Enriching Proteolysis Targeting Chimeras with a Second Modality: When Two Are Better Than One.

ABSTRACT: Proteolysis targeting chimera (PROTAC)-mediated protein degradation has prompted a radical rethink and is at a crucial stage in driving a drug discovery transition. To fully harness the potential of this technology, a growing paradigm toward enriching PROTACs with other therapeutic modalities has been proposed. Could researchers successfully combine two modalities to yield multifunctional PROTACs with an expanded profile? In this Perspective, we try to answer this question. We discuss how this possibility encompasses different approaches, leading to multitarget PROTACs, light-controllable PROTACs, PROTAC conjugates, and macrocycle- and oligonucleotide-based PROTACs. This possibility promises to further enhance PROTAC efficacy and selectivity, minim

SUBMITTER: Salerno A 

PROVIDER: S-EPMC9340767 | biostudies-literature | 2022 Jul

REPOSITORIES: biostudies-literature