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