7AD3
 
 | | Class D GPCR Ste2 dimer coupled to two G proteins | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Alpha-factor mating pheromone, CHOLESTEROL HEMISUCCINATE, ... | | Authors: | Velazhahan, V, Tate, C. | | Deposit date: | 2020-09-14 | | Release date: | 2020-12-09 | | Last modified: | 2021-01-13 | | Method: | ELECTRON MICROSCOPY (3.5 Å) | | Cite: | Structure of the class D GPCR Ste2 dimer coupled to two G proteins.
Nature, 589, 2021
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7BW0
 | | Active human TGR5 complex with a synthetic agonist 23H | | Descriptor: | Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(s) subunit alpha isoforms short,Guanine nucleotide-binding protein G(s) subunit alpha isoforms short, ... | | Authors: | Chen, G, Wang, X.K, Chen, Q, Hu, H.L, Ren, R.B. | | Deposit date: | 2020-04-12 | | Release date: | 2020-09-02 | | Last modified: | 2024-03-27 | | Method: | ELECTRON MICROSCOPY (3.9 Å) | | Cite: | Cryo-EM structure of activated bile acids receptor TGR5 in complex with stimulatory G protein.
Signal Transduct Target Ther, 5, 2020
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7BZ2
 | | Cryo-EM structure of the formoterol-bound beta2 adrenergic receptor-Gs protein complex. | | Descriptor: | Beta2 adrenergic receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, ... | | Authors: | Zhang, Y.N, Yang, F, Ling, S.L, Lv, P, Zhou, Y.X, Fang, W, Sun, W, Shi, P, Tian, C.L. | | Deposit date: | 2020-04-26 | | Release date: | 2020-08-05 | | Method: | ELECTRON MICROSCOPY (3.82 Å) | | Cite: | Single-particle cryo-EM structural studies of the beta2AR-Gs complex bound with a full agonist formoterol.
Cell Discov, 6, 2020
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5HE2
 | | Bovine GRK2 in complex with Gbetagamma subunits and CCG224406 | | Descriptor: | (4~{S})-4-[3-[(2,6-dimethoxyphenyl)methylcarbamoyl]-4-fluoranyl-phenyl]-~{N}-(1~{H}-indazol-5-yl)-6-methyl-2-oxidanylidene-3,4-dihydro-1~{H}-pyrimidine-5-carboxamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Cato, M.C, Waninger-Saroni, J, Tesmer, J.J.G. | | Deposit date: | 2016-01-05 | | Release date: | 2016-05-11 | | Last modified: | 2024-03-06 | | Method: | X-RAY DIFFRACTION (2.79 Å) | | Cite: | Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors.
J.Med.Chem., 59, 2016
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8SOE
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8SOD
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8SOC
 | | Phosphoinositide phosphate 3 kinase gamma bound with ADP and Gbetagamma | | Descriptor: | ADENOSINE-5'-DIPHOSPHATE, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, ... | | Authors: | Chen, C.-L, Tesmer, J.J.G. | | Deposit date: | 2023-04-28 | | Release date: | 2024-04-03 | | Last modified: | 2024-04-17 | | Method: | ELECTRON MICROSCOPY (3.5 Å) | | Cite: | Molecular basis for G beta gamma-mediated activation of phosphoinositide 3-kinase gamma.
Nat.Struct.Mol.Biol., 2024
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8SL3
 | | Human adenylyl Cyclase 5 in complex with Gbg | | Descriptor: | Adenylate cyclase type 5, GERAN-8-YL GERAN, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Yen, Y.C, Tesmer, J.J.G. | | Deposit date: | 2023-04-20 | | Release date: | 2024-04-03 | | Last modified: | 2024-04-24 | | Method: | ELECTRON MICROSCOPY (7 Å) | | Cite: | Structure of adenylyl cyclase 5 in complex with G beta gamma offers insights into ADCY5-related dyskinesia.
Nat.Struct.Mol.Biol., 2024
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8T3V
 | | Cryo-EM structure of the DHA bound FFA1-Gq complex | | Descriptor: | CHOLESTEROL, DOCOSA-4,7,10,13,16,19-HEXAENOIC ACID, Free fatty acid receptor 1, ... | | Authors: | Zhang, X, Tikhonova, I, Milligan, G, Zhang, C. | | Deposit date: | 2023-06-07 | | Release date: | 2024-01-24 | | Method: | ELECTRON MICROSCOPY (3.39 Å) | | Cite: | Structural basis for the ligand recognition and signaling of free fatty acid receptors.
Sci Adv, 10, 2024
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6B3J
 | | 3.3 angstrom phase-plate cryo-EM structure of a biased agonist-bound human GLP-1 receptor-Gs complex | | Descriptor: | Exendin-P5, Glucagon-like peptide 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Liang, Y.L, Khoshouei, M, Glukhova, A, Furness, S.G.B, Koole, C, Zhao, P, Clydesdale, L, Thal, D.M, Radjainia, M, Danev, R, Baumeister, W, Wang, M.W, Miller, L.J, Christopoulos, A, Sexton, P.M, Wootten, D. | | Deposit date: | 2017-09-22 | | Release date: | 2018-02-21 | | Last modified: | 2020-01-15 | | Method: | ELECTRON MICROSCOPY (3.3 Å) | | Cite: | Phase-plate cryo-EM structure of a biased agonist-bound human GLP-1 receptor-Gs complex.
Nature, 555, 2018
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6B20
 | | Crystal structure of a complex between G protein beta gamma dimer and an inhibitory Nanobody regulator | | Descriptor: | CHLORIDE ION, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(T) subunit gamma-T1, ... | | Authors: | Gulati, S, Kiser, P.D, Palczewski, K. | | Deposit date: | 2017-09-19 | | Release date: | 2018-05-30 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.34 Å) | | Cite: | Targeting G protein-coupled receptor signaling at the G protein level with a selective nanobody inhibitor.
Nat Commun, 9, 2018
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6C2Y
 | | Human GRK2 in complex with Gbetagamma subunits and CCG257142 | | Descriptor: | (4R,5R,6S)-4-[4-fluoro-3-({[3-(methoxymethyl)-1,2,4-oxadiazol-5-yl]methyl}carbamoyl)phenyl]-N-(2H-indazol-5-yl)-6-methyl-2-oxohexahydropyrimidine-5-carboxamide, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Bouley, R, Tesmer, J.J.G. | | Deposit date: | 2018-01-09 | | Release date: | 2018-04-25 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.74 Å) | | Cite: | Utilizing a structure-based docking approach to develop potent G protein-coupled receptor kinase (GRK) 2 and 5 inhibitors.
Bioorg. Med. Chem. Lett., 28, 2018
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6CRK
 | | Heterotrimeric G-protein in complex with an antibody fragment | | Descriptor: | CITRATE ANION, GUANOSINE-5'-DIPHOSPHATE, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Maeda, S, Dawson, R, Kobilka, B. | | Deposit date: | 2018-03-19 | | Release date: | 2018-10-24 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Development of an antibody fragment that stabilizes GPCR/G-protein complexes.
Nat Commun, 9, 2018
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6CMO
 | | Rhodopsin-Gi complex | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Fab Heavy chain, Fab light chain, ... | | Authors: | Kang, Y, Kuybeda, O, de Waal, P.W, Mukherjee, S, Van Eps, N, Dutka, P, Zhou, X.E, Bartesaghi, A, Erramilli, S, Morizumi, T, Gu, X, Yin, Y, Liu, P, Jiang, Y, Meng, X, Zhao, G, Melcher, K, Earnst, O.P, Kossiakoff, A.A, Subramaniam, S, Xu, H.E. | | Deposit date: | 2018-03-05 | | Release date: | 2018-06-20 | | Last modified: | 2020-07-29 | | Method: | ELECTRON MICROSCOPY (4.5 Å) | | Cite: | Cryo-EM structure of human rhodopsin bound to an inhibitory G protein.
Nature, 558, 2018
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7MBX
 | | Human Cholecystokinin 1 receptor (CCK1R) Gs complex | | Descriptor: | CHOLESTEROL HEMISUCCINATE, Cholecystokinin receptor type A, Cholecystokinin-8, ... | | Authors: | Mobbs, J.I, Belousoff, M.J, Danev, R, Thal, D.M, Sexton, P.M. | | Deposit date: | 2021-04-01 | | Release date: | 2021-05-26 | | Last modified: | 2021-07-14 | | Method: | ELECTRON MICROSCOPY (1.95 Å) | | Cite: | Structures of the human cholecystokinin 1 (CCK1) receptor bound to Gs and Gq mimetic proteins provide insight into mechanisms of G protein selectivity.
Plos Biol., 19, 2021
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7MBY
 | | Human Cholecystokinin 1 receptor (CCK1R) Gq chimera (mGsqi) complex | | Descriptor: | CHOLESTEROL HEMISUCCINATE, Cholecystokinin receptor type A, Cholecystokinin-8, ... | | Authors: | Mobbs, J.I, Belousoff, M.J, Danev, R, Thal, D.M, Sexton, P.M. | | Deposit date: | 2021-04-01 | | Release date: | 2021-05-26 | | Last modified: | 2021-07-14 | | Method: | ELECTRON MICROSCOPY (2.44 Å) | | Cite: | Structures of the human cholecystokinin 1 (CCK1) receptor bound to Gs and Gq mimetic proteins provide insight into mechanisms of G protein selectivity.
Plos Biol., 19, 2021
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6DDF
 | | Mu Opioid Receptor-Gi Protein Complex | | Descriptor: | DAMGO, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, ... | | Authors: | Koehl, A, Hu, H, Maeda, S, Manglik, A, Kobilka, B.K, Skiniotis, G, Weis, W.I. | | Deposit date: | 2018-05-10 | | Release date: | 2018-06-13 | | Last modified: | 2023-11-15 | | Method: | ELECTRON MICROSCOPY (3.5 Å) | | Cite: | Structure of the mu-opioid receptor-Giprotein complex.
Nature, 558, 2018
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7MTS
 | | CryoEM Structure of mGlu2 - Gi Complex | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-methoxy-6-propyl-N-(2-{4-[(1H-tetrazol-5-yl)methoxy]phenyl}ethyl)thieno[2,3-d]pyrimidin-4-amine, GLUTAMIC ACID, ... | | Authors: | Seven, A.B, Barros-Alvarez, X, Skiniotis, G. | | Deposit date: | 2021-05-13 | | Release date: | 2021-07-07 | | Last modified: | 2021-07-28 | | Method: | ELECTRON MICROSCOPY (3.2 Å) | | Cite: | G-protein activation by a metabotropic glutamate receptor.
Nature, 595, 2021
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6E3Y
 | | Cryo-EM structure of the active, Gs-protein complexed, human CGRP receptor | | Descriptor: | Calcitonin gene-related peptide 1, Calcitonin gene-related peptide type 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Liang, Y.L, Khoshouei, M, Deganutti, G, Glukhova, A, Koole, C, Peat, T.S, Radjainia, M, Plitzko, J.M, Baumeister, W, Miller, L.J, Hay, D.L, Christopoulos, A, Reynolds, C.A, Wootten, D, Sexton, P.M. | | Deposit date: | 2018-07-16 | | Release date: | 2018-09-19 | | Last modified: | 2020-01-15 | | Method: | ELECTRON MICROSCOPY (3.3 Å) | | Cite: | Cryo-EM structure of the active, Gs-protein complexed, human CGRP receptor.
Nature, 561, 2018
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7P00
 | | Human Neurokinin 1 receptor (NK1R) substance P Gq chimera (mGsqi) complex | | Descriptor: | Antibody fragment scFv16, CHOLESTEROL, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Thom, C, Ehrenmann, J, Vacca, S, Waltenspuhl, Y, Schoppe, J, Medalia, O, Pluckthun, A. | | Deposit date: | 2021-06-29 | | Release date: | 2021-12-15 | | Method: | ELECTRON MICROSCOPY (2.71 Å) | | Cite: | Structures of neurokinin 1 receptor in complex with G q and G s proteins reveal substance P binding mode and unique activation features.
Sci Adv, 7, 2021
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7P02
 | | Human Neurokinin 1 receptor (NK1R) substance P Gs complex | | Descriptor: | Antibody fragment scFv16, CHOLESTEROL, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Thom, C, Ehrenmann, J, Vacca, S, Waltenspuhl, Y, Schoppe, J, Medalia, O, Pluckthun, A. | | Deposit date: | 2021-06-29 | | Release date: | 2021-12-15 | | Method: | ELECTRON MICROSCOPY (2.87 Å) | | Cite: | Structures of neurokinin 1 receptor in complex with G q and G s proteins reveal substance P binding mode and unique activation features.
Sci Adv, 7, 2021
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6EG8
 | | Structure of the GDP-bound Gs heterotrimer | | Descriptor: | GUANOSINE-5'-DIPHOSPHATE, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, ... | | Authors: | Hilger, D, Liu, X, Aschauer, P, Kobilka, B.K. | | Deposit date: | 2018-08-19 | | Release date: | 2019-06-05 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Structural Insights into the Process of GPCR-G Protein Complex Formation.
Cell, 177, 2019
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7PWD
 | | Structure of an inhibited GRK2-G-beta and G-gamma complex | | Descriptor: | 4-chloranyl-N-[2-(4-chlorophenyl)ethyl]thieno[2,3-c]pyridine-2-carboxamide, Beta-adrenergic receptor kinase 1, CHLORIDE ION, ... | | Authors: | Faucher, N, Tauchert, M.J, Konz Makino, D.L, Vuillard, L.M. | | Deposit date: | 2021-10-06 | | Release date: | 2021-10-20 | | Last modified: | 2024-06-19 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Synthesis of thieno[2,3-c]pyridine derived GRK2 inhibitors
Monatsh Chem, 2022
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7PIU
 | | Cryo-EM structure of the agonist setmelanotide bound to the active melanocortin-4 receptor (MC4R) in complex with the heterotrimeric Gs protein at 2.6 A resolution. | | Descriptor: | CALCIUM ION, Camelid antibody fragment - nanobody 35, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Heyder, N.A, Schmidt, A, Kleinau, G, Hilal, T, Scheerer, P. | | Deposit date: | 2021-08-23 | | Release date: | 2021-11-17 | | Method: | ELECTRON MICROSCOPY (2.58 Å) | | Cite: | Structures of active melanocortin-4 receptor-Gs-protein complexes with NDP-alpha-MSH and setmelanotide.
Cell Res., 31, 2021
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7PIV
 | | Active Melanocortin-4 receptor (MC4R)- Gs protein complex bound to agonist NDP-alpha-MSH at 2.86 A resolution. | | Descriptor: | CALCIUM ION, Camelid antibody VHH fragment - nanobody 35, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Heyder, N.A, Schmidt, A, Kleinau, G, Hilal, T, Scheerer, P. | | Deposit date: | 2021-08-23 | | Release date: | 2021-11-17 | | Method: | ELECTRON MICROSCOPY (2.86 Å) | | Cite: | Structures of active melanocortin-4 receptor-Gs-protein complexes with NDP-alpha-MSH and setmelanotide.
Cell Res., 31, 2021
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