Monday, April 5, 2021

A targeted covalent small molecule inhibitor of HIV-1 fusion

Guangyan Zhou Li He Kathy H Li Cassio Cardoso Santos Pedroso and Miriam Gochin

Chem. Commun., 2021

DOI: 10.1039/D1CC01013A 

We describe a low molecular weight covalent inhibitor targeting a conserved lysine residue within the hydrophobic pocket of HIV-1 glycoprotein-41. The inhibitor bound selectively to the hydrophobic pocket and exhibited an order of magnitude enhancement of anti-fusion activity against HIV-1 compared to its non-covalent counterpart. The findings represent a significant advance in the quest to obtain non-peptide fusion inhibitor.

Rational Design of CDK12/13 and BRD4 Molecular Glue Degraders

Nathanael Schiander Gray ,  Zhe Zhuang ,  Woong Sub Byun ,  Zuzanna Kozicka ,  Katherine Donovan ,  Brendan Dwyer ,  Abby Thornhill ,  Hanna...