CCK2R antagonists: from SAR to clinical trials.

CCK2R antagonists: from SAR to clinical trials.
Drug Discov Today. 2020 May 18;:
Authors: Novak D, Anderluh M, Peitl PK
Abstract
The widespread involvement of the cholecystokinin-2/gastrin receptor (CCK2R) in multiple (patho)physiological processes has propelled extensive searches for nonpeptide small-molecule CCK2R antagonists. For the past three decades, considerable research has yielded numerous chemically heterogeneous compounds. None of these entered into the clinic, mainly because of inadequate biological effects. However, it appears that the ultimate goal of a clinically useful CCK2R antagonist is now just around the corner, with the most promising compounds, netazepide and nastorazepide, now in Phase II clinical trials. Here, we illustrate the structure-activity relationships (SARs) of stablished CCK2R antagonists of various structural classes, and the most recent proof-of-concept studies where new applicabilities of CCK2R antagonists as visualizing agents are presented.
PMID: 32439608 [PubMed - as supplied by publisher]

Source: Drug Discovery Today - May 17, 2020 Category: Drugs & Pharmacology Authors: Novak D, Anderluh M, Peitl PK Tags: Drug Discov Today Source Type: research