3KJ6
 
 | | Crystal structure of a Methylated beta2 Adrenergic Receptor-Fab complex | | Descriptor: | Beta-2 adrenergic receptor, Fab heavy chain, Fab light chain, ... | | Authors: | Bokoch, M.P, Zou, Y, Rasmussen, S.G.F, Liu, C.W, Nygaard, R, Rosenbaum, D.M, Fung, J.J, Choi, H.-J, Thian, F.S, Kobilka, T.S, Puglisi, J.D, Weis, W.I, Pardo, L, Prosser, S, Mueller, L, Kobilka, B.K. | | Deposit date: | 2009-11-02 | | Release date: | 2010-02-16 | | Last modified: | 2024-11-06 | | Method: | X-RAY DIFFRACTION (3.4 Å) | | Cite: | Ligand-specific regulation of the extracellular surface of a G-protein-coupled receptor.
Nature, 463, 2010
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6XOX
 | | cryo-EM of human GLP-1R bound to non-peptide agonist LY3502970 | | Descriptor: | 3-[(1S,2S)-1-(5-[(4S)-2,2-dimethyloxan-4-yl]-2-{(4S)-2-(4-fluoro-3,5-dimethylphenyl)-3-[3-(4-fluoro-1-methyl-1H-indazol-5-yl)-2-oxo-2,3-dihydro-1H-imidazol-1-yl]-4-methyl-2,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-carbonyl}-1H-indol-1-yl)-2-methylcyclopropyl]-1,2,4-oxadiazol-5(4H)-one, Alpha subunit of Gs with N-terminus swapped with equivalent residues in Gi,Guanine nucleotide-binding protein G(s) subunit alpha isoforms XLas, Glucagon-like peptide 1 receptor, ... | | Authors: | Sun, B, Kobilka, B.K, Sloop, K.W, Feng, D, Kobilka, T.S. | | Deposit date: | 2020-07-07 | | Release date: | 2020-11-18 | | Last modified: | 2024-11-13 | | Method: | ELECTRON MICROSCOPY (3.1 Å) | | Cite: | Structural basis for GLP-1 receptor activation by LY3502970, an orally active nonpeptide agonist.
Proc.Natl.Acad.Sci.USA, 117, 2020
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4EJ4
 | | Structure of the delta opioid receptor bound to naltrindole | | Descriptor: | (4bS,8R,8aS,14bR)-7-(cyclopropylmethyl)-5,6,7,8,14,14b-hexahydro-4,8-methano[1]benzofuro[2,3-a]pyrido[4,3-b]carbazole-1,8a(9H)-diol, Delta-type opioid receptor, Lysozyme chimera | | Authors: | Granier, S, Manglik, A, Kruse, A.C, Kobilka, T.S, Thian, F.S, Weis, W.I, Kobilka, B.K. | | Deposit date: | 2012-04-06 | | Release date: | 2012-05-16 | | Last modified: | 2024-10-30 | | Method: | X-RAY DIFFRACTION (3.4 Å) | | Cite: | Structure of the delta opioid receptor bound to naltrindole
Nature, 485, 2012
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4DKL
 | | Crystal structure of the mu-opioid receptor bound to a morphinan antagonist | | Descriptor: | CHLORIDE ION, CHOLESTEROL, Mu-type opioid receptor, ... | | Authors: | Manglik, A, Kruse, A.C, Kobilka, T.S, Thian, F.S, Mathiesen, J.M, Sunahara, R.K, Pardo, L, Weis, W.I, Kobilka, B.K, Granier, S. | | Deposit date: | 2012-02-03 | | Release date: | 2012-03-21 | | Last modified: | 2024-11-27 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Crystal structure of the {mu}-opioid receptor bound to a morphinan antagonist.
Nature, 485, 2012
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7JOZ
 | | Crystal structure of dopamine D1 receptor in complex with G protein and a non-catechol agonist | | Descriptor: | 6-{4-[(furo[3,2-c]pyridin-4-yl)oxy]-2-methylphenyl}-1,5-dimethylpyrimidine-2,4(1H,3H)-dione, Endolysin,D(1A) dopamine receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Sun, B, Feng, D, Chu, M.L, Fish, I, Kelm, S, Lebon, F, Lovera, S, Valade, A, Wood, M, Ceska, T, Kobilka, T.S, Sands, Z, Kobilka, B.K. | | Deposit date: | 2020-08-07 | | Release date: | 2021-04-14 | | Last modified: | 2024-10-16 | | Method: | X-RAY DIFFRACTION (3.8 Å) | | Cite: | Crystal structure of dopamine D1 receptor in complex with G protein and a non-catechol agonist.
Nat Commun, 12, 2021
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3P0G
 | | Structure of a nanobody-stabilized active state of the beta2 adrenoceptor | | Descriptor: | 8-[(1R)-2-{[1,1-dimethyl-2-(2-methylphenyl)ethyl]amino}-1-hydroxyethyl]-5-hydroxy-2H-1,4-benzoxazin-3(4H)-one, Beta-2 adrenergic receptor, Lysozyme, ... | | Authors: | Rasmussen, S.G.F, Choi, H.-J, Fung, J.J, Pardon, E, Casarosa, P, Chae, P.S, DeVree, B.T, Rosenbaum, D.M, Thian, F.S, Kobilka, T.S, Schnapp, A, Konetzki, I, Sunahara, R.K, Gellman, S.H, Pautsch, A, Steyaert, J, Weis, W.I, Kobilka, B.K. | | Deposit date: | 2010-09-28 | | Release date: | 2011-01-19 | | Last modified: | 2024-10-30 | | Method: | X-RAY DIFFRACTION (3.5 Å) | | Cite: | Structure of a nanobody-stabilized active state of the b2 adrenoceptor
Nature, 469, 2011
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3SN6
 | | Crystal structure of the beta2 adrenergic receptor-Gs protein complex | | Descriptor: | 8-[(1R)-2-{[1,1-dimethyl-2-(2-methylphenyl)ethyl]amino}-1-hydroxyethyl]-5-hydroxy-2H-1,4-benzoxazin-3(4H)-one, Camelid antibody VHH fragment, Endolysin,Beta-2 adrenergic receptor, ... | | Authors: | Rasmussen, S.G.F, DeVree, B.T, Zou, Y, Kruse, A.C, Chung, K.Y, Kobilka, T.S, Thian, F.S, Chae, P.S, Pardon, E, Calinski, D, Mathiesen, J.M, Shah, S.T.A, Lyons, J.A, Caffrey, M, Gellman, S.H, Steyaert, J, Skiniotis, G, Weis, W.I, Sunahara, R.K, Kobilka, B.K. | | Deposit date: | 2011-06-28 | | Release date: | 2011-07-20 | | Last modified: | 2024-11-20 | | Method: | X-RAY DIFFRACTION (3.2 Å) | | Cite: | Crystal structure of the beta2 adrenergic receptor-Gs protein complex
Nature, 477, 2011
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5VAI
 | | Cryo-EM structure of the activated Glucagon-like peptide-1 receptor in complex with G protein | | Descriptor: | Glucagon-like peptide 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: | Zhang, Y, Sun, B, Feng, D, Hu, H, Chu, M, Qu, Q, Tarrasch, J.T, Li, S, Kobilka, T.S, Kobilka, B.K, Skiniotis, G. | | Deposit date: | 2017-03-27 | | Release date: | 2017-05-24 | | Last modified: | 2025-05-14 | | Method: | ELECTRON MICROSCOPY (4.1 Å) | | Cite: | Cryo-EM structure of the activated GLP-1 receptor in complex with a G protein.
Nature, 546, 2017
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2RH1
 | | High resolution crystal structure of human B2-adrenergic G protein-coupled receptor. | | Descriptor: | (2S)-1-(9H-Carbazol-4-yloxy)-3-(isopropylamino)propan-2-ol, 1,4-BUTANEDIOL, ACETAMIDE, ... | | Authors: | Cherezov, V, Rosenbaum, D.M, Hanson, M.A, Rasmussen, S.G.F, Thian, F.S, Kobilka, T.S, Choi, H.J, Kuhn, P, Weis, W.I, Kobilka, B.K, Stevens, R.C, Accelerated Technologies Center for Gene to 3D Structure (ATCG3D), GPCR Network (GPCR) | | Deposit date: | 2007-10-05 | | Release date: | 2007-10-30 | | Last modified: | 2024-10-30 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor.
Science, 318, 2007
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2R4R
 | | Crystal structure of the human beta2 adrenoceptor | | Descriptor: | Beta-2 adrenergic receptor, antibody for beta2 adrenoceptor, heavy chain, ... | | Authors: | Rasmussen, S.G.F, Choi, H.J, Rosenbaum, D.M, Kobilka, T.S, Thian, F.S, Edwards, P.C, Burghammer, M, Ratnala, V.R, Sanishvili, R, Fischetti, R.F, Schertler, G.F, Weis, W.I, Kobilka, B.K. | | Deposit date: | 2007-08-31 | | Release date: | 2007-11-06 | | Last modified: | 2024-11-06 | | Method: | X-RAY DIFFRACTION (3.4 Å) | | Cite: | Crystal structure of the human beta2 adrenergic G-protein-coupled receptor.
Nature, 450, 2007
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2R4S
 | | Crystal structure of the human beta2 adrenoceptor | | Descriptor: | Beta-2 adrenergic receptor, antibody for beta2 adrenoceptor, heavy chain, ... | | Authors: | Rasmussen, S.G.F, Choi, H.J, Rosenbaum, D.M, Kobilka, T.S, Thian, F.S, Edwards, P.C, Burghammer, M, Ratnala, V.R, Sanishvili, R, Fischetti, R.F, Schertler, G.F, Weis, W.I, Kobilka, B.K. | | Deposit date: | 2007-08-31 | | Release date: | 2007-11-06 | | Last modified: | 2024-10-16 | | Method: | X-RAY DIFFRACTION (3.4 Å) | | Cite: | Crystal structure of the human beta2 adrenergic G-protein-coupled receptor.
Nature, 450, 2007
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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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7RBT
 | | cryo-EM structure of human Gastric inhibitory polypeptide receptor GIPR bound to tirzepatide | | Descriptor: | 2-fluoro-4-[(1R)-6-methoxy-1-methyl-2-{(1S)-1-[4-(propan-2-yl)phenyl]ethyl}-1,2,3,4-tetrahydroisoquinolin-5-yl]-6-[(2-methylpropyl)amino]phenol, Gastric inhibitory polypeptide receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Sun, B, Kobilka, B.K, Sloop, K.W, Feng, D, Kobilka, T.S. | | Deposit date: | 2021-07-06 | | Release date: | 2022-04-13 | | Method: | ELECTRON MICROSCOPY (3.08 Å) | | Cite: | Structural determinants of dual incretin receptor agonism by tirzepatide.
Proc.Natl.Acad.Sci.USA, 119, 2022
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7RA3
 | | cryo-EM of human Gastric inhibitory polypeptide receptor GIPR bound to GIP | | Descriptor: | Gastric inhibitory polypeptide, Gastric inhibitory polypeptide receptor, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Sun, B, Kobilka, B.K, Sloop, K.W, Feng, D, Kobilka, T.S. | | Deposit date: | 2021-06-29 | | Release date: | 2022-04-13 | | Last modified: | 2024-10-30 | | Method: | ELECTRON MICROSCOPY (3.24 Å) | | Cite: | Structural determinants of dual incretin receptor agonism by tirzepatide.
Proc.Natl.Acad.Sci.USA, 119, 2022
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7RG9
 | | cryo-EM of human Glucagon-like peptide 1 receptor GLP-1R in apo form | | 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: | 2021-07-14 | | Release date: | 2022-04-13 | | Last modified: | 2024-10-23 | | Method: | ELECTRON MICROSCOPY (3.2 Å) | | Cite: | Structural determinants of dual incretin receptor agonism by tirzepatide.
Proc.Natl.Acad.Sci.USA, 119, 2022
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8GHV
 | | Cannabinoid Receptor 1-G Protein Complex | | Descriptor: | (5Z,8Z,11Z,13S,14Z)-N-[(2R)-1-hydroxypropan-2-yl]-13-methylicosa-5,8,11,14-tetraenamide, Cannabinoid receptor 1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Krishna Kumar, K, Robertson, M.J, Skiniotis, G, Kobilka, B.K. | | Deposit date: | 2023-03-12 | | Release date: | 2023-05-24 | | Last modified: | 2024-10-09 | | Method: | ELECTRON MICROSCOPY (2.8 Å) | | Cite: | Structural basis for activation of CB1 by an endocannabinoid analog.
Nat Commun, 14, 2023
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5X7D
 | | Structure of beta2 adrenoceptor bound to carazolol and an intracellular allosteric antagonist | | Descriptor: | (2S)-1-(9H-Carbazol-4-yloxy)-3-(isopropylamino)propan-2-ol, 1,4-BUTANEDIOL, 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, ... | | Authors: | Liu, X, Ahn, S, Kahsai, A.W, Meng, K.-C, Latorraca, N.R, Pani, B, Venkatakrishnan, A.J, Masoudi, A, Weis, W.I, Dror, R.O, Chen, X, Lefkowitz, R.J, Kobilka, B.K. | | Deposit date: | 2017-02-25 | | Release date: | 2017-08-16 | | Last modified: | 2024-11-06 | | Method: | X-RAY DIFFRACTION (2.703 Å) | | Cite: | Mechanism of intracellular allosteric beta 2AR antagonist revealed by X-ray crystal structure.
Nature, 548, 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 | | Last modified: | 2024-11-06 | | Method: | ELECTRON MICROSCOPY (2.9 Å) | | Cite: | Negative allosteric modulation of the glucagon receptor by RAMP2.
Cell, 186, 2023
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5CXV
 | | Structure of the human M1 muscarinic acetylcholine receptor bound to antagonist Tiotropium | | Descriptor: | (1R,2R,4S,5S,7S)-7-{[hydroxy(dithiophen-2-yl)acetyl]oxy}-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.0~2,4~]nonane, 1,2-ETHANEDIOL, CHOLESTEROL HEMISUCCINATE, ... | | Authors: | Sun, B, Feng, D, Li, X, Kobilka, T.S, Kobilka, B.K. | | Deposit date: | 2015-07-29 | | Release date: | 2016-03-09 | | Last modified: | 2024-11-20 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Crystal structures of the M1 and M4 muscarinic acetylcholine receptors.
Nature, 531, 2016
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5JQH
 | | Structure of beta2 adrenoceptor bound to carazolol and inactive-state stabilizing nanobody, Nb60 | | Descriptor: | (2S)-1-(9H-Carbazol-4-yloxy)-3-(isopropylamino)propan-2-ol, CHOLESTEROL, Endolysin,Beta-2 adrenergic receptor, ... | | Authors: | Staus, D.P, Strachan, R.T, Manglik, A, Pani, B, Kahsai, A.W, Kim, T.H, Wingler, L.M, Ahn, S, Chatterjee, A, Masoudi, A, Kruse, A.C, Pardon, E, Steyaert, J, Weis, W.I, Prosser, R.S, Kobilka, B.K, Costa, T, Lefkowitz, R.J. | | Deposit date: | 2016-05-05 | | Release date: | 2016-07-13 | | Last modified: | 2024-10-23 | | Method: | X-RAY DIFFRACTION (3.2 Å) | | Cite: | Allosteric nanobodies reveal the dynamic range and diverse mechanisms of G-protein-coupled receptor activation.
Nature, 535, 2016
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5C1M
 | | Crystal structure of active mu-opioid receptor bound to the agonist BU72 | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (2R,3S,3aR,5aR,6R,11bR,11cS)-3a-methoxy-3,14-dimethyl-2-phenyl-2,3,3a,6,7,11c-hexahydro-1H-6,11b-(epiminoethano)-3,5a-methanonaphtho[2,1-g]indol-10-ol, CHOLESTEROL, ... | | Authors: | Huang, W.J, Manglik, A, Venkatakrishnan, A.J, Laeremans, T, Feinberg, E.N, Sanborn, A.L, Kato, H.E, Livingston, K.E, Thorsen, T.S, Kling, R, Granier, S, Gmeiner, P, Husbands, S.M, Traynor, J.R, Weis, W.I, Steyaert, J, Dror, R.O, Kobilka, B.K. | | Deposit date: | 2015-06-15 | | Release date: | 2015-08-05 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (2.07 Å) | | Cite: | Structural insights into mu-opioid receptor activation.
Nature, 524, 2015
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6UP7
 | | neurotensin receptor and arrestin2 complex | | Descriptor: | ARG-ARG-PRO-TYR-ILE-LEU, Beta-arrestin-1, Neurotensin receptor type 1, ... | | Authors: | Qu, Q.H, Huang, W, Masureel, M, Janetzko, J, Kobilka, B.K, Skiniotis, G. | | Deposit date: | 2019-10-16 | | Release date: | 2020-02-26 | | Last modified: | 2024-11-06 | | Method: | ELECTRON MICROSCOPY (4.2 Å) | | Cite: | Structure of the neurotensin receptor 1 in complex with beta-arrestin 1.
Nature, 579, 2020
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4MQS
 | | Structure of active human M2 muscarinic acetylcholine receptor bound to the agonist iperoxo | | Descriptor: | 4-(4,5-dihydro-1,2-oxazol-3-yloxy)-N,N,N-trimethylbut-2-yn-1-aminium, Muscarinic acetylcholine receptor M2, Nanobody 9-8 | | Authors: | Kruse, A.C, Ring, A.M, Manglik, A, Hu, J, Hu, K, Eitel, K, Huebner, H, Pardon, E, Valant, C, Sexton, P.M, Christopoulos, A, Felder, C.C, Gmeiner, P, Steyaert, J, Weis, W.I, Garcia, K.C, Wess, J, Kobilka, B.K. | | Deposit date: | 2013-09-16 | | Release date: | 2013-11-27 | | Last modified: | 2024-10-09 | | Method: | X-RAY DIFFRACTION (3.5 Å) | | Cite: | Activation and allosteric modulation of a muscarinic acetylcholine receptor.
Nature, 504, 2013
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4MQT
 | | Structure of active human M2 muscarinic acetylcholine receptor bound to the agonist iperoxo and allosteric modulator LY2119620 | | Descriptor: | 3-amino-5-chloro-N-cyclopropyl-4-methyl-6-[2-(4-methylpiperazin-1-yl)-2-oxoethoxy]thieno[2,3-b]pyridine-2-carboxamide, 4-(4,5-dihydro-1,2-oxazol-3-yloxy)-N,N,N-trimethylbut-2-yn-1-aminium, Muscarinic acetylcholine receptor M2, ... | | Authors: | Kruse, A.C, Ring, A.M, Manglik, A, Hu, J, Hu, K, Eitel, K, Huebner, H, Pardon, E, Valant, C, Sexton, P.M, Christopoulos, A, Felder, C.C, Gmeiner, P, Steyaert, J, Weis, W.I, Garcia, K.C, Wess, J, Kobilka, B.K. | | Deposit date: | 2013-09-16 | | Release date: | 2013-11-27 | | Last modified: | 2024-11-06 | | Method: | X-RAY DIFFRACTION (3.7 Å) | | Cite: | Activation and allosteric modulation of a muscarinic acetylcholine receptor.
Nature, 504, 2013
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4GBR
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