Probing Biological Mechanisms with Chemical Tools

Publication date: Available online 18 January 2020Source: Pharmacological ResearchAuthor(s): Congbao Kang, Thomas H. KellerAbstractTraditionally small molecules have mainly been used to inhibit biochemical activities of proteins, however such compounds can also be used to change the conformational energy landscape of proteins. Tool compounds that allosterically modulate protein conformations often reveal unexpected biological mechanisms, which have therapeutic potential. We discuss two examples where screening hits were found to bind to unexpected binding pockets on well know proteins, establishing new routes for the inhibition of proteins that were thought to be undruggable.Graphical abstract
Source: Pharmacological Research - Category: Drugs & Pharmacology Source Type: research