Structural and functional characterization of ubiquitin variant inhibitors for the JAMM-family deubiquitinases STAMBP and STAMBPL1
Yusong Guo, Qi Liu, Evan Mallette, Cody Caba, Feng Hou, Julia Fux, Gabriel LaPlante, Aiping Dong, Qi Zhang, Hui Zheng, Yufeng Tong, Wei Zhang
Abstract
are potent inhibitors of STAMBP isopeptidase activity, far exceeding the reported small-molecule inhibitor BC-1471. This work demonstrates that UbV technology is suitable to develop molecules as tools to target metalloproteases, which can be used to further understand the cellular function of JAMM family DUBs.
Topics & Concepts
Deubiquitinating enzymeUbiquitinProteasesDrug discoveryCysteine proteaseComputational biologyProteaseSmall moleculeBiologyBiochemistryEnzymeChemistryGeneUbiquitin and proteasome pathwaysPeptidase Inhibition and AnalysisGlycosylation and Glycoproteins Research