 116 total — 2 likely-pathogenic
  • Phenotypes (HPO): 4
  • Druggable target: yes
  • Cancer dependency (DepMap): dependent in 92.5% of screened cell lines (common-essential)
  • MANE Select transcript: NM_031485

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:21270
Approved symbolGRWD1
Nameglutamate rich WD repeat containing 1
Location19q13.33
Locus typegene with protein product
StatusApproved
AliasesWDR28, GRWD, RRB1
Ensembl geneENSG00000105447
Ensembl biotypeprotein_coding
OMIM610597
Entrez83743

Gene structure

Transcript identifiers

Ensembl transcripts: 4 — 3 protein_coding, 1 retained_intron

ENST00000253237, ENST00000598711, ENST00000599949, ENST00000928855

RefSeq mRNA: 1 — MANE Select: NM_031485 NM_031485

CCDS: CCDS12720

Canonical transcript exons

ENST00000253237 — 7 exons

ExonStartEnd
ENSE000008965364845103448451231
ENSE000008965374845066648450808
ENSE000008965424844598348446192
ENSE000012494914845270848457022
ENSE000022126244845031348450526
ENSE000034852874844638548446502
ENSE000036272734844668148446843

Expression profiles

Bgee: expression breadth ubiquitous, 285 present calls, max score 88.53.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 29.1248 / max 205.5598, expressed in 1818 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter IDTPM avgSamples expressed
17678724.90201814
1767852.66091451
1767861.56191042

Top tissues by expression

291 total, by Bgee expression score (0-100, higher = more expressed):

TissueAnatomy IDExpression scoreQuality
tongue squamous epitheliumUBERON:000691988.53silver quality
gastrocnemiusUBERON:000138888.20gold quality
muscle of legUBERON:000138387.36gold quality
type B pancreatic cellCL:000016985.75silver quality
stromal cell of endometriumCL:000225585.24gold quality
skeletal muscle organUBERON:001489284.68gold quality
muscle organUBERON:000163084.67gold quality
olfactory bulbUBERON:000226484.45silver quality
primordial germ cell in gonadCL:0000670 ∩ UBERON:000099184.17gold quality
hindlimb stylopod muscleUBERON:000425284.02gold quality
esophagus mucosaUBERON:000246983.79gold quality
left uterine tubeUBERON:000130383.68gold quality
skin of legUBERON:000151183.59gold quality
apex of heartUBERON:000209883.44gold quality
granulocyteCL:000009483.35gold quality
body of stomachUBERON:000116183.30gold quality
right adrenal glandUBERON:000123383.29gold quality
skin of abdomenUBERON:000141683.26gold quality
left adrenal glandUBERON:000123483.19gold quality
pancreatic ductal cellCL:000207983.17silver quality
right coronary arteryUBERON:000162583.12gold quality
ectocervixUBERON:001224983.03gold quality
lymph nodeUBERON:000002982.99gold quality
heart left ventricleUBERON:000208482.96gold quality
right adrenal gland cortexUBERON:003582782.95gold quality
hair follicleUBERON:000207382.94silver quality
vena cavaUBERON:000408782.91silver quality
mucosa of transverse colonUBERON:000499182.89gold quality
esophagusUBERON:000104382.86gold quality
left adrenal gland cortexUBERON:003582582.82gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 1.

ExperimentMarker?Max mean expression
E-ANND-3no0.00

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): GLI3

miRNA regulators (miRDB)

39 targeting GRWD1, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-9-5P100.0072.282361
HSA-MIR-518D-5P100.0067.51979
HSA-MIR-518E-5P100.0067.66954
HSA-MIR-518F-5P100.0067.51979
HSA-MIR-519A-5P100.0067.66954
HSA-MIR-519B-5P100.0067.66954
HSA-MIR-519C-5P100.0067.66954
HSA-MIR-520C-5P100.0067.51979
HSA-MIR-522-5P100.0067.66954
HSA-MIR-523-5P100.0067.66954
HSA-MIR-526A-5P100.0067.51979
HSA-MIR-4650-5P99.9864.69999
HSA-MIR-495-3P99.9672.814197
HSA-MIR-568899.9673.234504
HSA-MIR-6756-5P99.8267.972466
HSA-MIR-6766-5P99.6867.702325
HSA-MIR-7112-5P99.5965.76104
HSA-MIR-444199.4966.563216
HSA-MIR-312399.4767.152693
HSA-MIR-6828-5P99.3169.211433
HSA-MIR-3925-5P99.2167.901466
HSA-MIR-371A-5P99.0866.511914
HSA-MIR-427099.0266.261987
HSA-MIR-330-5P98.7367.631788
HSA-MIR-7851-3P98.7264.88980
HSA-MIR-6754-5P98.6065.541627
HSA-MIR-6776-5P98.5467.431304
HSA-MIR-32698.2566.441565
HSA-MIR-4717-5P98.1967.97894
HSA-MIR-340-3P98.1168.25679

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 92.5% of screened cell lines, common-essential.

Literature-anchored findings (GeneRIF, showing 6)

  • Cdt1-binding protein GRWD1 promotes chromatin fluidity by influencing nucleosome structures, e.g., by transient eviction of H2A-H2B, and thereby promotes efficient MCM loading at replication origins. (PMID:27552915)
  • GRWD1 overexpression in combination with HPV16 E7 and activated KRAS confers anchorage-independent growth and tumorigenic capacity on normal human fibroblasts. Consistent with this, GRWD1 overexpression is associated with poor prognosis in cancer patients. (PMID:27856536)
  • findings suggest a novel oncogenic function of GRWD1 as a transcriptional regulator of p53 and that GRWD1 might be an attractive therapeutic target and prognostic marker in cancer therapy (PMID:31545368)
  • GRWD1 promotes cell proliferation and migration in non-small cell lung cancer by activating the Notch pathway. (PMID:31891681)
  • Comprehensive Analysis of Glutamate-Rich WD Repeat-Containing Protein 1 and Its Potential Clinical Significance for Pancancer. (PMID:34616846)
  • GRWD1-WDR5-MLL2 Epigenetic Complex Mediates H3K4me3 Mark and Is Essential for Kaposi’s Sarcoma-Associated Herpesvirus-Induced Cellular Transformation. (PMID:34933446)

Cross-species orthologs

5 orthologs

OrganismSymbolGene ID
danio_reriogrwd1ENSDARG00000004806
mus_musculusGrwd1ENSMUSG00000053801
rattus_norvegicusGrwd1ENSRNOG00000021058
drosophila_melanogasterl(2)09851FBGN0022288
caenorhabditis_elegansWBGENE00021899

Paralogs (9): ERCC8 (ENSG00000049167), GEMIN5 (ENSG00000082516), RBBP7 (ENSG00000102054), WDR59 (ENSG00000103091), PEX7 (ENSG00000112357), WDR77 (ENSG00000116455), WDR24 (ENSG00000127580), RBBP4 (ENSG00000162521), WDR73 (ENSG00000177082)

Protein

Protein identifiers

Glutamate-rich WD repeat-containing protein 1Q9BQ67 (reviewed: Q9BQ67)

All UniProt accessions (2): Q9BQ67, M0QX71

UniProt curated annotations — full annotation on UniProt →

Function. Histone binding-protein that regulates chromatin dynamics and loading of minichromosome maintenance (MCM) complex at replication origins, possibly by promoting chromatin openness. Plays a role in ribosomal biogenesis.

Subunit / interactions. Interacts with pre-ribosomal ribonucleoprotein complexes. Interacts with METTL18. Interacts with CDT1; origin binding of GRWD1 is dependent on CDT1. Interacts with CDC6; origin binding of GRWD1 is dependent on CDC6. Interacts with RPL3. Binds to histone H2A-H2B and H3-H4 complexes.

Subcellular location. Nucleus. Nucleolus. Chromosome.

Tissue specificity. Widely expressed.

Disease relevance. Diarrhea 14, congenital (DIAR14) [MIM:621160] An autosomal recessive disorder characterized by diarrhea manifesting within the first year of life, and diffuse arterial hypoplasia. The disease is caused by variants affecting the gene represented in this entry.

Induction. Induced by E2F transcription factors.

RefSeq proteins (1): NP_113673* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR001680WD40_rptRepeat
IPR015943WD40/YVTN_repeat-like_dom_sfHomologous_superfamily
IPR019775WD40_repeat_CSConserved_site
IPR020472WD40_PAC1Repeat
IPR022052Histone-bd_RBBP4-like_NDomain
IPR036322WD40_repeat_dom_sfHomologous_superfamily
IPR051972Glutamate-rich_WD_repeatFamily

Pfam: PF00400, PF12265

UniProt features (18 total): repeat 7, modified residue 4, sequence variant 3, region of interest 2, chain 1, compositionally biased region 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-Q9BQ67-F189.210.77

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Post-translational modifications (4): 10, 119, 122, 344

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 165 (showing top): RRAGTTGT_UNKNOWN, GOBP_RIBOSOME_BIOGENESIS, YAO_TEMPORAL_RESPONSE_TO_PROGESTERONE_CLUSTER_10, MONNIER_POSTRADIATION_TUMOR_ESCAPE_UP, AACWWCAANK_UNKNOWN, OCT1_03, WTGAAAT_UNKNOWN, BERTUCCI_MEDULLARY_VS_DUCTAL_BREAST_CANCER_UP, FISCHER_DREAM_TARGETS, RFX1_02, GOBP_PROTEIN_DNA_COMPLEX_ORGANIZATION, HAN_SATB1_TARGETS_DN, GOBP_CHROMATIN_REMODELING, BURTON_ADIPOGENESIS_2, HAMAI_APOPTOSIS_VIA_TRAIL_DN

GO Biological Process (4): DNA replication (GO:0006260), nucleosome assembly (GO:0006334), nucleosome disassembly (GO:0006337), ribosome biogenesis (GO:0042254)

GO Molecular Function (5): chromatin binding (GO:0003682), DNA replication origin binding (GO:0003688), RNA binding (GO:0003723), histone binding (GO:0042393), protein binding (GO:0005515)

GO Cellular Component (6): nucleus (GO:0005634), nucleoplasm (GO:0005654), chromosome (GO:0005694), nucleolus (GO:0005730), cytosol (GO:0005829), protein-containing complex (GO:0032991)

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
nucleosome organization2
binding2
nuclear lumen2
cellular anatomical structure2
intracellular membraneless organelle2
DNA metabolic process1
DNA biosynthetic process1
chromatin organization1
protein-DNA complex assembly1
protein-DNA complex disassembly1
ribonucleoprotein complex biogenesis1
sequence-specific double-stranded DNA binding1
nucleic acid binding1
protein binding1
intracellular membrane-bounded organelle1
cytoplasm1
cellular_component1

Protein interactions and networks

STRING

2374 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
GRWD1RPL3P39023952
GRWD1BOP1Q14137945
GRWD1CDT1Q9H211935
GRWD1TSR2Q969E8776
GRWD1RPL11P25121753
GRWD1HEATR3Q7Z4Q2736
GRWD1DCAF5Q96JK2599
GRWD1SURF6O75683574
GRWD1RPL5P46777545
GRWD1ORC6Q9Y5N6534
GRWD1METTL18O95568509
GRWD1COPS7AQ9UBW8508
GRWD1BCCIPQ9P287486
GRWD1PPM1GO15355471
GRWD1DDB1Q16531471

IntAct

89 interactions, top by confidence:

ABTypeScore
DTLDDB1psi-mi:“MI:0914”(association)0.740
CUL4BCUL4Apsi-mi:“MI:0914”(association)0.730
SPTLC1SPTLC2psi-mi:“MI:0914”(association)0.680
SEC13SEC16Apsi-mi:“MI:0914”(association)0.640
CUL4BEEDpsi-mi:“MI:0914”(association)0.560
COP1DDB1psi-mi:“MI:0914”(association)0.530
TNFAIP3LRRIQ3psi-mi:“MI:2364”(proximity)0.420
SDC1ILVBLpsi-mi:“MI:0915”(physical association)0.400
JUNpsi-mi:“MI:0914”(association)0.350
JUNTPM3psi-mi:“MI:0914”(association)0.350
Xpo1IFT56psi-mi:“MI:0914”(association)0.350
CUL4BTLE1psi-mi:“MI:0914”(association)0.350
SNRNP40WDR5psi-mi:“MI:0914”(association)0.350
WDR26DDB1psi-mi:“MI:0914”(association)0.350
WDR5BDDB1psi-mi:“MI:0914”(association)0.350
WDR5DDB1psi-mi:“MI:0914”(association)0.350
PPM1GHADHApsi-mi:“MI:0914”(association)0.350
RRP1BZNF785psi-mi:“MI:0914”(association)0.350
psi-mi:“MI:0914”(association)0.350
NUDCD1TUBAL3psi-mi:“MI:0914”(association)0.350
Prdm16ESYT2psi-mi:“MI:0914”(association)0.350
MecomESYT2psi-mi:“MI:0914”(association)0.350
ESR1ESYT2psi-mi:“MI:0914”(association)0.350
CAND1GTPBP10psi-mi:“MI:0914”(association)0.350
CUL1LGALS8psi-mi:“MI:0914”(association)0.350
COPS5FBLL1psi-mi:“MI:0914”(association)0.350

BioGRID (602): GRWD1 (Affinity Capture-RNA), GRWD1 (Affinity Capture-RNA), GRWD1 (Reconstituted Complex), GRWD1 (Co-fractionation), GRWD1 (Co-fractionation), GRWD1 (Co-fractionation), GRWD1 (Co-fractionation), GRWD1 (Co-fractionation), GRWD1 (Co-fractionation), GRWD1 (Co-fractionation), GRWD1 (Co-fractionation), NOC2L (Co-fractionation), POLR1E (Co-fractionation), RBM19 (Co-fractionation), GRWD1 (Affinity Capture-MS)

ESM2 similar proteins: A1L112, A4IHS2, A8NZM5, B2ZZS9, O00423, O80775, O95834, P93107, P97452, Q05BC3, Q0DYP5, Q13216, Q13610, Q13685, Q15269, Q1JQD2, Q2HJ56, Q32KQ2, Q32P44, Q3SZK1, Q4V8C3, Q562C2, Q58DT8, Q5BIM8, Q5F3K4, Q5R9T6, Q5RCG7, Q5RFQ3, Q5VU92, Q5XI13, Q5ZK69, Q6DRF9, Q6P6T4, Q6PFM9, Q7TNG5, Q7YR70, Q810D6, Q8BH57, Q8BHB4, Q8BU03

Diamond homologs: A1CH75, A1CXL0, A2QI22, A3LQ86, A4R2Q6, A5DL92, A5DST9, A6R3K5, A6S0T8, A6ZPA9, A7ECP3, A7TMF9, A8IR43, B0Y5V6, B2B5V0, B2VZH2, B3RQN1, G0SFB5, O74184, P41318, P61480, Q0CLJ4, Q0UXP3, Q12024, Q1DJF7, Q1JQD2, Q2GXT0, Q2T9T9, Q2UGK1, Q4WP10, Q5APF0, Q5B4R1, Q5BJ90, Q5XI13, Q5XUX1, Q5ZJW8, Q6BLS5, Q6CEW7, Q6CU59, Q6FKK3

SIGNOR signaling

0 interactions.

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 123 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:

PathwayPartnersFoldFDR
Signaling by ALK fusions and activated point mutants712.7×9e-04
Neddylation105.7×3e-03

GO biological processes:

GO termPartnersFoldFDR
cell surface receptor protein tyrosine kinase signaling pathway813.5×1e-04
ribosomal small subunit biogenesis511.1×7e-03
insulin receptor signaling pathway510.8×7e-03
positive regulation of protein catabolic process59.9×1e-02
regulation of cell cycle85.8×7e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

116 variants total. Per-class counts are floors (≥ shown; pagination cap):

ClassificationCount (floor)
Pathogenic0
Likely pathogenic2
Uncertain significance91
Likely benign11
Benign2

Top pathogenic / likely-pathogenic (2)

Variant IDHGVSClassification
3252071NM_031485.4(GRWD1):c.920A>G (p.His307Arg)Likely pathogenic
3252072NM_031485.4(GRWD1):c.1102G>T (p.Val368Phe)Likely pathogenic

SpliceAI

1114 predictions. Top by Δscore:

VariantEffectΔscore
19:48446162:GCC:Gdonor_gain1.0000
19:48446188:GACTG:Gdonor_gain1.0000
19:48446499:ACAGG:Adonor_loss1.0000
19:48446501:AGG:Adonor_loss1.0000
19:48446504:T:Gdonor_loss1.0000
19:48446677:CCA:Cacceptor_loss1.0000
19:48446678:CAGA:Cacceptor_loss1.0000
19:48446679:A:AGacceptor_gain1.0000
19:48446679:AGAC:Aacceptor_loss1.0000
19:48446679:AGACT:Aacceptor_gain1.0000
19:48446680:G:GAacceptor_gain1.0000
19:48446680:GA:Gacceptor_gain1.0000
19:48446680:GAC:Gacceptor_gain1.0000
19:48446680:GACT:Gacceptor_gain1.0000
19:48446680:GACTG:Gacceptor_gain1.0000
19:48446839:TTCGG:Tdonor_gain1.0000
19:48446840:TCGG:Tdonor_gain1.0000
19:48446841:CGG:Cdonor_gain1.0000
19:48446841:CGGGT:Cdonor_gain1.0000
19:48446842:GG:Gdonor_gain1.0000
19:48446842:GGG:Gdonor_gain1.0000
19:48446843:GG:Gdonor_gain1.0000
19:48446843:GGTA:Gdonor_loss1.0000
19:48446844:G:GGdonor_gain1.0000
19:48446844:GT:Gdonor_loss1.0000
19:48450307:CTGCA:Cacceptor_loss1.0000
19:48450308:TGCAG:Tacceptor_loss1.0000
19:48450309:GCA:Gacceptor_loss1.0000
19:48450310:CAGGT:Cacceptor_loss1.0000
19:48450311:A:Cacceptor_loss1.0000

AlphaMissense

2899 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
19:48451181:A:CS325R0.999
19:48451183:T:AS325R0.999
19:48451183:T:GS325R0.999
19:48452825:T:AW381R0.999
19:48452825:T:CW381R0.999
19:48452909:T:CF409L0.999
19:48452911:C:AF409L0.999
19:48452911:C:GF409L0.999
19:48450496:T:CF218L0.998
19:48450498:T:AF218L0.998
19:48450498:T:GF218L0.998
19:48451041:C:AA278D0.998
19:48451073:T:AW289R0.998
19:48451073:T:CW289R0.998
19:48451076:G:CD290H0.998
19:48451077:A:CD290A0.998
19:48451077:A:TD290V0.998
19:48452765:T:AW361R0.998
19:48452765:T:CW361R0.998
19:48452827:G:CW381C0.998
19:48452827:G:TW381C0.998
19:48446399:A:CS68R0.997
19:48446401:C:AS68R0.997
19:48446401:C:GS68R0.997
19:48446471:G:TG92W0.997
19:48450508:T:AW222R0.997
19:48450508:T:CW222R0.997
19:48450707:T:AW242R0.997
19:48450707:T:CW242R0.997
19:48450788:T:AW269R0.997

dbSNP variants (sampled 300 via entrez): RS1000055611 (19:48456853 A>G,T), RS1000126016 (19:48454942 ATTTCT>A), RS1000178712 (19:48455144 A>G,T), RS1000278968 (19:48449874 G>A), RS1000430115 (19:48457139 G>C), RS1000511465 (19:48454071 C>A,T), RS1000851469 (19:48452298 A>G), RS1000915004 (19:48451744 G>A,T), RS1001012202 (19:48448662 G>T), RS1001674836 (19:48449012 G>T), RS1001945327 (19:48446231 G>C), RS1002184073 (19:48452911 C>A,G,T), RS1002235592 (19:48456491 G>A), RS1002285330 (19:48447460 G>A), RS1002408610 (19:48447624 G>A)

Disease associations

OMIM: gene MIM:610597 | disease phenotypes: MIM:214700, MIM:621160

GenCC curated gene-disease

DiseaseClassificationInheritance
congenital diarrheaLimitedAutosomal recessive

Mondo (3): prostate cancer (MONDO:0008315), congenital diarrhea (MONDO:0000824), diarrhea 14, congenital (MONDO:0976266)

Orphanet (1): Familial prostate cancer (Orphanet:1331)

HPO phenotypes

4 total (4 of 4 shown, HPO-id order):

HPOTerm
HP:0000007Autosomal recessive inheritance
HP:0002014Diarrhea
HP:0003577Congenital onset
HP:0033994Dependency on parenteral nutrition

GWAS associations

0 associations (top):

MeSH disease descriptors (1)

DescriptorNameTree numbers
D011471Prostatic NeoplasmsC04.588.945.440.770; C12.100.500.260.750; C12.100.500.565.625; C12.200.294.260.750; C12.200.294.565.625; C12.200.758.409.750; C12.900.619.750

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5724692 (SINGLE PROTEIN)

PharmGKB: 1 entry (VIP=true, CPIC=false)

CTD chemical–gene interactions

49 total (human), top 30 by PubMed support.

ChemicalActions (top 5)PubMed papers
sodium arseniteincreases expression, affects expression, decreases expression, affects cotreatment, increases abundance3
bisphenol Adecreases expression2
Smokedecreases expression, increases abundance, increases expression2
Valproic Acidaffects cotreatment, increases expression, increases methylation2
Cadmium Chloridedecreases expression, increases abundance, increases expression2
FR900359increases phosphorylation1
TAK-243increases sumoylation1
TL8-506affects cotreatment, increases expression1
cinobufagindecreases expression1
2,4,6-tribromophenoldecreases expression1
deoxynivalenolincreases expression1
decabromobiphenyl etherincreases expression1
tris(1,3-dichloro-2-propyl)phosphatedecreases expression1
tetrabromobisphenol Aincreases expression1
manganese chlorideaffects cotreatment, increases abundance, increases expression1
nivalenolincreases expression1
di-n-butylphosphoric acidaffects expression1
cylindrospermopsinincreases expression1
K 7174decreases expression1
erucylphospho-N,N,N-trimethylpropylammoniumdecreases expression1
ICG 001decreases expression1
abrineincreases expression1
2,2’,4,4’-tetrabromodiphenyl etherdecreases expression1
(+)-JQ1 compounddecreases expression1
4-(4-((5-(4,5-dimethyl-2-nitrophenyl)-2-furanyl)methylene)-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl)benzoic aciddecreases expression1
Temozolomideincreases expression1
Air Pollutantsincreases abundance, increases expression1
Arsenicaffects cotreatment, increases abundance, increases expression1
Cadmiumincreases abundance, increases expression1
Caffeinedecreases phosphorylation1

ChEMBL screening assays

6 unique, capped per target: 6 binding

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL5697358BindingInhibition of GRWD1 (unknown origin) assessed as fold change at 10 uM incubated for 1 hr by colloidal coomassie staining based LC-MS/MS analysisInhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia. — Nature

Clinical trials (associated diseases)

300 trials via MONDO — disease-level, not drug-specific.

TrialPhaseStatusTitle
NCT00029224PHASE4COMPLETEDTreatment With Zoledronic Acid in Patients With Breast Cancer, Multiple Myeloma, and Prostate Cancer With Cancer Related Bone Lesions
NCT00035997PHASE4COMPLETEDOpen-label Trial on the Effect of I.V. Zoledronic Acid 4 mg on Bone Density in Hormone Sensitive Prostate Cancer Patients With Bone Metastasis
NCT00063609PHASE4COMPLETEDThe Effect of Zoledronic Acid on Bone Loss in Prostate Cancer Patients Undergoing Androgen Deprivation Therapy
NCT00103623PHASE4SUSPENDEDThe Plenaxis® Experience Study
NCT00106392PHASE4COMPLETEDA Safety and Efficacy Study of Prograf in the Prevention of Erectile Dysfunction After Radical Prostatectomy
NCT00185029PHASE4UNKNOWNMR-Lymphography and Lymph Node Staging in Prostate Cancer
NCT00199485PHASE4COMPLETEDAngelica Sinensis for the Treatment of Hot Flashes in Men Undergoing LHRH Therapy for Prostate Cancer
NCT00219219PHASE4COMPLETEDZoledronic Acid in the Prevention of Skeletal-related Events in Hormone Refractory and Hormone-sensitive Prostate Cancer Patients With Bone Metastases
NCT00219271PHASE4COMPLETEDEffect Of Zoledronic Acid On Circulating And Bone Marrow-Residing Prostate Cancer Cells In Patients With Clinically Localized Prostate Cancer
NCT00237146PHASE4COMPLETEDStudy to Evaluate Zoledronic Acid on Quality of Life and Skeletal-related Events as Adjuvant Treatment in Patients With Hormone-naïve Prostate Cancer and Bone Metastasis Who Have Undergone Orchiectomy
NCT00242554PHASE4COMPLETEDOpen-label Phase IV Clinical Trial to Evaluate the Safety and Tolerability of Zoledronic Acid in Patients With Prostate Cancer and Bone Metastases
NCT00280098PHASE4COMPLETEDDocetaxel in the Treatment of Hormone Refractory Prostate Cancer
NCT00293696PHASE4COMPLETEDCasodex/Zoladex Biomarkers in Localised Prostate Cancer
NCT00334139PHASE4COMPLETEDEffect of Zoledronic Acid on Bone Metabolism in Patients With Bone Metastasis and Prostate or Breast Cancer
NCT00375765PHASE4COMPLETEDEffects On Dihydrotestosterone Regulated Gene Expression In Benign Prostatic Hyperplasia Or Prostate Cancer
NCT00391690PHASE4COMPLETEDEvaluation of Bone Markers as Diagnostic Tools for Early Detection of Bone Metastases in Patients With High Risk Prostate Cancer
NCT00422708PHASE4COMPLETEDLocal Anesthesia for Prostate Biopsy
NCT00526331PHASE4COMPLETEDEvaluation of Arterial Pressure Based Cardiac Output for Goal-Directed Perioperative Therapy
NCT00590213PHASE4COMPLETEDCompare the Value of Prophylactic Versus Therapeutic Breast Radiotherapy in CASODEX
NCT00629330PHASE4TERMINATEDDissemination of Prostate Cancer Screening to PCP’s in African American Communities
NCT00771966PHASE4COMPLETEDRadical Prostatectomy and Perioperative Fluid Therapy
NCT00805701PHASE4COMPLETEDStudy Assessing The Efficacy And Safety Of Avodart (Dutasteride) At Improving Urinary Symptoms In Men With Prostate Cancer Who Are Undergoing Seed Implantation
NCT00859027PHASE4COMPLETEDEffect Of Risedronate On Bone Mass In Older Men Receiving Neoadjuvant Therapy For Prostate Cancer
NCT00906269PHASE4UNKNOWNCan Hyperbaric Oxygen Improve Erectile Function Following Surgery for Prostate Cancer
NCT00953277PHASE4COMPLETEDStudy of Nerve Reconstruction Using AVANCE in Subjects Who Undergo Robotic Assisted Prostatectomy for Treatment of Prostate Cancer
NCT00982800PHASE4COMPLETEDDoes Postoperative Gabapentin Reduce Pain, Opioid Consumption and Anxiety and Have a Positive Effect on Health Related Quality of Life After Radical Prostatectomy?
NCT01083199PHASE4COMPLETEDGlobal Performance Evaluation of the AMS CONTINUUM™ Device
NCT01136226PHASE4COMPLETEDEvaluate Recovery of Testosterone for Patients Using Eligard
NCT01161563PHASE4COMPLETEDRandomized Crossover Trial to Assess the Tolerability of Gonadotropin Releasing Hormone (GnRH) Analogue Administration
NCT01230905PHASE4COMPLETEDStudy to Monitor the Effects of Androgen Suppression Treatment on the Heart
NCT01296672PHASE4COMPLETED3 Month Finasteride Challenge Test Can Significantly Improve the Performance of Screening for Prostate Cancer
NCT01365143PHASE4TERMINATEDProspective Randomized Trial Comparing Robotic Versus Open Radical Prostatectomy
NCT01379742PHASE4UNKNOWNComparison of Between ThinSeed™ and OncoSeed™ for Permanent Prostate Brachytherapy
NCT01486563PHASE4COMPLETEDHydroxyethyl Starch and Renal Function After Radical Prostatectomy
NCT01511874PHASE4COMPLETEDEfficacy and Safety Study of ELIGARD 22.5mg With Prostate Cancer
NCT01512472PHASE4TERMINATEDFirmagon (Degarelix) Intermittent Therapy
NCT01547416PHASE4COMPLETEDThe Effect of Combined General/Epidural Anesthesia Versus General Anesthesia on Diaphragmatic Function
NCT01571544PHASE4COMPLETEDThe Use of Thermal Suits as Preventing Hypothermia During Surgery
NCT01581749PHASE4UNKNOWNEvaluation of Truebeam for Low-Intermediate Risk Prostate Cancer
NCT01649635PHASE4COMPLETEDStudy of Cabazitaxel Combined With Prednisone and Prophylaxis of Neutropenia Complications in the Treatment of Patients With Metastatic Castration-resistant Prostate Cancer