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CCK2R antagonists: from SAR to clinical trials.
Drug Discovery Today ( IF 7.4 ) Pub Date : 2020-05-18 , DOI: 10.1016/j.drudis.2020.05.008
Doroteja Novak 1 , Marko Anderluh 2 , Petra Kolenc Peitl 3
Affiliation  

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.



中文翻译:

CCK2R 拮抗剂:从 SAR 到临床试验。

胆囊收缩素-2/胃泌素受体 (CCK 2 R) 在多个(病理)生理过程中的广泛参与推动了对非肽小分子 CCK 2 R 拮抗剂的广泛研究。在过去的三十年里,大量的研究已经产生了许多化学异质化合物。这些都没有进入临床,主要是因为生物学效应不足。然而,临床上有用的 CCK 2 R 拮抗剂的最终目标似乎即将实现,最有希望的化合物,netazepide 和 nastorazepide,现在处于 II 期临床试验。在这里,我们说明了稳定的 CCK 2 的构效关系 (SAR)各种结构类别的 R 拮抗剂,以及最新的概念验证研究,其中介绍了 CCK 2 R 拮抗剂作为可视化剂的新适用性。

更新日期:2020-05-18
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