Development of PROTACs using computational approaches
Proteolysis-targeting chimeras (PROTACs) are drugs designed to degrade target proteins
via the ubiquitin-proteasome system. With the application of computational biology/chemistry …
via the ubiquitin-proteasome system. With the application of computational biology/chemistry …
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 …
Crystal structures of DCAF1-PROTAC-WDR5 ternary complexes provide insight into DCAF1 substrate specificity
MF Mabanglo, B Wilson, M Noureldin… - Nature …, 2024 - nature.com
Proteolysis-targeting chimeras (PROTACs) have been explored for the degradation of drug
targets for more than two decades. However, only a handful of E3 ligase substrate receptors …
targets for more than two decades. However, only a handful of E3 ligase substrate receptors …
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 …
Next steps for targeted protein degradation
Targeted protein degradation (TPD) has greatly advanced as a therapeutic strategy in the
past two decades, and we are on the cusp of rationally designed protein degraders reaching …
past two decades, and we are on the cusp of rationally designed protein degraders reaching …
MBD2 regulates the progression and chemoresistance of cholangiocarcinoma through interaction with WDR5
D Wang, J Chen, G Wu, F **ong, W Liu, Q Wang… - Journal of Experimental …, 2024 - Springer
Background Cholangiocarcinoma (CCA) is a highly malignant, rapidly progressing tumor of
the bile duct. Owing to its chemoresistance, it always has an extremely poor prognosis …
the bile duct. Owing to its chemoresistance, it always has an extremely poor prognosis …
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 …
targets, particularly undruggable proteins, for more than two decades. They have been …