8K8J
 
 | | Cannabinoid Receptor 1 bound to Fenofibrate coupling MiniGsq and Nb35 Complex | | 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, ... | | Authors: | Tang, W.Q, Wang, T.X, Li, F.H, Wang, J.Y. | | Deposit date: | 2023-07-30 | | Release date: | 2024-02-14 | | Last modified: | 2024-04-24 | | Method: | ELECTRON MICROSCOPY (2.88 Å) | | Cite: | Fenofibrate Recognition and G q Protein Coupling Mechanisms of the Human Cannabinoid Receptor CB1.
Adv Sci, 11, 2024
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8I95
 | | Structure of EP54-C3aR-Go complex | | Descriptor: | Antibody fragment - ScFv16, C3a anaphylatoxin chemotactic receptor, EP54 ligand, ... | | Authors: | Yadav, M.K, Yadav, R, Maharana, J, Sarma, P, Banerjee, R, Shukla, A.K, Gati, C. | | Deposit date: | 2023-02-06 | | Release date: | 2023-10-18 | | Last modified: | 2023-11-08 | | Method: | ELECTRON MICROSCOPY (2.88 Å) | | Cite: | Molecular basis of anaphylatoxin binding, activation, and signaling bias at complement receptors.
Cell, 186, 2023
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8FN0
 | | CryoEM structure of Go-coupled NTSR1 with a biased allosteric modulator | | Descriptor: | 2-[{2-(1-fluorocyclopropyl)-4-[4-(2-methoxyphenyl)piperidin-1-yl]quinazolin-6-yl}(methyl)amino]ethan-1-ol, 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: | Krumm, B.E, DiBerto, J.F, Olsen, R.H.J, Kang, H, Slocum, S.T, Zhang, S, Strachan, R.T, Fay, J.F, Roth, B.L. | | Deposit date: | 2022-12-26 | | Release date: | 2023-03-29 | | Last modified: | 2023-04-19 | | Method: | ELECTRON MICROSCOPY (2.89 Å) | | Cite: | Neurotensin Receptor Allosterism Revealed in Complex with a Biased Allosteric Modulator.
Biochemistry, 62, 2023
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8W8Q
 | | Cryo-EM structure of the GPR101-Gs complex | | 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, ... | | Authors: | Sun, J.P, Gao, N, Yu, X, Wang, G.P, Yang, F, Wang, J.Y, Yang, Z, Guan, Y. | | Deposit date: | 2023-09-04 | | Release date: | 2024-01-03 | | Last modified: | 2024-04-10 | | Method: | ELECTRON MICROSCOPY (2.89 Å) | | Cite: | Structure of GPR101-Gs enables identification of ligands with rejuvenating potential.
Nat.Chem.Biol., 20, 2024
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7VUZ
 | | Cryo-EM structure of pseudoallergen receptor MRGPRX2 complex with PAMP-12, state2 | | Descriptor: | CHOLESTEROL, 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: | Li, Y, Yang, F. | | Deposit date: | 2021-11-04 | | Release date: | 2021-12-01 | | Last modified: | 2022-07-20 | | Method: | ELECTRON MICROSCOPY (2.89 Å) | | Cite: | Structure, function and pharmacology of human itch receptor complexes.
Nature, 600, 2021
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7VIG
 | | Cryo-EM structure of Gi coupled Sphingosine 1-phosphate receptor bound with CBP-307 | | Descriptor: | 1-[[2-fluoranyl-4-[5-[4-(2-methylpropyl)phenyl]-1,2,4-oxadiazol-3-yl]phenyl]methyl]azetidine-3-carboxylic acid, 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: | Yu, L.Y, Gan, B, Xiao, Q.J, Ren, R.B. | | Deposit date: | 2021-09-26 | | Release date: | 2022-09-28 | | Last modified: | 2022-10-05 | | Method: | ELECTRON MICROSCOPY (2.89 Å) | | Cite: | Structural insights into sphingosine-1-phosphate receptor activation.
Proc.Natl.Acad.Sci.USA, 119, 2022
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7EO2
 | | Cryo-EM of Sphingosine 1-phosphate receptor 1 / Gi complex bound to FTY720p | | Descriptor: | (2~{S})-2-azanyl-4-(4-octylphenyl)-2-[[oxidanyl-bis(oxidanylidene)-$l^{6}-phosphanyl]oxymethyl]butan-1-ol, 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: | He, Y, Xu, Z, Ikuta, T. | | Deposit date: | 2021-04-21 | | Release date: | 2022-01-05 | | Last modified: | 2022-03-16 | | Method: | ELECTRON MICROSCOPY (2.89 Å) | | Cite: | Structural basis of sphingosine-1-phosphate receptor 1 activation and biased agonism.
Nat.Chem.Biol., 18, 2022
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8J18
 | | Cryo-EM structure of the 3-OH-C12-bound GPR84 receptor-Gi complex | | Descriptor: | (3R)-3-HYDROXYDODECANOIC ACID, Antibody fragment ScFv16, G-protein coupled receptor 84, ... | | Authors: | Liu, H, Yin, W, Xu, H.E. | | Deposit date: | 2023-04-12 | | Release date: | 2023-06-21 | | Last modified: | 2024-05-08 | | Method: | ELECTRON MICROSCOPY (2.89 Å) | | Cite: | Structural insights into ligand recognition and activation of the medium-chain fatty acid-sensing receptor GPR84.
Nat Commun, 14, 2023
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7YDM
 | | Cryo-EM structure of CD97/Gq complex | | Descriptor: | Adhesion G protein-coupled receptor E5 subunit beta, 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: | He, Y, Wang, N. | | Deposit date: | 2022-07-04 | | Release date: | 2023-07-12 | | Last modified: | 2023-11-29 | | Method: | ELECTRON MICROSCOPY (2.89 Å) | | Cite: | Structural basis of CD97 activation and G-protein coupling.
Cell Chem Biol, 30, 2023
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5WG3
 | | Human GRK2 in complex with Gbetagamma subunits and CCG258748 | | Descriptor: | 2-fluoro-5-[(3S,4R)-3-{[(1H-indazol-5-yl)oxy]methyl}piperidin-4-yl]-N-[(1H-pyrazol-3-yl)methyl]benzamide, 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: | 2017-07-13 | | Release date: | 2017-12-27 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.896 Å) | | Cite: | Structural Determinants Influencing the Potency and Selectivity of Indazole-Paroxetine Hybrid G Protein-Coupled Receptor Kinase 2 Inhibitors.
Mol. Pharmacol., 92, 2017
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8FU6
 | | GCGR-Gs complex in the presence of RAMP2 | | Descriptor: | Glucagon derivative ZP3780, Glucagon receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Krishna Kumar, K, O'Brien, E.S, Wang, H, Montabana, E, Kobilka, B.K. | | Deposit date: | 2023-01-16 | | Release date: | 2023-04-12 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Negative allosteric modulation of the glucagon receptor by RAMP2.
Cell, 186, 2023
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8WC8
 | | Cryo-EM structure of the ZH8651-bound hTAAR1-Gs complex | | Descriptor: | 2-(4-bromophenyl)ethanamine, 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: | Rong, N.K, Guo, L.L, Zhang, M.H, Li, Q, Yang, F, Sun, J.P. | | Deposit date: | 2023-09-11 | | Release date: | 2023-12-27 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Structural and signaling mechanisms of TAAR1 enabled preferential agonist design.
Cell, 186, 2023
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8JBH
 | | Substance P bound to active human neurokinin 3 receptor in complex with Gq | | 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 Gq subunit alpha (G324), ... | | Authors: | Sun, W.J, Yang, F, Zhang, H.H, Yuan, Q.N, Yin, W.C, Shi, P, Eric, X, Tian, C.L. | | Deposit date: | 2023-05-08 | | Release date: | 2024-02-07 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Structural insights into neurokinin 3 receptor activation by endogenous and analogue peptide agonists.
Cell Discov, 9, 2023
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7JVP
 | | Cryo-EM structure of SKF-83959-bound dopamine receptor 1 in complex with Gs protein | | Descriptor: | (1R)-6-chloro-3-methyl-1-(3-methylphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol, CHOLESTEROL, D(1A) dopamine receptor, ... | | Authors: | Zhuang, Y, Xu, P, Mao, C, Wang, L, Krumm, B, Zhou, X.E, Huang, S, Liu, H, Cheng, X, Huang, X.-P, Sheng, D.-D, Xu, T, Liu, Y.-F, Wang, Y, Guo, J, Jiang, Y, Jiang, H, Melcher, K, Roth, B.L, Zhang, Y, Zhang, C, Xu, H.E. | | Deposit date: | 2020-08-22 | | Release date: | 2021-02-24 | | Last modified: | 2021-03-03 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Structural insights into the human D1 and D2 dopamine receptor signaling complexes.
Cell, 184, 2021
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6KPF
 | | Cryo-EM structure of a class A GPCR with G protein complex | | Descriptor: | 7-[(6aR,9R,10aR)-1-Hydroxy-9-(hydroxymethyl)-6,6-dimethyl-6a,7,8,9,10,10a-hexahydro-6H-benzo[c]chromen-3-yl]- 7-methyloctanenitrile, Cannabinoid receptor 2, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Li, X.T, Hua, T, Wu, L.J, Makriyannis, A, Shen, L, Wang, Y.X, Liu, Z.J. | | Deposit date: | 2019-08-15 | | Release date: | 2020-02-12 | | Last modified: | 2022-04-27 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Activation and Signaling Mechanism Revealed by Cannabinoid Receptor-GiComplex Structures.
Cell, 180, 2020
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8XOG
 | | Cryo-EM structure of apo-GPR30-Gq complex structure | | Descriptor: | G-protein coupled estrogen receptor 1, 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: | Liu, H, Xu, P, Xu, H.E. | | Deposit date: | 2024-01-01 | | Release date: | 2024-04-10 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Cryo-EM structure of apo-GPR30-Gq complex structure
To Be Published
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7CX4
 | | Cryo-EM structure of the Evatanepag-bound EP2-Gs complex | | Descriptor: | 2-[3-[[(4-~{tert}-butylphenyl)methyl-pyridin-3-ylsulfonyl-amino]methyl]phenoxy]ethanoic acid, 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: | Qu, C, Mao, C, Xiao, P, Shen, Q, Zhong, Y, Yang, F, Shen, D, Tao, X, Zhang, H, Yan, X, Zhao, R, He, J, Guan, Y, Zhang, C, Hou, G, Zhang, P, Yu, X, Guan, Y, Sun, J, Zhang, Y. | | Deposit date: | 2020-09-01 | | Release date: | 2021-05-05 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Ligand recognition, unconventional activation, and G protein coupling of the prostaglandin E 2 receptor EP2 subtype.
Sci Adv, 7, 2021
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3KRW
 | | Human GRK2 in complex with Gbetgamma subunits and balanol (soak) | | Descriptor: | BALANOL, Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Tesmer, J.J.G, Tesmer, V.M. | | Deposit date: | 2009-11-19 | | Release date: | 2010-02-16 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.9 Å) | | Cite: | Structure of human g protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.
J.Med.Chem., 53, 2010
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8GW8
 | | the human PTH1 receptor bound to an intracellular biased agonist | | 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, Isoform Gnas-2 of Guanine nucleotide-binding protein G(s) subunit alpha isoforms short, ... | | Authors: | Kobayashi, K, Kusakizako, T, Okamoto, H.H, Nureki, O. | | Deposit date: | 2022-09-16 | | Release date: | 2023-06-14 | | Last modified: | 2023-09-27 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Class B1 GPCR activation by an intracellular agonist.
Nature, 618, 2023
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7D77
 | | Cryo-EM structure of the cortisol-bound adhesion receptor GPR97-Go complex | | Descriptor: | (11alpha,14beta)-11,17,21-trihydroxypregn-4-ene-3,20-dione, Adhesion G protein-coupled receptor G3; GPR97, CHOLESTEROL, ... | | Authors: | Ping, Y, Mao, C, Xiao, P, Zhao, R, Jiang, Y, Yang, Z, An, W, Shen, D, Yang, F, Zhang, H, Qu, C, Shen, Q, Tian, C, Li, Z, Li, S, Wang, G, Tao, X, Wen, X, Zhong, Y, Yang, J, Yi, F, Yu, X, Xu, E, Zhang, Y, Sun, J. | | Deposit date: | 2020-10-03 | | Release date: | 2021-02-03 | | Last modified: | 2021-02-10 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Structures of the glucocorticoid-bound adhesion receptor GPR97-G o complex.
Nature, 589, 2021
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7D3S
 | | Human SECR in complex with an engineered Gs heterotrimer | | 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, ... | | Authors: | Fukuhara, S, Kobayashi, K, Kusakizako, T, Shihoya, W, Nureki, O. | | Deposit date: | 2020-09-20 | | Release date: | 2020-11-04 | | Last modified: | 2020-12-30 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Structure of the human secretin receptor coupled to an engineered heterotrimeric G protein.
Biochem.Biophys.Res.Commun., 533, 2020
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8GG0
 | | CryoEM structure of beta-2-adrenergic receptor in complex with GTP-bound Gs heterotrimer (transition intermediate #6 of 20) | | Descriptor: | (5R,6R)-6-(methylamino)-5,6,7,8-tetrahydronaphthalene-1,2,5-triol, Beta-2 adrenergic receptor, GUANOSINE-5'-TRIPHOSPHATE, ... | | Authors: | Papasergi-Scott, M.M, Skiniotis, G. | | Deposit date: | 2023-03-08 | | Release date: | 2024-03-06 | | Last modified: | 2024-03-27 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Time-resolved cryo-EM of G-protein activation by a GPCR.
Nature, 2024
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7RGP
 | | cryo-EM of human Glucagon-like peptide 1 receptor GLP-1R bound to tirzepatide | | Descriptor: | Glucagon-like peptide 1 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: | Sun, B, Kobilka, B.K, Sloop, K.W, Feng, D, Kobilka, T.S. | | Deposit date: | 2021-07-15 | | Release date: | 2022-04-13 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Structural determinants of dual incretin receptor agonism by tirzepatide.
Proc.Natl.Acad.Sci.USA, 119, 2022
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7VDH
 | | Cryo-EM structure of pseudoallergen receptor MRGPRX2 complex with C48/80, state2 | | Descriptor: | 2-[4-methoxy-3-[[2-methoxy-3-[[2-methoxy-5-[2-(methylamino)ethyl]phenyl]methyl]-5-[2-(methylamino)ethyl]phenyl]methyl]phenyl]-~{N}-methyl-ethanamine, CHOLESTEROL, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Li, Y, Yang, F. | | Deposit date: | 2021-09-07 | | Release date: | 2021-12-01 | | Last modified: | 2022-07-20 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Structure, function and pharmacology of human itch receptor complexes.
Nature, 600, 2021
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7LCI
 | | PF 06882961 bound to the glucagon-like peptide-1 receptor (GLP-1R):Gs complex | | Descriptor: | 2-[(4-{6-[(4-cyano-2-fluorophenyl)methoxy]pyridin-2-yl}piperidin-1-yl)methyl]-1-{[(2S)-oxetan-2-yl]methyl}-1H-benzimidazole-6-carboxylic acid, Glucagon-like peptide 1 receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Belousoff, M.J, Johnson, R.M, Drulyte, I, Yu, L, Kotecha, A, Danev, R, Wootten, D, Zhang, X, Sexton, P.M. | | Deposit date: | 2021-01-11 | | Release date: | 2021-01-20 | | Last modified: | 2021-09-15 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Evolving cryo-EM structural approaches for GPCR drug discovery.
Structure, 29, 2021
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