7L1V
 
 | | Orexin Receptor 2 (OX2R) in Complex with G Protein and Small-Molecule Agonist Compound 1 | | Descriptor: | 4'-methoxy-N,N-dimethyl-3'-{[3-(2-{[2-(2H-1,2,3-triazol-2-yl)benzene-1-carbonyl]amino}ethyl)phenyl]sulfamoyl}[1,1'-biphenyl]-3-carboxamide, Engineered Guanine nucleotide-binding protein subunit alpha, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Hong, C, Byrne, N.J, Zamlynny, B, Tummala, S, Xiao, L, Shipman, J.M, Partridge, A.T, Minnick, C, Breslin, M.J, Rudd, M.T, Stachel, S.J, Rada, V.L, Kern, J.C, Armacost, K.A, Hollingsworth, S.A, O'Brien, J.A, Hall, D.L, McDonald, T.P, Strickland, C, Brooun, A, Soisson, S.M, Hollenstein, K. | | Deposit date: | 2020-12-15 | | Release date: | 2021-02-10 | | Last modified: | 2021-02-17 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Structures of active-state orexin receptor 2 rationalize peptide and small-molecule agonist recognition and receptor activation.
Nat Commun, 12, 2021
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6BQG
 | | Crystal structure of 5-HT2C in complex with ergotamine | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 5-hydroxytryptamine receptor 2C,Soluble cytochrome b562, Ergotamine | | Authors: | Peng, Y, McCorvy, J.D, Harpsoe, K, Lansu, K, Yuan, S, Popov, P, Qu, L, Pu, M, Che, T, Nikolajse, L.F, Huang, X.P, Wu, Y, Shen, L, Bjorn-Yoshimoto, W.E, Ding, K, Wacker, D, Han, G.W, Cheng, J, Katritch, V, Jensen, A.A, Hanson, M.A, Zhao, S, Gloriam, D.E, Roth, B.L, Stevens, R.C, Liu, Z. | | Deposit date: | 2017-11-27 | | Release date: | 2018-02-14 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | 5-HT2C Receptor Structures Reveal the Structural Basis of GPCR Polypharmacology.
Cell, 172, 2018
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7LJC
 | | Allosteric modulator LY3154207 binding to SKF-81297-bound dopamine receptor 1 in complex with miniGs protein | | Descriptor: | (1R)-6-chloro-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol, 2-[2,6-bis(chloranyl)phenyl]-1-[(1S,3R)-3-(hydroxymethyl)-1-methyl-5-(3-methyl-3-oxidanyl-butyl)-3,4-dihydro-1H-isoquinolin-2-yl]ethanone, CHOLESTEROL, ... | | Authors: | Zhuang, Y, Krumm, B, Zhang, H, Zhou, X.E, Wang, Y, Guo, J, Huang, X.-P, Liu, Y, Wang, L, Cheng, X, Jiang, Y, Jiang, H, Melcher, K, Zhang, C, Yi, W, Roth, B.L, Zhang, Y, Xu, H.E. | | Deposit date: | 2021-01-28 | | Release date: | 2021-03-03 | | Last modified: | 2021-05-12 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Mechanism of dopamine binding and allosteric modulation of the human D1 dopamine receptor.
Cell Res., 31, 2021
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6C1R
 | | Crystal structure of human C5a receptor in complex with an orthosteric antagonist PMX53 and an allosteric antagonist avacopan | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, MALONATE ION, OLEIC ACID, ... | | Authors: | Liu, H, Wang, L, Wei, Z, Zhang, C. | | Deposit date: | 2018-01-05 | | Release date: | 2018-05-30 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Orthosteric and allosteric action of the C5a receptor antagonists.
Nat. Struct. Mol. Biol., 25, 2018
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7LJD
 | | Allosteric modulator LY3154207 binding to dopamine-bound dopamine receptor 1 in complex with miniGs protein | | Descriptor: | 2-[2,6-bis(chloranyl)phenyl]-1-[(1S,3R)-3-(hydroxymethyl)-1-methyl-5-(3-methyl-3-oxidanyl-butyl)-3,4-dihydro-1H-isoquinolin-2-yl]ethanone, CHOLESTEROL, D(1A) dopamine receptor, ... | | Authors: | Zhuang, Y, Krumm, B, Zhang, H, Zhou, X.E, Wang, Y, Guo, J, Huang, X.-P, Liu, Y, Wang, L, Cheng, X, Jiang, Y, Jiang, H, Melcher, K, Zhang, C, Yi, W, Roth, B.L, Zhang, Y, Xu, H.E. | | Deposit date: | 2021-01-28 | | Release date: | 2021-03-03 | | Last modified: | 2021-05-12 | | Method: | ELECTRON MICROSCOPY (3.2 Å) | | Cite: | Mechanism of dopamine binding and allosteric modulation of the human D1 dopamine receptor.
Cell Res., 31, 2021
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6BQH
 | | Crystal structure of 5-HT2C in complex with ritanserin | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 5-hydroxytryptamine receptor 2C,Soluble cytochrome b562, 6-(2-{4-[bis(4-fluorophenyl)methylidene]piperidin-1-yl}ethyl)-7-methyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one, ... | | Authors: | Peng, Y, McCorvy, J.D, Harpsoe, K, Lansu, K, Yuan, S, Popov, P, Qu, L, Pu, M, Che, T, Nikolajse, L.F, Huang, X.P, Wu, Y, Shen, L, Bjorn-Yoshimoto, W.E, Ding, K, Wacker, D, Han, G.W, Cheng, J, Katritch, V, Jensen, A.A, Hanson, M.A, Zhao, S, Gloriam, D.E, Roth, B.L, Stevens, R.C, Liu, Z. | | Deposit date: | 2017-11-27 | | Release date: | 2018-02-14 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | 5-HT2C Receptor Structures Reveal the Structural Basis of GPCR Polypharmacology.
Cell, 172, 2018
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6C1Q
 | | Crystal structure of human C5a receptor in complex with an orthosteric antagonist PMX53 and an allosteric antagonist NDT9513727 | | Descriptor: | 1-(1,3-benzodioxol-5-yl)-~{N}-(1,3-benzodioxol-5-ylmethyl)-~{N}-[(3-butyl-2,5-diphenyl-imidazol-4-yl)methyl]methanamine, PMX53, Soluble cytochrome b562, ... | | Authors: | Liu, H, Wang, L, Wei, Z, Zhang, C. | | Deposit date: | 2018-01-05 | | Release date: | 2018-05-30 | | Last modified: | 2020-01-08 | | Method: | X-RAY DIFFRACTION (2.9 Å) | | Cite: | Orthosteric and allosteric action of the C5a receptor antagonists.
Nat. Struct. Mol. Biol., 25, 2018
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7LD3
 | | Cryo-EM structure of the human adenosine A1 receptor-Gi2-protein complex bound to its endogenous agonist and an allosteric ligand | | Descriptor: | ADENOSINE, Chimera protein of Muscarinic acetylcholine receptor M4 and Adenosine receptor A1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Draper-Joyce, C.J, Danev, R, Thal, D.M, Christopoulos, A, Glukhova, A. | | Deposit date: | 2021-01-12 | | Release date: | 2021-09-08 | | Last modified: | 2021-10-13 | | Method: | ELECTRON MICROSCOPY (3.2 Å) | | Cite: | Positive allosteric mechanisms of adenosine A 1 receptor-mediated analgesia.
Nature, 597, 2021
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7LD4
 | | Cryo-EM structure of the human adenosine A1 receptor-Gi2-protein complex bound to its endogenous agonist | | Descriptor: | ADENOSINE, Chimera protein of Muscarinic acetylcholine receptor M4 and Adenosine receptor A1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Draper-Joyce, C.J, Danev, R, Thal, D.M, Christopoulos, A, Glukhova, A. | | Deposit date: | 2021-01-12 | | Release date: | 2021-09-08 | | Last modified: | 2021-10-13 | | Method: | ELECTRON MICROSCOPY (3.3 Å) | | Cite: | Positive allosteric mechanisms of adenosine A 1 receptor-mediated analgesia.
Nature, 597, 2021
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6CM4
 | | Structure of the D2 Dopamine Receptor Bound to the Atypical Antipsychotic Drug Risperidone | | Descriptor: | 3-[2-[4-(6-fluoranyl-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one, D(2) dopamine receptor, endolysin chimera, ... | | Authors: | Wang, S, Che, T, Levit, A, Shoichet, B.K, Wacker, D, Roth, B.L. | | Deposit date: | 2018-03-02 | | Release date: | 2018-03-14 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.867 Å) | | Cite: | Structure of the D2 dopamine receptor bound to the atypical antipsychotic drug risperidone.
Nature, 555, 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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7ARO
 | | Crystal structure of the non-ribose partial agonist LUF5833 bound to the adenosine A2A receptor | | Descriptor: | 2-azanyl-6-(1~{H}-imidazol-2-ylmethylsulfanyl)-4-phenyl-pyridine-3,5-dicarbonitrile, Adenosine receptor A2a,Soluble cytochrome b562,Adenosine receptor A2a, CHOLESTEROL, ... | | Authors: | Verdon, G, Amelia, T, van Veldhoven, J, Falsini, M, Liu, R, Heitman, L, van Westen, G, Segala, E, Cheng, R, Cooke, R, van der Es, D, Ijzerman, A. | | Deposit date: | 2020-10-25 | | Release date: | 2021-04-07 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (3.119 Å) | | Cite: | Crystal Structure and Subsequent Ligand Design of a Nonriboside Partial Agonist Bound to the Adenosine A 2A Receptor.
J.Med.Chem., 64, 2021
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7AUE
 | | Melanocortin receptor 4 (MC4R) Gs protein complex | | Descriptor: | AMINOSERINE, CALCIUM ION, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Degtjarik, O, Israeli, H, Prabahar, V, Shalev-Benami, M. | | Deposit date: | 2020-11-02 | | Release date: | 2021-04-28 | | Last modified: | 2023-03-15 | | Method: | ELECTRON MICROSCOPY (2.97 Å) | | Cite: | Structure reveals the activation mechanism of the MC4 receptor to initiate satiation signaling.
Science, 372, 2021
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6D26
 | | Crystal structure of the prostaglandin D2 receptor CRTH2 with fevipiprant | | Descriptor: | OLEIC ACID, Prostaglandin D2 receptor 2, Endolysin chimera, ... | | Authors: | Wang, L, Yao, D, Deepak, K, Liu, H, Gong, W, Fan, H, Wei, Z, Zhang, C. | | Deposit date: | 2018-04-13 | | Release date: | 2018-10-03 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.798 Å) | | Cite: | Structures of the Human PGD2Receptor CRTH2 Reveal Novel Mechanisms for Ligand Recognition.
Mol. Cell, 72, 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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7MTB
 | | Rhodopsin kinase (GRK1)-S5E/S488E/T489E in complex with rhodopsin and Fab6 | | Descriptor: | Fab6 heavy chain, Fab6 light chain, RETINAL, ... | | Authors: | Chen, Q, Chen, C.-L, Tesmer, J.J.G. | | Deposit date: | 2021-05-13 | | Release date: | 2021-07-07 | | Last modified: | 2021-08-25 | | Method: | ELECTRON MICROSCOPY (4 Å) | | Cite: | Structures of rhodopsin in complex with G-protein-coupled receptor kinase 1.
Nature, 595, 2021
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7MT8
 | | Rhodopsin kinase (GRK1)-S5E/S488E/T489E in complex with rhodopsin | | Descriptor: | RETINAL, Rhodopsin, Rhodopsin kinase GRK1, ... | | Authors: | Chen, Q, Chen, C.-L, Tesmer, J.J.G. | | Deposit date: | 2021-05-13 | | Release date: | 2021-07-07 | | Last modified: | 2021-08-25 | | Method: | ELECTRON MICROSCOPY (5.8 Å) | | Cite: | Structures of rhodopsin in complex with G-protein-coupled receptor kinase 1.
Nature, 595, 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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7BU7
 | | Structure of human beta1 adrenergic receptor bound to BI-167107 and nanobody 6B9 | | Descriptor: | (2S)-2,3-dihydroxypropyl (7Z)-tetradec-7-enoate, 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, 8-[(1R)-2-{[1,1-dimethyl-2-(2-methylphenyl)ethyl]amino}-1-hydroxyethyl]-5-hydroxy-2H-1,4-benzoxazin-3(4H)-one, ... | | Authors: | Xu, X, Kaindl, J, Clark, M, Hubner, H, Hirata, K, Sunahara, R, Gmeiner, P, Kobilka, B.K, Liu, X. | | Deposit date: | 2020-04-04 | | Release date: | 2020-12-02 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Binding pathway determines norepinephrine selectivity for the human beta 1 AR over beta 2 AR.
Cell Res., 31, 2021
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7MTA
 | | Rhodopsin kinase (GRK1)-S5E/S488E/T489E in complex with rhodopsin and Fab1 | | Descriptor: | Fab1 Heavy chain, Fab1 Light chain, RETINAL, ... | | Authors: | Chen, Q, Chen, C.-L, Tesmer, J.J.G. | | Deposit date: | 2021-05-13 | | Release date: | 2021-07-07 | | Last modified: | 2021-08-25 | | Method: | ELECTRON MICROSCOPY (4.1 Å) | | Cite: | Structures of rhodopsin in complex with G-protein-coupled receptor kinase 1.
Nature, 595, 2021
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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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7MT9
 | | Rhodopsin kinase (GRK1) in complex with rhodopsin | | Descriptor: | RETINAL, Rhodopsin, Rhodopsin kinase GRK1, ... | | Authors: | Chen, Q, Chen, C.-L, Tesmer, J.J.G. | | Deposit date: | 2021-05-13 | | Release date: | 2021-07-07 | | Last modified: | 2021-08-25 | | Method: | ELECTRON MICROSCOPY (7 Å) | | Cite: | Structures of rhodopsin in complex with G-protein-coupled receptor kinase 1.
Nature, 595, 2021
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6D27
 | | Crystal structure of the prostaglandin D2 receptor CRTH2 with CAY10471 | | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, DI(HYDROXYETHYL)ETHER, OLEIC ACID, ... | | Authors: | Wang, L, Yao, D, Deepak, K, Liu, H, Gong, W, Fan, H, Wei, Z, Zhang, C. | | Deposit date: | 2018-04-13 | | Release date: | 2018-10-03 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.738 Å) | | Cite: | Structures of the Human PGD2Receptor CRTH2 Reveal Novel Mechanisms for Ligand Recognition.
Mol. Cell, 72, 2018
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7BVQ
 | | Structure of human beta1 adrenergic receptor bound to carazolol | | Descriptor: | (2S)-1-(9H-Carbazol-4-yloxy)-3-(isopropylamino)propan-2-ol, (2S)-2,3-dihydroxypropyl (7Z)-tetradec-7-enoate, CHOLESTEROL, ... | | Authors: | Xu, X, Kaindl, J, Clark, M, Hubner, H, Hirata, K, Sunahara, R, Gmeiner, P, Kobilka, B.K, Liu, X. | | Deposit date: | 2020-04-11 | | Release date: | 2020-12-02 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Binding pathway determines norepinephrine selectivity for the human beta 1 AR over beta 2 AR.
Cell Res., 31, 2021
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