ABHD2 Inhibitor Identified by Activity-Based Protein Profiling Reduces Acrosome Reaction.

ABSTRACT: ABHD2 is a serine hydrolase that belongs to the subgroup of the α,β-hydrolase fold-containing proteins, which is involved in virus propagation, immune response, and fertilization. Chemical tools to selectively modulate the activity of ABHD2 in an acute setting are highly desired to investigate its biological role, but are currently lacking. Here, we report a library-versus-library screening using activity-based protein profiling (ABPP) to evaluate in parallel the selectivity and activity of a focused lipase inhibitor library against ABHD2 and a panel of closely related ABHD proteins. This screen resulted in the rapid identification of novel inhibitors for ABHD2. The selectivity of the inhibitor was further investigated in native mouse testis proteome by competitive ABPP, revealing a highly

SUBMITTER: Baggelaar MP 

PROVIDER: S-EPMC6878212 | biostudies-literature | 2019 Oct

REPOSITORIES: biostudies-literature