A Toolbox for the Generation of Chemical Probes for Baculovirus IAP Repeat Containing Proteins.

ABSTRACT: E3 ligases constitute a large and diverse family of proteins that play a central role in regulating protein homeostasis by recruiting substrate proteins via recruitment domains to the proteasomal degradation machinery. Small molecules can either inhibit, modulate or hijack E3 function. The latter class of small molecules led to the development of selective protein degraders, such as PROTACs (PROteolysis TArgeting Chimeras), that recruit protein targets to the ubiquitin system leading to a new class of pharmacologically active drugs and to new therapeutic options. Recent efforts have focused on the E3 family of Baculovirus IAP Repeat (BIR) domains that comprise a structurally conserved but diverse 70 amino acid long protein interaction domain. In the human proteome, 16 BIR domains ha

SUBMITTER: Schwalm MP 

PROVIDER: S-EPMC9204419 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature