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- W3177102087 abstract "The Ca2+-activated TRPM5 channel plays essential roles in taste perception and insulin secretion. However, the mechanism by which Ca2+ regulates TRPM5 activity remains elusive. We report cryo-EM structures of the zebrafish TRPM5 in an apo closed state, a Ca2+-bound open state, and an antagonist-bound inhibited state. We define two novel ligand binding sites: a Ca2+ site (CaICD) in the intracellular domain and an antagonist site in the transmembrane domain (TMD). The CaICD site is unique to TRPM5 and has two roles: modulating the voltage dependence and promoting Ca2+ binding to the CaTMD site, which is conserved throughout TRPM channels. Conformational changes initialized from both Ca2+ sites cooperatively open the ion-conducting pore. The antagonist NDNA wedges into the space between the S1-S4 domain and pore domain, stabilizing the transmembrane domain in an apo-like closed state. Our results lay the foundation for understanding the voltage-dependent TRPM channels and developing new therapeutic agents." @default.
- W3177102087 created "2021-07-05" @default.
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- W3177102087 date "2021-06-24" @default.
- W3177102087 modified "2023-10-01" @default.
- W3177102087 title "Structures of the TRPM5 channel elucidate mechanisms of activation and inhibition" @default.
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- W3177102087 doi "https://doi.org/10.1038/s41594-021-00607-4" @default.
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