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Gene and Protein Information ![]() |
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Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 334 | 9q34.2 | WDR5 | WD repeat domain 5 | |
Mouse | - | 334 | 2 A3 | Wdr5 | WD repeat domain 5 | |
Rat | - | 334 | 3p12 | Wdr5 | WD repeat domain 5 |
Previous and Unofficial Names ![]() |
CFAP89 | cilia and flagella associated protein 89 | SWD3, Set1c WD40 repeat protein |
Database Links ![]() |
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Alphafold | P61964 (Hs), P61965 (Mm), Q498M4 (Rn) |
ChEMBL Target | CHEMBL1075317 (Hs) |
Ensembl Gene | ENSG00000196363 (Hs), ENSMUSG00000026917 (Mm), ENSRNOG00000008212 (Rn) |
Entrez Gene | 11091 (Hs), 140858 (Mm), 362093 (Rn) |
Human Protein Atlas | ENSG00000196363 (Hs) |
KEGG Gene | hsa:11091 (Hs), mmu:140858 (Mm), rno:362093 (Rn) |
OMIM | 609012 (Hs) |
Pharos | P61964 (Hs) |
RefSeq Nucleotide | NM_017588 (Hs), NM_080848 (Mm), NM_001039034 (Rn) |
RefSeq Protein | NP_060058 (Hs), NP_543124 (Mm), NP_001034123 (Rn) |
SynPHARM | 81844 (in complex with OICR-9429) |
UniProtKB | P61964 (Hs), P61965 (Mm), Q498M4 (Rn) |
Wikipedia | WDR5 (Hs) |
Selected 3D Structures ![]() |
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Download all structure-activity data for this target as a CSV file
Inhibitors | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Immuno Process Associations | ||
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General Comments |
WDR5 is involved in the formation of heterotrimeric or multiprotein complexes eg the histone acetyltransferase complex and the histone methyltransferase complex [6-7]. Members of the WD repeat-containing protein family are involved in many cellular processes, including cell cycle progression, signal transduction, apoptosis, and gene regulation. WDR5 is reported to associate with the long non-coding RNA HOTTIP which drives histone H3 lysine 4 trimethylation and gene transcription [5]. |
1. Grebien F, Vedadi M, Getlik M, Giambruno R, Grover A, Avellino R, Skucha A, Vittori S, Kuznetsova E, Smil D et al.. (2015) Erratum: Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia. Nat Chem Biol, 11 (10): 815. [PMID:26379026]
2. Li D, Yu X, Kottur J, Gong W, Zhang Z, Storey AJ, Tsai YH, Uryu H, Shen Y, Byrum SD et al.. (2022) Discovery of a dual WDR5 and Ikaros PROTAC degrader as an anti-cancer therapeutic. Oncogene, [Epub ahead of print]. DOI: 10.1038/s41388-022-02340-8 [PMID:35525905]
3. SGC. OICR-9429 - a chemical probe for WDR5. Accessed on 03/03/2015. Modified on 03/03/2015. thesgc.org, http://www.thesgc.org/node/9204
4. Teuscher KB, Meyers KM, Wei Q, Mills JJ, Tian J, Alvarado J, Sai J, Van Meveren M, South TM, Rietz TA et al.. (2022) Discovery of Potent Orally Bioavailable WD Repeat Domain 5 (WDR5) Inhibitors Using a Pharmacophore-Based Optimization. J Med Chem, 65 (8): 6287-6312. [PMID:35436124]
5. Wang KC, Yang YW, Liu B, Sanyal A, Corces-Zimmerman R, Chen Y, Lajoie BR, Protacio A, Flynn RA, Gupta RA et al.. (2011) A long noncoding RNA maintains active chromatin to coordinate homeotic gene expression. Nature, 472 (7341): 120-4. [PMID:21423168]
6. Wysocka J, Myers MP, Laherty CD, Eisenman RN, Herr W. (2003) Human Sin3 deacetylase and trithorax-related Set1/Ash2 histone H3-K4 methyltransferase are tethered together selectively by the cell-proliferation factor HCF-1. Genes Dev, 17 (7): 896-911. [PMID:12670868]
7. Yokoyama A, Wang Z, Wysocka J, Sanyal M, Aufiero DJ, Kitabayashi I, Herr W, Cleary ML. (2004) Leukemia proto-oncoprotein MLL forms a SET1-like histone methyltransferase complex with menin to regulate Hox gene expression. Mol Cell Biol, 24 (13): 5639-49. [PMID:15199122]
WD repeat-containing proteins: WD repeat domain 5. Last modified on 23/05/2022. Accessed on 02/02/2023. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2831.