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 …

Ribosome subunit attrition and activation of the p53–MDM4 axis dominate the response of MLL-rearranged cancer cells to WDR5 WIN site inhibition

GC Howard, J Wang, KL Rose, C Jones, P Patel, T Tsui… - Elife, 2024 - elifesciences.org
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 …

Crystal structures of DCAF1-PROTAC-WDR5 ternary complexes provide insight into DCAF1 substrate specificity

M Vedadi, M Mabanglo, B Wilson, M Noureldin… - 2024 - researchsquare.com
Proteolysis-targeting chimeras (PROTACs) have been explored for the degradation of drug
targets, particularly undruggable proteins, for more than two decades. They have been …