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	Structural and functional analyses of a GPCR-inhibited ion channel TRPM3.
Journal, issue, pages	Neuron, Vol. 111, Issue 1, Page 81-91.e7, Year 2023
Publish date	Jan 4, 2023
Authors	Chen Zhao / Roderick MacKinnon /
PubMed Abstract	G-protein coupled receptors (GPCRs) govern the physiological response to stimuli by modulating the activity of downstream effectors, including ion channels. TRPM3 is an ion channel inhibited by GPCRs ...G-protein coupled receptors (GPCRs) govern the physiological response to stimuli by modulating the activity of downstream effectors, including ion channels. TRPM3 is an ion channel inhibited by GPCRs through direct interaction with G protein (Gβγ) released upon their activation. This GPCR-TRPM3 signaling pathway contributes to the analgesic effect of morphine. Here, we characterized Gβγ inhibition of TRPM3 using electrophysiology and single particle cryo-electron microscopy (cryo-EM). From electrophysiology, we obtained a half inhibition constant (IC50) of ∼240 nM. Using cryo-EM, we determined structures of mouse TRPM3 expressed in human cells with and without Gβγ and with and without PIP, a lipid required for TRPM3 activity, at resolutions of 2.7-4.7 Å. Gβγ-TRPM3 interfaces vary depending on PIP occupancy; however, in all cases, Gβγ appears loosely attached to TRPM3. The IC50 in electrophysiology experiments raises the possibility that additional unknown factors may stabilize the TRPM3-Gβγ complex.
External links	Neuron / PubMed:36283409
Methods	EM (single particle)
Resolution	2.7 - 4.7 Å
Structure data	27338 8ddq EMDB-27338, PDB-8ddq: cryo-EM structure of TRPM3 ion channel in the presence of soluble Gbg, focused on channel Method: EM (single particle) / Resolution: 2.7 Å 27339 8ddr EMDB-27339, PDB-8ddr: cryo-EM structure of TRPM3 ion channel in the absence of PIP2 Method: EM (single particle) / Resolution: 3.2 Å 27340 8dds EMDB-27340, PDB-8dds: cryo-EM structure of TRPM3 ion channel in the presence of PIP2, state1 Method: EM (single particle) / Resolution: 3.5 Å 27341 8ddt EMDB-27341, PDB-8ddt: cryo-EM structure of TRPM3 ion channel in the presence of PIP2, state2 Method: EM (single particle) / Resolution: 3.1 Å 27342 8ddu EMDB-27342, PDB-8ddu: cryo-EM structure of TRPM3 ion channel in the presence of PIP2, state3 Method: EM (single particle) / Resolution: 3.0 Å 27343 8ddv EMDB-27343, PDB-8ddv: Cryo-EM structure of TRPM3 ion channel in the presence of PIP2, state4 Method: EM (single particle) / Resolution: 3.2 Å 27344 8ddw EMDB-27344, PDB-8ddw: cryo-EM structure of TRPM3 ion channel in complex with Gbg, tethered by ALFA-nanobody Method: EM (single particle) / Resolution: 4.7 Å 27345 8ddx EMDB-27345, PDB-8ddx: cryo-EM structure of TRPM3 ion channel in complex with Gbg in the presence of PIP2, tethered by ALFA-nanobody Method: EM (single particle) / Resolution: 3.8 Å 28031 8ed7 EMDB-28031, PDB-8ed7: cryo-EM structure of TRPM3 ion channel in apo state Method: EM (single particle) / Resolution: 3.7 Å 28032 8ed8 EMDB-28032, PDB-8ed8: cryo-EM structure of TRPM3 ion channel in the presence of PIP2 and PregS, state 1 Method: EM (single particle) / Resolution: 3.2 Å 28033 8ed9 EMDB-28033, PDB-8ed9: cryo-EM structure of TRPM3 ion channel in the presence with PIP2 and PregS, state 2 Method: EM (single particle) / Resolution: 3.4 Å
Chemicals	ChemComp-3PH: 1,2-DIACYL-GLYCEROL-3-SN-PHOSPHATE / Phosphatidic acid ChemComp-9Z9: (3beta,14beta,17beta,25R)-3-[4-methoxy-3-(methoxymethyl)butoxy]spirost-5-en / detergentYM ChemComp-NA: Unknown entry ChemComp-PIO*: [(2R)-2-octanoyloxy-3-[oxidanyl-[(1R,2R,3S,4R,5R,6S)-2,3,6-tris(oxidanyl)-4,5-diphosphonooxy-cyclohexyl]oxy-phosphoryl]oxy-propyl] octanoate
Source	mus musculus (house mouse) homo sapiens (human)
Keywords	MEMBRANE PROTEIN / TRPM3 / ion channel / Gbg / PIP2