Ontology highlight
ABSTRACT:
SUBMITTER: Klein VG
PROVIDER: S-EPMC7488288 | biostudies-literature | 2020 Sep
REPOSITORIES: biostudies-literature
Klein Victoria G VG Townsend Chad E CE Testa Andrea A Zengerle Michael M Maniaci Chiara C Hughes Scott J SJ Chan Kwok-Ho KH Ciulli Alessio A Lokey R Scott RS
ACS medicinal chemistry letters 20200730 9
Proteolysis targeting chimeras (PROTACs) are catalytic heterobifunctional molecules that can selectively degrade a protein of interest by recruiting a ubiquitin E3 ligase to the target, leading to its ubiquitylation and degradation by the proteasome. Most degraders lie outside the chemical space associated with most membrane-permeable drugs. Although many PROTACs have been described with potent activity in cells, our understanding of the relationship between structure and permeability in these c ...[more]