Database of articles cited by EMDB/PDB/SASBDB data

Keywords
Structure methods	All X-ray diffraction NMR electron microscopy small angle scattering neutron diffraction fiber diffraction powder diffraction infrared spectroscopy EPR fluorescence transfer theoretical model Hybrid
Author
Journal
IF	>30 >20 >10 >5 all

Title	A single allosteric site merges activation, modulation and inhibition in TRPM5.
Journal, issue, pages	Nat Chem Biol, Year 2026
Publish date	Jan 5, 2026
Authors	Zheng Ruan / Junuk Lee / Yangyang Li / Ian J Orozco / Juan Du / Wei Lü /
PubMed Abstract	TRPM5 is a Ca-activated monovalent cation channel essential for taste perception, insulin secretion and gastrointestinal chemosensation. Canonical TRPM5 activation requires Ca binding at two distinct ...TRPM5 is a Ca-activated monovalent cation channel essential for taste perception, insulin secretion and gastrointestinal chemosensation. Canonical TRPM5 activation requires Ca binding at two distinct sites: an agonist site within the lower vestibule of the S1-S4 pocket in the transmembrane domain (Ca) and a modulatory site in the intracellular domain (Ca) that tunes voltage dependence and agonist sensitivity. Here we characterize CBTA as a noncalcium agonist that binds to the upper vestibule of the S1-S4 pocket, directly above Ca. CBTA alone mimics the dual role of Ca and Ca, merging agonist activation with voltage modulation. CBTA also renders TRPM5 supersensitive to Ca, synergistically hyperactivating the channel even at near-resting Ca levels. We further demonstrate that the inhibitor triphenylphosphine oxide binds the same site but stabilizes a nonconductive state. These opposing effects reveal the upper S1-S4 pocket as a multifunctional regulatory hub integrating activation, inhibition and modulation in TRPM5.
External links	Nat Chem Biol / PubMed:41491833
Methods	EM (single particle)
Resolution	2.75 - 3.5 Å
Structure data	EMDB-71244: The consensus map of zebrafish TRPM5 with 1mM EDTA and 0.5mM CBTA Method: EM (single particle) / Resolution: 3.1 Å 71245 9p3n EMDB-71245, PDB-9p3n: The open state of zebrafish TRPM5 with 1mM EDTA and 0.5mM CBTA Method: EM (single particle) / Resolution: 3.5 Å 71246 9p3o EMDB-71246, PDB-9p3o: Zebrafish TRPM5 with 5mM calcium and 0.5mM CBTA Method: EM (single particle) / Resolution: 2.92 Å EMDB-71247: Zebrafish TRPM5 with 0.2mM calcium Method: EM (single particle) / Resolution: 2.9 Å EMDB-71248: Zebrafish TRPM5 with 1uM calcium Method: EM (single particle) / Resolution: 3.24 Å EMDB-71249: Zebrafish TRPM5 with 2uM Ca in GDN detergent Method: EM (single particle) / Resolution: 3.3 Å 71250 9p3p EMDB-71250, PDB-9p3p: Zebrafish TRPM5 with 5mM EGTA and 0.5mM CBTA Method: EM (single particle) / Resolution: 3.0 Å 71251 9p3q EMDB-71251, PDB-9p3q: Zebrafish TRPM5 D797A mutant with 5mM calcium Method: EM (single particle) / Resolution: 3.5 Å 71252 9p3r EMDB-71252, PDB-9p3r: Zebrafish TRPM5 D797A mutant with 5mM calcium and 0.5mM CBTA Method: EM (single particle) / Resolution: 3.5 Å 71253 9p3s EMDB-71253, PDB-9p3s: Zebrafish TRPM5 D797N mutant with 5mM calcium and 0.5mM CBTA Method: EM (single particle) / Resolution: 3.27 Å 71254 9p3t EMDB-71254, PDB-9p3t: Zebrafish TRPM5 with 5mM calcium and 0.5mM TPPO Method: EM (single particle) / Resolution: 3.0 Å 71255 9p3u EMDB-71255, PDB-9p3u: Zebrafish TRPM5 E337A mutant with 5mM calcium and 0.5mM CBTA Method: EM (single particle) / Resolution: 2.75 Å 71256 9p3v EMDB-71256, PDB-9p3v: Zebrafish TRPM5 Q771A mutant with 5mM calcium and 0.5mM CBTA Method: EM (single particle) / Resolution: 2.75 Å 71257 9p3w EMDB-71257, PDB-9p3w: Zebrafish TRPM5 Q771A mutant with 5mM calcium Method: EM (single particle) / Resolution: 2.85 Å
Chemicals	ChemComp-CA: Unknown entry ChemComp-YUY: (2R)-2-(hydroxymethyl)-4-{[(25R)-10alpha,14beta,17beta-spirost-5-en-3beta-yl]oxy}butyl 4-O-alpha-D-glucopyranosyl-beta-D-glucopyranoside ChemComp-YUV: (25R)-14beta,17beta-spirost-5-en-3beta-ol PDB-1cgw: SITE DIRECTED MUTATIONS OF THE ACTIVE SITE RESIDUE TYROSINE 195 OF CYCLODEXTRIN GLYCOSYLTRANSFERASE FROM BACILLUS CIRCULANS STRAIN 251 AFFECTING ACTIVITY AND PRODUCT SPECIFICITY ChemComp-NAG: 2-acetamido-2-deoxy-beta-D-glucopyranose PDB-1cgz: CHALCONE SYNTHASE FROM ALFALFA COMPLEXED WITH RESVERATROL PDB-1cg0: STRUCTURE OF ADENYLOSUCCINATE SYNTHETASE FROM E. COLI COMPLEXED WITH HADACIDIN, GDP, 6-PHOSPHORYL-IMP, AND MG2+ PDB-1cg5: DEOXY FORM HEMOGLOBIN FROM DASYATIS AKAJEI ChemComp-HOH: WATER
Source	danio rerio (zebrafish)
Keywords	TRANSPORT PROTEIN / TRPM5 channel; ion channel; cation channel; sodium channel; calcium; CBTA / TRPM5 channel / ion channel / cation channel / sodium channel / TRANSFERASE