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: | 2020-12-09 | | 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
|
|
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: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Crystal structure of the {mu}-opioid receptor bound to a morphinan antagonist.
Nature, 485, 2012
|
|
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: | 2023-08-30 | | 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
|
|
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: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (3.4 Å) | | Cite: | Crystal structure of the human beta2 adrenergic G-protein-coupled receptor.
Nature, 450, 2007
|
|
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: | 2021-10-13 | | Method: | X-RAY DIFFRACTION (3.4 Å) | | Cite: | Ligand-specific regulation of the extracellular surface of a G-protein-coupled receptor.
Nature, 463, 2010
|
|
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: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (3.5 Å) | | Cite: | Structure of a nanobody-stabilized active state of the b2 adrenoceptor
Nature, 469, 2011
|
|
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: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (3.4 Å) | | Cite: | Crystal structure of the human beta2 adrenergic G-protein-coupled receptor.
Nature, 450, 2007
|
|
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: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (3.2 Å) | | Cite: | Crystal structure of the beta2 adrenergic receptor-Gs protein complex
Nature, 477, 2011
|
|
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: | 2023-10-18 | | 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
|
|
6N51
 | | Metabotropic Glutamate Receptor 5 bound to L-quisqualate and Nb43 | | Descriptor: | (S)-2-AMINO-3-(3,5-DIOXO-[1,2,4]OXADIAZOLIDIN-2-YL)-PROPIONIC ACID, 2-acetamido-2-deoxy-beta-D-glucopyranose, Metabotropic glutamate receptor 5, ... | | Authors: | Koehl, A, Hu, H, Feng, D, Sun, B, Weis, W.I, Skiniotis, G.S, Mathiesen, J.M, Kobilka, B.K. | | Deposit date: | 2018-11-20 | | Release date: | 2019-01-23 | | Last modified: | 2020-07-29 | | Method: | ELECTRON MICROSCOPY (4 Å) | | Cite: | Structural insights into the activation of metabotropic glutamate receptors.
Nature, 566, 2019
|
|
6N52
 | | Metabotropic Glutamate Receptor 5 Apo Form | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Metabotropic glutamate receptor 5 | | Authors: | Koehl, A, Hu, H, Feng, D, Sun, B, Weis, W.I, Skiniotis, G.S, Mathiesen, J.M, Kobilka, B.K. | | Deposit date: | 2018-11-20 | | Release date: | 2019-01-23 | | Last modified: | 2020-07-29 | | Method: | ELECTRON MICROSCOPY (4 Å) | | Cite: | Structural insights into the activation of metabotropic glutamate receptors.
Nature, 566, 2019
|
|
6OBA
 | | The beta2 adrenergic receptor bound to a negative allosteric modulator | | Descriptor: | (2S)-1-[(1-methylethyl)amino]-3-(2-prop-2-en-1-ylphenoxy)propan-2-ol, 6-bromo-N~2~-phenylquinazoline-2,4-diamine, Beta-2 adrenergic receptor,Lysozyme,Beta-2 adrenergic receptor, ... | | Authors: | Liu, X, Stobel, A, Kaindl, J, Dengler, D, ClarK, M, Mahoney, J, Korczynska, M, Matt, R.A, Hubner, H, Xu, X, Stanek, M, Hirata, K, Shoichet, B, Sunahara, R, Gmeiner, R, Kobilka, B.K. | | Deposit date: | 2019-03-20 | | Release date: | 2020-03-25 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (3.1 Å) | | Cite: | An allosteric modulator binds to a conformational hub in the beta2adrenergic receptor.
Nat.Chem.Biol., 16, 2020
|
|
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: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (3.4 Å) | | Cite: | Structure of the delta opioid receptor bound to naltrindole
Nature, 485, 2012
|
|
3PDS
 | | Irreversible Agonist-Beta2 Adrenoceptor Complex | | Descriptor: | 8-hydroxy-5-[(1R)-1-hydroxy-2-({2-[3-methoxy-4-(3-sulfanylpropoxy)phenyl]ethyl}amino)ethyl]quinolin-2(1H)-one, CHOLESTEROL, Fusion protein Beta-2 adrenergic receptor/Lysozyme, ... | | Authors: | Rosenbaum, D.M, Zhang, C, Lyons, J.A, Holl, R, Aragao, D, Arlow, D.H, Rasmussen, S.G.F, Choi, H.-J, DeVree, B.T, Sunahara, R.K, Chae, P.S, Gellman, S.H, Dror, R.O, Shaw, D.E, Weis, W.I, Caffrey, M, Gmeiner, P, Kobilka, B.K. | | Deposit date: | 2010-10-24 | | Release date: | 2011-01-12 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (3.5 Å) | | Cite: | Structure and function of an irreversible agonist-beta(2) adrenoceptor complex
Nature, 469, 2011
|
|
6N4X
 | | Metabotropic Glutamate Receptor 5 Apo Form Ligand Binding Domain | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, MAGNESIUM ION, Metabotropic glutamate receptor 5 | | Authors: | Koehl, A, Hu, H, Feng, D, Sun, B, Weis, W.I, Skiniotis, G.S, Mathiesen, J.M, Kobilka, B.K. | | Deposit date: | 2018-11-20 | | Release date: | 2019-01-23 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (4 Å) | | Cite: | Structural insights into the activation of metabotropic glutamate receptors.
Nature, 566, 2019
|
|
6N50
 | | Metabotropic Glutamate Receptor 5 Extracellular Domain in Complex with Nb43 and L-quisqualic acid | | Descriptor: | (S)-2-AMINO-3-(3,5-DIOXO-[1,2,4]OXADIAZOLIDIN-2-YL)-PROPIONIC ACID, 2-acetamido-2-deoxy-beta-D-glucopyranose, Metabotropic glutamate receptor 5, ... | | Authors: | Koehl, A, Hu, H, Feng, D, Sun, B, Chu, M, Weis, W.I, Skiniotis, G, Mathiesen, J.M, Kobilka, B.K. | | Deposit date: | 2018-11-20 | | Release date: | 2019-01-23 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (3.751 Å) | | Cite: | Structural insights into the activation of metabotropic glutamate receptors.
Nature, 566, 2019
|
|
6N4Y
 | | Metabotropic Glutamate Receptor 5 Extracellular Domain with Nb43 | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-[alpha-L-fucopyranose-(1-6)]2-acetamido-2-deoxy-beta-D-glucopyranose, Metabotropic glutamate receptor 5, ... | | Authors: | Koehl, A, Hu, H, Feng, D, Sun, B, Chu, M, Weis, W.I, Mathiesen, J.M, Skiniotis, G, Kobilka, B.K. | | Deposit date: | 2018-11-20 | | Release date: | 2019-01-23 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (3.262 Å) | | Cite: | Structural insights into the activation of metabotropic glutamate receptors.
Nature, 566, 2019
|
|
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: | 2023-09-27 | | 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
|
|
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
|
|
3UON
 | | Structure of the human M2 muscarinic acetylcholine receptor bound to an antagonist | | Descriptor: | (3R)-1-azabicyclo[2.2.2]oct-3-yl hydroxy(diphenyl)acetate, CHLORIDE ION, Human M2 muscarinic acetylcholine, ... | | Authors: | Haga, K, Kruse, A.C, Asada, H, Yurugi-Kobayashi, T, Shiroishi, M, Zhang, C, Weis, W.I, Okada, T, Kobilka, B.K, Haga, T, Kobayashi, T. | | Deposit date: | 2011-11-16 | | Release date: | 2012-02-01 | | Last modified: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Structure of the human M2 muscarinic acetylcholine receptor bound to an antagonist.
Nature, 482, 2012
|
|
3VW7
 | | Crystal structure of human protease-activated receptor 1 (PAR1) bound with antagonist vorapaxar at 2.2 angstrom | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, CHLORIDE ION, Proteinase-activated receptor 1, ... | | Authors: | Zhang, C, Srinivasan, Y, Arlow, D.H, Fung, J.J, Palmer, D, Zheng, Y, Green, H.F, Pandey, A, Dror, R.O, Shaw, D.E, Weis, W.I, Coughlin, S.R, Kobilka, B.K. | | Deposit date: | 2012-08-07 | | Release date: | 2012-12-12 | | Last modified: | 2023-11-08 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | High-resolution crystal structure of human protease-activated receptor 1
Nature, 492, 2012
|
|
6OSA
 | | human Neurotensin Receptor 1 (hNTSR1) - Gi1 Protein Complex in non-canonical conformation (NC state) | | 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(i) subunit alpha-1, ... | | Authors: | Kato, H.E, Zhang, Y, Kobilka, B.K, Skiniotis, G. | | Deposit date: | 2019-05-01 | | Release date: | 2019-07-10 | | Last modified: | 2019-12-18 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Conformational transitions of a neurotensin receptor 1-Gi1complex.
Nature, 572, 2019
|
|
6OS9
 | | human Neurotensin Receptor 1 (hNTSR1) - Gi1 Protein Complex in canonical conformation (C state) | | 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(i) subunit alpha-1, ... | | Authors: | Kato, H.E, Zhang, Y, Kobilka, B.K, Skiniotis, G. | | Deposit date: | 2019-05-01 | | Release date: | 2019-07-10 | | Last modified: | 2019-12-18 | | Method: | ELECTRON MICROSCOPY (3 Å) | | Cite: | Conformational transitions of a neurotensin receptor 1-Gi1complex.
Nature, 572, 2019
|
|
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
|
|
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
|
|
