3VG9 | | CRYSTAL STRUCTURE OF HUMAN ADENOSINE A2A RECEPTOR WITH AN ALLOSTERIC INVERSE-AGONIST ANTIBODY AT 2.7 A RESOLUTION | | Descriptor: | Adenosine receptor A2a, antibody fab fragment light chain, antibody fab fragment heavy chain, ... | | Authors: | Hino, T., Arakawa, T., Iwanari, H., Yurugi-Kobayashi, T., Ikeda-Suno, C., Nakada-Nakura, Y., Kusano-Arai, O., Weyand, S., Shimamura, T., Nomura, N., Cameron, A.D., Kobayashi, T., Hamakubo, T., Iwata, S., Murata, T. | | Deposit date: | 2011-08-04 | | Release date: | 2012-02-01 | | Last modified: | 2012-02-15 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | G-protein-coupled receptor inactivation by an allosteric inverse-agonist antibody
Nature, 482, 2012
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3VGA | | CRYSTAL STRUCTURE OF HUMAN ADENOSINE A2A RECEPTOR WITH AN ALLOSTERIC INVERSE-AGONIST ANTIBODY AT 3.1 A RESOLUTION | | Descriptor: | Adenosine receptor A2a, antibody fab fragment light chain, antibody fab fragment heavy chain, ... | | Authors: | Hino, T., Arakawa, T., Iwanari, H., Yurugi-Kobayashi, T., Ikeda-Suno, C., Nakada-Nakura, Y., Kusano-Arai, O., Weyand, S., Shimamura, T., Nomura, N., Cameron, A.D., Kobayashi, T., Hamakubo, T., Iwata, S., Murata, T. | | Deposit date: | 2011-08-04 | | Release date: | 2012-02-01 | | Last modified: | 2012-02-15 | | Method: | X-RAY DIFFRACTION (3.1 Å) | | Cite: | G-protein-coupled receptor inactivation by an allosteric inverse-agonist antibody
Nature, 482, 2012
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3ZEV | | STRUCTURE OF THERMOSTABLE AGONIST-BOUND NEUROTENSIN RECEPTOR 1 MUTANT WITHOUT LYSOZYME FUSION | | Descriptor: | NEUROTENSIN RECEPTOR 1 TM86V, NEUROTENSIN, GLYCINE | | Authors: | Egloff, P., Hillenbrand, M., Schlinkmann, K.M., Batyuk, A., Mittl, P., Plueckthun, A. | | Deposit date: | 2012-12-07 | | Release date: | 2014-01-29 | | Last modified: | 2014-02-26 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Structure of Signaling-Competent Neurotensin Receptor 1 Obtained by Directed Evolution in Escherichia Coli
Proc.Natl.Acad.Sci.USA, 111, 2014
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3ZPQ | | THERMOSTABILISED TURKEY BETA1 ADRENERGIC RECEPTOR WITH 4-(PIPERAZIN-1- YL)-1H-INDOLE BOUND (COMPOUND 19) | | Descriptor: | BETA-1 ADRENERGIC RECEPTOR, CHOLESTEROL HEMISUCCINATE, HEGA-10, ... | | Authors: | Christopher, J.A., Congreve, M., Dore, A.S., Marshall, F.H., Myszka, D.G., Brown, J., Koglin, M., Tehan, B., Errey, J.C., Tate, C.G., Warne, T. | | Deposit date: | 2013-03-01 | | Release date: | 2013-04-03 | | Last modified: | 2019-05-15 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Biophysical Fragment Screening of the Beta1-Adrenergic Receptor: Identification of High Affinity Aryl Piperazine Leads Using Structure-Based Drug Design.
J.Med.Chem., 56, 2013
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3ZPR | | THERMOSTABILISED TURKEY BETA1 ADRENERGIC RECEPTOR WITH 4-METHYL-2-(PIPERAZIN-1-YL) QUINOLINE BOUND | | Descriptor: | BETA-1 ADRENERGIC RECEPTOR, SODIUM ION, CHOLESTEROL HEMISUCCINATE, ... | | Authors: | Christopher, J.A., Congreve, M., Dore, A.S., Marshall, F.H., Myszka, D.G., Brown, J., Koglin, M., Tehan, B., Errey, J.C., Tate, C.G., Warne, T. | | Deposit date: | 2013-03-01 | | Release date: | 2013-04-03 | | Last modified: | 2019-05-15 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Biophysical Fragment Screening of the Beta1-Adrenergic Receptor: Identification of High Affinity Aryl Piperazine Leads Using Structure-Based Drug Design.
J.Med.Chem., 56, 2013
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4AMI | | TURKEY BETA1 ADRENERGIC RECEPTOR WITH STABILISING MUTATIONS AND BOUND BIASED AGONIST BUCINDOLOL | | Descriptor: | BETA-1 ADRENERGIC RECEPTOR, 2-[(2S)-3-[[1-(1H-indol-3-yl)-2-methyl-propan-2-yl]amino]-2-oxidanyl-propoxy]benzenecarbonitrile, HEGA-10 | | Authors: | Warne, T., Edwards, P.C., Leslie, A.G., Tate, C.G. | | Deposit date: | 2012-03-11 | | Release date: | 2012-05-23 | | Last modified: | 2019-04-03 | | Method: | X-RAY DIFFRACTION (3.2 Å) | | Cite: | Crystal Structures of a Stabilized Beta1-Adrenoceptor Bound to the Biased Agonists Bucindolol and Carvedilol
Structure, 20, 2012
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4AMJ | | TURKEY BETA1 ADRENERGIC RECEPTOR WITH STABILISING MUTATIONS AND BOUND BIASED AGONIST CARVEDILOL | | Descriptor: | BETA-1 ADRENERGIC RECEPTOR, (2S)-1-(8H-CARBAZOL-4-YLOXY)-3-[2-(2-METHOXYPHENOXY)ETHYLAMINO]PROPAN-2-OL, SODIUM ION, ... | | Authors: | Warne, T., Edwards, P.C., Leslie, A.G., Tate, C.G. | | Deposit date: | 2012-03-12 | | Release date: | 2012-05-23 | | Last modified: | 2019-04-03 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Crystal Structures of a Stabilized Beta1-Adrenoceptor Bound to the Biased Agonists Bucindolol and Carvedilol
Structure, 20, 2012
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4BV0 | | HIGH RESOLUTION STRUCTURE OF EVOLVED AGONIST-BOUND NEUROTENSIN RECEPTOR 1 MUTANT WITHOUT LYSOZYME FUSION | | Descriptor: | NEUROTENSIN RECEPTOR TYPE 1, NEUROTENSIN/NEUROMEDIN N | | Authors: | Egloff, P., Hillenbrand, M., Scott, D.J., Schlinkmann, K.M., Heine, P., Balada, S., Batyuk, A., Mittl, P., Schuetz, M., Plueckthun, A. | | Deposit date: | 2013-06-24 | | Release date: | 2014-01-29 | | Last modified: | 2018-06-20 | | Method: | X-RAY DIFFRACTION (3.1 Å) | | Cite: | Structure of Signaling-Competent Neurotensin Receptor 1 Obtained by Directed Evolution in Escherichia Coli
Proc.Natl.Acad.Sci.USA, 111, 2014
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4BVN | | ULTRA-THERMOSTABLE BETA1-ADRENOCEPTOR WITH CYANOPINDOLOL BOUND | | Descriptor: | BETA-1 ADRENERGIC RECEPTOR, SODIUM ION, 4-{[(2S)-3-(tert-butylamino)-2-hydroxypropyl]oxy}-3H-indole-2-carbonitrile, ... | | Authors: | Miller, J., Nehme, R., Warne, T., Edwards, P.C., Leslie, A.G.W., Schertler, G., Tate, C.G. | | Deposit date: | 2013-06-26 | | Release date: | 2014-04-02 | | Last modified: | 2019-04-03 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | The 2.1 A Resolution Structure of Cyanopindolol-Bound Beta1- Adrenoceptor Identifies an Intramembrane Na+ Ion that Stabilises the Ligand-Free Receptor.
Plos One, 9, 2014
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4BWB | | STRUCTURE OF EVOLVED AGONIST-BOUND NEUROTENSIN RECEPTOR 1 MUTANT WITHOUT LYSOZYME FUSION | | Descriptor: | NEUROTENSIN RECEPTOR TYPE 1, NEUROTENSIN | | Authors: | Egloff, P., Hillenbrand, M., Scott, D.J., Schlinkmann, K.M., Heine, P., Balada, S., Batyuk, A., Mittl, P., Plueckthun, A. | | Deposit date: | 2013-07-01 | | Release date: | 2014-01-29 | | Last modified: | 2014-02-26 | | Method: | X-RAY DIFFRACTION (3.57 Å) | | Cite: | Structure of Signaling-Competent Neurotensin Receptor 1 Obtained by Directed Evolution in Escherichia Coli
Proc.Natl.Acad.Sci.USA, 111, 2014
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4GPO | |
4MQS | | STRUCTURE OF ACTIVE HUMAN M2 MUSCARINIC ACETYLCHOLINE RECEPTOR BOUND TO THE AGONIST IPEROXO | | Descriptor: | Muscarinic acetylcholine receptor M2, Nanobody 9-8, 4-(4,5-dihydro-1,2-oxazol-3-yloxy)-N,N,N-trimethylbut-2-yn-1-aminium | | 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: | 2017-07-05 | | 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: | Muscarinic acetylcholine receptor M2, Nanobody 9-8, 4-(4,5-dihydro-1,2-oxazol-3-yloxy)-N,N,N-trimethylbut-2-yn-1-aminium, ... | | 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: | 2019-05-01 | | Method: | X-RAY DIFFRACTION (3.7 Å) | | Cite: | Activation and allosteric modulation of a muscarinic acetylcholine receptor.
Nature, 504, 2013
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4U15 | | M3-MT4L RECEPTOR BOUND TO TIOTROPIUM | | Descriptor: | Muscarinic acetylcholine receptor M3,Lysozyme,Muscarinic acetylcholine receptor M3, (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, HEXAETHYLENE GLYCOL, ... | | Authors: | Thorsen, T.S., Matt, R., Weis, W.I., Kobilka, B. | | Deposit date: | 2014-07-15 | | Release date: | 2014-11-26 | | Last modified: | 2017-11-22 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Modified T4 Lysozyme Fusion Proteins Facilitate G Protein-Coupled Receptor Crystallogenesis.
Structure, 22, 2014
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4U16 | | M3-MT4L RECEPTOR BOUND TO NMS | | Descriptor: | Muscarinic acetylcholine receptor M3,Lysozyme,Muscarinic acetylcholine receptor M3, D(-)-TARTARIC ACID, N-methyl scopolamine | | Authors: | Thorsen, T.S., Matt, R., Weis, W.I., Kobilka, B. | | Deposit date: | 2014-07-15 | | Release date: | 2014-11-26 | | Last modified: | 2017-11-22 | | Method: | X-RAY DIFFRACTION (3.7 Å) | | Cite: | Modified T4 Lysozyme Fusion Proteins Facilitate G Protein-Coupled Receptor Crystallogenesis.
Structure, 22, 2014
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4UG2 | | THERMOSTABILISED HUMAN A2A RECEPTOR WITH CGS21680 BOUND | | Descriptor: | THERMOSTABILISED HUMAN A2A RECEPTOR, (2S)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 2-[P-(2-CARBOXYETHYL)PHENYLETHYL-AMINO]-5'-N-ETHYLCARBOXAMIDO ADENOSINE | | Authors: | Lebon, G., Edwards, P.C., Leslie, A.G.W., Tate, C.G. | | Deposit date: | 2015-03-21 | | Release date: | 2015-04-08 | | Last modified: | 2019-04-03 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Molecular Determinants of Cgs21680 Binding to the Human Adenosine A2A Receptor.
Mol.Pharmacol., 87, 2015
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4UHR | | THERMOSTABILISED HUMAN A2A RECEPTOR WITH CGS21680 BOUND | | Descriptor: | THERMOSTABILISED HUMAN A2A RECEPTOR, 2-[P-(2-CARBOXYETHYL)PHENYLETHYL-AMINO]-5'-N-ETHYLCARBOXAMIDO ADENOSINE | | Authors: | Lebon, G., Edwards, P.C., Leslie, A.G.W., Tate, C.G. | | Deposit date: | 2015-03-25 | | Release date: | 2015-04-08 | | Last modified: | 2019-04-03 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Molecular Determinants of Cgs21680 Binding to the Human Adenosine A2A Receptor.
Mol.Pharmacol., 87, 2015
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4WW3 | |
4YAY | | XFEL STRUCTURE OF HUMAN ANGIOTENSIN RECEPTOR | | Descriptor: | Soluble cytochrome b562,Type-1 angiotensin II receptor, 5,7-diethyl-1-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-3,4-dihydro-1,6-naphthyridin-2(1H)-one | | Authors: | Zhang, H., Unal, H., Gati, C., Han, G.W., Zatsepin, N.A., James, D., Wang, D., Nelson, G., Weierstall, U., Messerschmidt, M., Williams, G.J., Boutet, S., Yefanov, O.M., White, T.A., Liu, W., Ishchenko, A., Tirupula, K.C., Desnoyer, R., Sawaya, M.C., Xu, Q., Coe, J., Cornrad, C.E., Fromme, P., Stevens, R.C., Katritch, V., Karnik, S.S., Cherezov, V., GPCR Network (GPCR) | | Deposit date: | 2015-02-18 | | Release date: | 2015-04-22 | | Last modified: | 2019-12-25 | | Method: | X-RAY DIFFRACTION (2.9 Å) | | Cite: | Structure of the Angiotensin receptor revealed by serial femtosecond crystallography.
Cell, 161, 2015
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4Z34 | | CRYSTAL STRUCTURE OF HUMAN LYSOPHOSPHATIDIC ACID RECEPTOR 1 IN COMPLEX WITH ONO9780307 | | Descriptor: | Lysophosphatidic acid receptor 1, Soluble cytochrome b562, {1-[(2S,3S)-2-(2,3-dihydro-1H-inden-2-ylmethyl)-3-(3,5-dimethoxy-4-methylphenyl)-3-hydroxypropyl]-4-(methoxycarbonyl)-1H-pyrrol-3-yl}acetic acid, ... | | Authors: | Chrencik, J.E., Roth, C.B., Terakado, M., Kurata, H., Omi, R., Kihara, Y., Warshaviak, D., Nakade, S., Asmar-Rovira, G., Mileni, M., Mizuno, H., Griffith, M.T., Rodgers, C., Han, G.W., Velasquez, J., Chun, J., Stevens, R.C., Hanson, M.A., GPCR Network (GPCR) | | Deposit date: | 2015-03-30 | | Release date: | 2015-06-03 | | Last modified: | 2015-07-01 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Crystal Structure of Antagonist Bound Human Lysophosphatidic Acid Receptor 1.
Cell, 161, 2015
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4Z35 | | CRYSTAL STRUCTURE OF HUMAN LYSOPHOSPHATIDIC ACID RECEPTOR 1 IN COMPLEX WITH ONO-9910539 | | Descriptor: | Lysophosphatidic acid receptor 1,Soluble cytochrome b562, 3-{1-[(2S,3S)-3-(4-acetyl-3,5-dimethoxyphenyl)-2-(2,3-dihydro-1H-inden-2-ylmethyl)-3-hydroxypropyl]-4-(methoxycarbonyl)-1H-pyrrol-3-yl}propanoic acid, (2S)-2,3-dihydroxypropyl (7Z)-tetradec-7-enoate | | Authors: | Chrencik, J.E., Roth, C.B., Terakado, M., Kurata, H., Omi, R., Kihara, Y., Warshaviak, D., Nakade, S., Asmar-Rovira, G., Mileni, M., Mizuno, H., Griffith, M.T., Rodgers, C., Han, G.W., Velasquez, J., Chun, J., Stevens, R.C., Hanson, M.A., GPCR Network (GPCR) | | Deposit date: | 2015-03-30 | | Release date: | 2015-06-03 | | Last modified: | 2015-07-01 | | Method: | X-RAY DIFFRACTION (2.9 Å) | | Cite: | Crystal Structure of Antagonist Bound Human Lysophosphatidic Acid Receptor 1.
Cell, 161, 2015
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4Z36 | | CRYSTAL STRUCTURE OF HUMAN LYSOPHOSPHATIDIC ACID RECEPTOR 1 IN COMPLEX WITH ONO-3080573 | | Descriptor: | Lysophosphatidic acid receptor 1,Soluble cytochrome b562, 1-(4-{[(2S,3R)-2-(2,3-dihydro-1H-inden-2-yloxy)-3-(3,5-dimethoxy-4-methylphenyl)-3-hydroxypropyl]oxy}phenyl)cyclopropanecarboxylic acid, (2S)-2,3-dihydroxypropyl (7Z)-tetradec-7-enoate | | Authors: | Chrencik, J.E., Roth, C.B., Terakado, M., Kurata, H., Omi, R., Kihara, Y., Warshaviak, D., Nakade, S., Asmar-Rovira, G., Mileni, M., Mizuno, H., Griffith, M.T., Rodgers, C., Han, G.W., Velasquez, J., Chun, J., Stevens, R.C., Hanson, M.A., GPCR Network (GPCR) | | Deposit date: | 2015-03-30 | | Release date: | 2015-06-03 | | Last modified: | 2015-07-01 | | Method: | X-RAY DIFFRACTION (2.9 Å) | | Cite: | Crystal Structure of Antagonist Bound Human Lysophosphatidic Acid Receptor 1.
Cell, 161, 2015
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5A8E | | THERMOSTABILISED BETA1-ADRENOCEPTOR WITH RATIONALLY DESIGNED INVERSE AGONIST 7-METHYLCYANOPINDOLOL BOUND | | Descriptor: | BETA1 ADRENERGIC RECEPTOR, SODIUM ION, 4-[(2S)-3-(tert-butylamino)-2-hydroxypropoxy]-7-methyl-1H-indole-2-carbonitrile, ... | | Authors: | Sato, T., Baker, J.G., Warne, T., Brown, G.A., Congreve, M., Leslie, A.G.W., Tate, C.G. | | Deposit date: | 2015-07-15 | | Release date: | 2015-09-30 | | Last modified: | 2019-04-03 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Pharmacological Analysis and Structure Determination of 7-Methylcyanopindolol-Bound Beta1-Adrenergic Receptor.
Mol.Pharmacol., 88, 2015
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5C1M | | CRYSTAL STRUCTURE OF ACTIVE MU-OPIOID RECEPTOR BOUND TO THE AGONIST BU72 | | Descriptor: | Mu-type opioid receptor, Nanobody 39, (2S,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, ... | | 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: | 2019-12-11 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Structural insights into mu-opioid receptor activation.
Nature, 524, 2015
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5DSG | | STRUCTURE OF THE M4 MUSCARINIC ACETYLCHOLINE RECEPTOR (M4-MT4L) BOUND TO TIOTROPIUM | | Descriptor: | Muscarinic acetylcholine receptor M4,Endolysin,Endolysin,Muscarinic acetylcholine receptor M4, (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, OLEIC ACID, ... | | Authors: | Thal, D.M., Kobilka, B.K., Sexton, P.M., Christopoulos, A. | | Deposit date: | 2015-09-17 | | Release date: | 2016-03-16 | | Last modified: | 2020-01-08 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Crystal structures of the M1 and M4 muscarinic acetylcholine receptors.
Nature, 531, 2016
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