Article
The structural basis for an on-off switch controlling Gβγ-mediated inhibition of TRPM3 channels.
Proceedings of the National Academy of Sciences of the United States of America - 17 Nov 2020
Behrendt Marc, Gruss Fabian, Enzeroth Raissa, Dembla Sandeep, Zhao Siyuan, Crassous Pierre-Antoine, Mohr Florian, Nys Mieke, Louros Nikolaos, Gallardo Rodrigo, Zorzini Valentina, Wagner Doris, Economou Anastassios, Rousseau Frederic, Schymkowitz Joost, Philipp Stephan E, Rohacs Tibor, Ulens Chris, Oberwinkler Johannes
Abstract excerpt
TRPM3 channels play important roles in the detection of noxious heat and in inflammatory thermal hyperalgesia. The activity of these ion channels in somatosensory neurons is tightly regulated by µ-opioid receptors through the signaling of Gβγ proteins, thereby reducing TRPM3-mediated pain. We show here that Gβγ directly binds to a domain of 10 amino acids in TRPM3 and solve a cocrystal structure of this domain...
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