Structure-affinity and structure-residence time relationships of macrocyclic Gαq protein inhibitors

Structure-affinity and structure-residence time relationships of macrocyclic Gαq protein inhibitors

Summary: The macrocyclic depsipeptides YM-254890 (YM) and FR900359 (FR) are potent inhibitors of Gαq/11 proteins. They are important pharmacological tools and have potential as therapeutic drugs. The hydrogenated, tritium-labeled YM and FR derivatives display largely different residence times despit...

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Bibliographic Details
Main Authors: Jan H. Voss, Max Crüsemann, Christian R.O. Bartling, Stefan Kehraus, Asuka Inoue, Gabriele M. König, Kristian Strømgaard, Christa E. Müller
Format: Article
Language:English
Published: Elsevier 2023-04-01
Series:iScience
Subjects:
Pharmacology
Biological sciences
Biochemistry
Online Access:http://www.sciencedirect.com/science/article/pii/S2589004223005692

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http://www.sciencedirect.com/science/article/pii/S2589004223005692

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