Rapalogues as hCES2A Inhibitors: In Vitro and In Silico Investigations

ConclusionOur findings demonstrate that several marketed rapalogues are potent and specific hCES2A inhibitors, and these agents can serve as leading compounds for the development of more efficacious hCES2A inhibitors to modulate the pharmacokinetic profiles and toxicity of hCES2A-substrate drugs (such as the anticancer agent irinotecan).Graphic Abstract
Source: European Journal of Drug Metabolism and Pharmacokinetics - Category: Drugs & Pharmacology Source Type: research