Chemical inhibitors targeting histone methylation readers
X Huang, Y Chen, Q Xiao, X Shang, Y Liu - Pharmacology & Therapeutics, 2024 - Elsevier
Histone methylation reader domains are protein modules that recognize specific histone
methylation marks, such as methylated or unmethylated lysine or arginine residues on …
methylation marks, such as methylated or unmethylated lysine or arginine residues on …
Recent Progress in Modulation of WD40-Repeat Domain 5 Protein (WDR5): Inhibitors and Degraders
Simple Summary WD40-repeat (WDR) domain proteins play a crucial role in mediating
protein–protein interactions that sustain oncogenesis in human cancers. WDR5 has two …
protein–protein interactions that sustain oncogenesis in human cancers. WDR5 has two …
Discovery of potent and selective WDR5 proteolysis targeting chimeras as potential therapeutics for pancreatic cancer
As a core chromatin-regulatory scaffolding protein, WDR5 mediates numerous protein–
protein interactions (PPIs) with other partner oncoproteins. However, small-molecule …
protein interactions (PPIs) with other partner oncoproteins. However, small-molecule …
Discovery of a First-in-Class Small-Molecule Ligand for WDR91 Using DNA-Encoded Chemical Library Selection Followed by Machine Learning
WD40 repeat-containing protein 91 (WDR91) regulates early-to-late endosome conversion
and plays vital roles in endosome fusion, recycling, and transport. WDR91 was recently …
and plays vital roles in endosome fusion, recycling, and transport. WDR91 was recently …
Expanded profiling of WD repeat domain 5 inhibitors reveals actionable strategies for the treatment of hematologic malignancies
WD40 Repeat Domain 5 (WDR5) is a highly conserved nuclear protein that recruits MYC
oncoprotein transcription factors to chromatin to stimulate ribosomal protein gene …
oncoprotein transcription factors to chromatin to stimulate ribosomal protein gene …
A Target Class Ligandability Evaluation of WD40 Repeat-Containing Proteins
S Ackloo, F Li, M Szewczyk, A Seitova… - Journal of Medicinal …, 2024 - ACS Publications
Target class-focused drug discovery has a strong track record in pharmaceutical research,
yet public domain data indicate that many members of protein families remain unliganded …
yet public domain data indicate that many members of protein families remain unliganded …
Structure-based discovery of potent, orally bioavailable benzoxazepinone-based WD repeat domain 5 inhibitors
KB Teuscher, JJ Mills, J Tian, C Han… - Journal of Medicinal …, 2023 - ACS Publications
The chromatin-associated protein WDR5 (WD repeat domain 5) is an essential cofactor for
MYC and a conserved regulator of ribosome protein gene transcription. It is also a high …
MYC and a conserved regulator of ribosome protein gene transcription. It is also a high …
WD repeat domain 5 inhibitors for cancer therapy: not what you think
AM Weissmiller, SW Fesik, WP Tansey - Journal of Clinical Medicine, 2024 - mdpi.com
WDR5 is a conserved nuclear protein that scaffolds the assembly of epigenetic regulatory
complexes and moonlights in functions ranging from recruiting MYC oncoproteins to …
complexes and moonlights in functions ranging from recruiting MYC oncoproteins to …
Ribosome subunit attrition and activation of the p53–MDM4 axis dominate the response of MLL-rearranged cancer cells to WDR5 WIN site inhibition
The chromatin-associated protein WD Repeat Domain 5 (WDR5) is a promising target for
cancer drug discovery, with most efforts blocking an arginine-binding cavity on the protein …
cancer drug discovery, with most efforts blocking an arginine-binding cavity on the protein …
WD repeat domain 5 (WDR5) inhibitors: a patent review (2016-present)
JA Coker, SR Stauffer - Expert Opinion on Therapeutic Patents, 2025 - Taylor & Francis
Introduction WDR5 is an epigenetic scaffolding protein that has attracted significant interest
as an anti-cancer drug target, especially in MLL-rearranged leukemias. The most druggable …
as an anti-cancer drug target, especially in MLL-rearranged leukemias. The most druggable …