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Target intelligence / Profile preview
WD repeat domain 5 (WDR5)
- Target
- WDR5
- Molecular classification
- WD40-repeat protein family, Chromatin-associated protein, Epigenetic scaffolding protein
01
Overview
WD repeat domain 5 is a highly conserved nuclear scaffolding protein that organizes multiprotein chromatin complexes, most famously the MLL/SET histone methyltransferase complexes responsible for H3K4 methylation, and is essential for the recruitment of MYC oncoproteins to chromatin to stimulate ribosomal protein gene transcription. Overexpression of WDR5 is closely linked to the development and maintenance of numerous cancers and poor prognosis. WDR5 is considered a promising therapeutic target, with several small-molecule inhibitors developed to block its protein-protein interactions, notably at its WIN site, effectively disrupting oncogenic chromatin modification programs in preclinical models.
- Other names
- WD repeat-containing protein 5WDR5WD40 repeat domain 5
02
Mechanism of action
Inhibition of WDR5 WIN site blocks protein–protein interactions required for MYC recruitment and MLL/SET histone methyltransferase complex assembly, impairing H3K4 methylation and RPG transcription. Downregulation of MYC-driven gene expression.
03
Biological functions
Scaffolding multiprotein complexes in the nucleusHistone modification—facilitates methylation (and dimethylation) at lysine-4 of histone H3Recruitment of MYC oncoprotein to chromatinGene regulationCell cycle progressionSignal transductionApoptosisCell proliferation (especially in cancers)
04
Disease associations
Cancer (solid and hematological, including leukemia, breast, prostate, pancreatic, neuroblastoma, liver, colorectal, gastric, bladder, head and neck carcinoma)Oncogenesis (sustains tumor development and poor prognosis)Potential role in late-onset preeclampsia
05
Safety considerations
So far, WDR5 WIN-site inhibition appears well tolerated in rodentsLimited information on human safety; off-target effects possible for chromatin modifiersIn cancer models, oral WDR5 inhibitors showed high-dose tolerability
06
Interacting drugs
Small-molecule WDR5 WIN site inhibitors (WINi; various chemical classes)
2 more in the full profile.
07
Biomarkers
WDR5 overexpression (high levels found in aggressive cancers; prognostic indicator)H3K4 methylation status may be monitored
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