Early evaluation of opportunities in oral delivery of PROTACs to overcome their molecular challenges

Drug Discov Today. 2023 Dec 26:103865. doi: 10.1016/j.drudis.2023.103865. Online ahead of print.ABSTRACTPROteolysis TArgeting Chimeras (PROTACs) offer new opportunities in modern medicine by targeting proteins that are intractable to classic inhibitors. Heterobifunctional in nature, PROTACs are small molecules that offer a unique mechanism of protein degradation by hijacking the ubiquitin-mediated protein degradation pathway, known as the ubiquitin-proteasome system. Herein, we present an analysis on the structural characteristics of this novel chemical modality. Furthermore, we review and discuss the formulation opportunities to overcome the oral delivery challenges of PROTACs in drug discovery.PMID:38154757 | DOI:10.1016/j.drudis.2023.103865
Source: Drug Discovery Today - Category: Drugs & Pharmacology Authors: Source Type: research