CCK2R antagonists: from SAR to clinical trials
作者： Doroteja Novak , Marko Anderluh , Petra Kolenc Peitl
DOI: 10.1016/J.DRUDIS.2020.05.008
关键词: Phases of clinical research 、 Bioinformatics 、 Antagonist 、 Clinical trial 、 Netazepide 、 Gastrin 、 Medicine
摘要: 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 past three decades, considerable research yielded numerous chemically heterogeneous compounds. None these entered into clinic, mainly because inadequate biological effects. However, it appears that ultimate goal a clinically useful antagonist is now just around corner, with most promising compounds, netazepide and nastorazepide, Phase II clinical trials. Here, we illustrate structure–activity relationships (SARs) stablished antagonists various structural classes, recent proof-of-concept studies where new applicabilities as visualizing agents are presented.
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