5NDD
| Crystal structure of a thermostabilised human protease-activated receptor-2 (PAR2) in complex with AZ8838 at 2.8 angstrom resolution | Descriptor: | (~{S})-(4-fluoranyl-2-propyl-phenyl)-(1~{H}-imidazol-2-yl)methanol, Lysozyme,Proteinase-activated receptor 2,Soluble cytochrome b562,Proteinase-activated receptor 2, PHOSPHATE ION, ... | Authors: | Cheng, R.K.Y, Fiez-Vandal, C, Schlenker, O, Edman, K, Aggeler, B, Brown, D.G, Brown, G, Cooke, R.M, Dumelin, C.E, Dore, A.S, Geschwindner, S, Grebner, C, Hermansson, N.-O, Jazayeri, A, Johansson, P, Leong, L, Prihandoko, R, Rappas, M, Soutter, H, Snijder, A, Sundstrom, L, Tehan, B, Thornton, P, Troast, D, Wiggin, G, Zhukov, A, Marshall, F.H, Dekker, N. | Deposit date: | 2017-03-08 | Release date: | 2017-05-03 | Last modified: | 2024-01-17 | Method: | X-RAY DIFFRACTION (2.801 Å) | Cite: | Structural insight into allosteric modulation of protease-activated receptor 2. Nature, 545, 2017
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4K5Y
| Crystal structure of human corticotropin-releasing factor receptor 1 (CRF1R) in complex with the antagonist CP-376395 | Descriptor: | (1R)-2-{[(S)-{[(2S)-2,3-dihydroxypropyl]oxy}(hydroxy)phosphoryl]oxy}-1-[(hexadecanoyloxy)methyl]ethyl (9Z)-octadec-9-enoate, (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 3,6-dimethyl-N-(pentan-3-yl)-2-(2,4,6-trimethylphenoxy)pyridin-4-amine, ... | Authors: | Hollenstein, K, Kean, J, Bortolato, A, Cheng, R.K.Y, Dore, A.S, Jazayeri, A, Cooke, R.M, Weir, M, Marshall, F.H. | Deposit date: | 2013-04-15 | Release date: | 2013-07-17 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (2.977 Å) | Cite: | Structure of class B GPCR corticotropin-releasing factor receptor 1. Nature, 499, 2013
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6LUQ
| Haloperidol bound D2 dopamine receptor structure inspired discovery of subtype selective ligands | Descriptor: | 4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-1-(4-fluorophenyl)butan-1-one, OLEIC ACID, chimera of D(2) dopamine receptor and Endolysin | Authors: | Fan, L, Tan, L, Chen, Z, Qi, J, Nie, F, Luo, Z, Cheng, J, Wang, S. | Deposit date: | 2020-01-30 | Release date: | 2020-03-04 | Last modified: | 2023-11-29 | Method: | X-RAY DIFFRACTION (3.1 Å) | Cite: | Haloperidol bound D2dopamine receptor structure inspired the discovery of subtype selective ligands. Nat Commun, 11, 2020
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4LDO
| Structure of beta2 adrenoceptor bound to adrenaline and an engineered nanobody | Descriptor: | (2S)-2,3-dihydroxypropyl (7Z)-tetradec-7-enoate, Camelid Antibody Fragment, L-EPINEPHRINE, ... | Authors: | Ring, A.M, Manglik, A, Kruse, A.C, Enos, M.D, Weis, W.I, Garcia, K.C, Kobilka, B.K. | Deposit date: | 2013-06-24 | Release date: | 2013-09-25 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (3.2 Å) | Cite: | Adrenaline-activated structure of beta 2-adrenoceptor stabilized by an engineered nanobody. Nature, 502, 2013
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6M9T
| Crystal structure of EP3 receptor bound to misoprostol-FA | Descriptor: | (11alpha,12alpha,13E,16S)-11,16-dihydroxy-16-methyl-9-oxoprost-13-en-1-oic acid, (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, OLEIC ACID, ... | Authors: | Audet, M, White, K.L, Breton, B, Zarzycka, B, Han, G.W, Lu, Y, Gati, C, Batyuk, A, Popov, P, Velasquez, J, Manahan, D, Hu, H, Weierstall, U, Liu, W, Shui, W, Katrich, V, Cherezov, V, Hanson, M.A, Stevens, R.C. | Deposit date: | 2018-08-24 | Release date: | 2018-12-05 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (2.5 Å) | Cite: | Crystal structure of misoprostol bound to the labor inducer prostaglandin E2receptor. Nat. Chem. Biol., 15, 2019
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6MXT
| Crystal structure of human beta2 adrenergic receptor bound to salmeterol and Nb71 | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 3,6,9,12,15,18-HEXAOXAICOSANE-1,20-DIOL, Endolysin, ... | Authors: | Masureel, M, Zou, Y, Picard, L.P, van der Westhuizen, E, Mahoney, J.P, Rodrigues, J.P.G.L.M, Mildorf, T.J, Dror, R.O, Shaw, D.E, Bouvier, M, Pardon, E, Steyaert, J, Sunahara, R.K, Weis, W.I, Zhang, C, Kobilka, B.K. | Deposit date: | 2018-10-31 | Release date: | 2018-11-14 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (2.95934224 Å) | Cite: | Structural insights into binding specificity, efficacy and bias of a beta2AR partial agonist. Nat. Chem. Biol., 14, 2018
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4LDE
| Structure of beta2 adrenoceptor bound to BI167107 and an engineered nanobody | Descriptor: | (2S)-2,3-dihydroxypropyl (7Z)-tetradec-7-enoate, 8-[(1R)-2-{[1,1-dimethyl-2-(2-methylphenyl)ethyl]amino}-1-hydroxyethyl]-5-hydroxy-2H-1,4-benzoxazin-3(4H)-one, Camelid Antibody Fragment, ... | Authors: | Ring, A.M, Manglik, A, Kruse, A.C, Enos, M.D, Weis, W.I, Garcia, K.C, Kobilka, B.K. | Deposit date: | 2013-06-24 | Release date: | 2013-09-25 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (2.79 Å) | Cite: | Adrenaline-activated structure of beta 2-adrenoceptor stabilized by an engineered nanobody. Nature, 502, 2013
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6NI3
| B2V2R-Gs protein subcomplex of a GPCR-G protein-beta-arrestin mega-complex | Descriptor: | 8-[(1R)-2-{[1,1-dimethyl-2-(2-methylphenyl)ethyl]amino}-1-hydroxyethyl]-5-hydroxy-2H-1,4-benzoxazin-3(4H)-one, Endolysin,Beta-2 adrenergic receptor chimera, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | Authors: | Nguyen, A.H, Thomsen, A.R.B, Cahill, T.J, des Georges, A, Lefkowitz, R.J. | Deposit date: | 2018-12-26 | Release date: | 2019-11-20 | Last modified: | 2019-12-18 | Method: | ELECTRON MICROSCOPY (3.8 Å) | Cite: | Structure of an endosomal signaling GPCR-G protein-beta-arrestin megacomplex. Nat.Struct.Mol.Biol., 26, 2019
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4LDL
| Structure of beta2 adrenoceptor bound to hydroxybenzylisoproterenol and an engineered nanobody | Descriptor: | (2S)-2,3-dihydroxypropyl (7Z)-tetradec-7-enoate, 4-[(1R)-1-hydroxy-2-{[1-(4-hydroxyphenyl)-2-methylpropan-2-yl]amino}ethyl]benzene-1,2-diol, Camelid Antibody Fragment, ... | Authors: | Ring, A.M, Manglik, A, Kruse, A.C, Enos, M.D, Weis, W.I, Garcia, K.C, Kobilka, B.K. | Deposit date: | 2013-06-24 | Release date: | 2013-09-25 | Last modified: | 2023-09-20 | Method: | X-RAY DIFFRACTION (3.1 Å) | Cite: | Adrenaline-activated structure of beta 2-adrenoceptor stabilized by an engineered nanobody. Nature, 502, 2013
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5DSG
| Structure of the M4 muscarinic acetylcholine receptor (M4-mT4L) bound to 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, (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 1-(2-METHOXY-ETHOXY)-2-{2-[2-(2-METHOXY-ETHOXY]-ETHOXY}-ETHANE, ... | Authors: | Thal, D.M, Kobilka, B.K, Sexton, P.M, Christopoulos, A. | Deposit date: | 2015-09-17 | Release date: | 2016-03-16 | Last modified: | 2024-03-13 | 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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4WTV
| Crystal structure of the phosphatidylinositol 4-kinase IIbeta | Descriptor: | ADENOSINE-5'-TRIPHOSPHATE, Phosphatidylinositol 4-kinase type 2-beta,Endolysin,Phosphatidylinositol 4-kinase type 2-beta | Authors: | Klima, M, Baumlova, A, Chalupska, D, Boura, E. | Deposit date: | 2014-10-30 | Release date: | 2015-07-15 | Last modified: | 2024-01-10 | Method: | X-RAY DIFFRACTION (1.9 Å) | Cite: | The high-resolution crystal structure of phosphatidylinositol 4-kinase II beta and the crystal structure of phosphatidylinositol 4-kinase II alpha containing a nucleoside analogue provide a structural basis for isoform-specific inhibitor design. Acta Crystallogr.,Sect.D, 71, 2015
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6J20
| Crystal structure of the human NK1 substance P receptor | Descriptor: | 5-[[(2~{R},3~{S})-2-[(1~{R})-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl]-1,2-dihydro-1,2,4-triazol-3-one, Substance-P receptor,Endolysin | Authors: | Chen, S, Lu, M, Zhang, H, Wu, B, Zhao, Q. | Deposit date: | 2018-12-30 | Release date: | 2019-03-06 | Last modified: | 2023-11-22 | Method: | X-RAY DIFFRACTION (2.7 Å) | Cite: | Human substance P receptor binding mode of the antagonist drug aprepitant by NMR and crystallography. Nat Commun, 10, 2019
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4XES
| Structure of active-like neurotensin receptor | Descriptor: | 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, CITRIC ACID, DI(HYDROXYETHYL)ETHER, ... | Authors: | Krumm, B.E, White, J.F, Shah, P, Grisshammer, R. | Deposit date: | 2014-12-24 | Release date: | 2015-07-29 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (2.6 Å) | Cite: | Structural prerequisites for G-protein activation by the neurotensin receptor. Nat Commun, 6, 2015
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6J21
| Crystal structure of the human NK1 substance P receptor | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 5-[[(2~{R},3~{S})-2-[(1~{R})-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl]-1,2-dihydro-1,2,4-triazol-3-one, Substance-P receptor,Endolysin | Authors: | Chen, S, Lu, M, Zhang, H, Wu, B, Zhao, Q. | Deposit date: | 2018-12-30 | Release date: | 2019-03-06 | Last modified: | 2023-11-22 | Method: | X-RAY DIFFRACTION (3.2 Å) | Cite: | Human substance P receptor binding mode of the antagonist drug aprepitant by NMR and crystallography. Nat Commun, 10, 2019
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4XEE
| Structure of active-like neurotensin receptor | Descriptor: | 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, CITRATE ANION, DI(HYDROXYETHYL)ETHER, ... | Authors: | Krumm, B.E, White, J.F, Shah, P, Grisshammer, R. | Deposit date: | 2014-12-23 | Release date: | 2015-07-29 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (2.9 Å) | Cite: | Structural prerequisites for G-protein activation by the neurotensin receptor. Nat Commun, 6, 2015
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6VMS
| Structure of a D2 dopamine receptor-G-protein complex in a lipid membrane | Descriptor: | Endolysin,D(2) dopamine receptor,D(2) dopamine 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: | Yin, J, Chen, K.M, Clark, M.J, Hijazi, M, Kumari, P, Bai, X, Sunahara, R.K, Barth, P, Rosenbaum, D.M. | Deposit date: | 2020-01-28 | Release date: | 2020-06-17 | Last modified: | 2020-08-19 | Method: | ELECTRON MICROSCOPY (3.8 Å) | Cite: | Structure of a D2 dopamine receptor-G-protein complex in a lipid membrane. Nature, 584, 2020
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5GLH
| Human endothelin receptor type-B in complex with ET-1 | Descriptor: | Endothelin Receptor Subtype-B, Peptide from Endothelin-1 | Authors: | Shihoya, W, Nishizawa, T, Okuta, A, Tani, K, Fujiyoshi, Y, Dohmae, N, Nureki, O, Doi, T. | Deposit date: | 2016-07-11 | Release date: | 2016-09-07 | Last modified: | 2020-02-26 | Method: | X-RAY DIFFRACTION (2.8 Å) | Cite: | Activation mechanism of endothelin ETB receptor by endothelin-1. Nature, 537, 2016
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5EE7
| Crystal structure of the human glucagon receptor (GCGR) in complex with the antagonist MK-0893 | Descriptor: | 3,6,9,12,15,18,21,24-OCTAOXAHEXACOSAN-1-OL, 3-[[4-[(1~{S})-1-[3-[3,5-bis(chloranyl)phenyl]-5-(6-methoxynaphthalen-2-yl)pyrazol-1-yl]ethyl]phenyl]carbonylamino]propanoic acid, Glucagon receptor,Endolysin,Glucagon receptor, ... | Authors: | Jazayeri, A, Dore, A.S, Lamb, D, Krishnamurthy, H, Southall, S.M, Baig, A.H, Bortolato, A, Koglin, M, Robertson, N.J, Errey, J.C, Andrews, S.P, Brown, A.J.H, Cooke, R.M, Weir, M, Marshall, F.H. | Deposit date: | 2015-10-22 | Release date: | 2016-04-20 | Last modified: | 2024-01-10 | Method: | X-RAY DIFFRACTION (2.5 Å) | Cite: | Extra-helical binding site of a glucagon receptor antagonist. Nature, 533, 2016
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4YC4
| Crystal structure of phosphatidyl inositol 4-kinase II alpha in complex with nucleotide analog | Descriptor: | ADENOSINE-5'-DIPHOSPHATE, Phosphatidylinositol 4-kinase type 2-alpha,Lysozyme,Phosphatidylinositol 4-kinase type 2-alpha, [(1S,3S,4S)-3-(6-amino-9H-purin-9-yl)bicyclo[2.2.1]hept-1-yl]methanol | Authors: | Klima, M, Boura, E. | Deposit date: | 2015-02-19 | Release date: | 2015-07-15 | Last modified: | 2024-05-08 | Method: | X-RAY DIFFRACTION (2.58 Å) | Cite: | The high-resolution crystal structure of phosphatidylinositol 4-kinase II beta and the crystal structure of phosphatidylinositol 4-kinase II alpha containing a nucleoside analogue provide a structural basis for isoform-specific inhibitor design. Acta Crystallogr.,Sect.D, 71, 2015
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5GLI
| Human endothelin receptor type-B in the ligand-free form | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, Endothelin Receptor Subtype-B, OLEIC ACID, ... | Authors: | Shihoya, W, Nishizawa, T, Okuta, A, Tani, K, Fujiyoshi, Y, Dohmae, N, Nureki, O, Doi, T. | Deposit date: | 2016-07-11 | Release date: | 2016-09-07 | Last modified: | 2020-02-26 | Method: | X-RAY DIFFRACTION (2.5 Å) | Cite: | Activation mechanism of endothelin ETB receptor by endothelin-1. Nature, 537, 2016
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6WJC
| Muscarinic acetylcholine receptor 1 - muscarinic toxin 7 complex | Descriptor: | (1R,5S)-8-METHYL-8-AZABICYCLO[3.2.1]OCT-3-YL (2R)-3-HYDROXY-2-PHENYLPROPANOATE, ACETAMIDE, CHOLESTEROL HEMISUCCINATE, ... | Authors: | Maeda, S, Kobilka, B.K. | Deposit date: | 2020-04-13 | Release date: | 2020-07-08 | Last modified: | 2023-10-18 | Method: | X-RAY DIFFRACTION (2.55 Å) | Cite: | Structure and selectivity engineering of the M1muscarinic receptor toxin complex. Science, 369, 2020
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5EUT
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6K1Q
| Human endothelin receptor type-B in complex with inverse agonist IRL2500 | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (2~{S})-2-[[(2~{R})-2-[(3,5-dimethylphenyl)carbonyl-methyl-amino]-3-(4-phenylphenyl)propanoyl]amino]-3-(1~{H}-indol-3-yl)propanoic acid, Endothelin B receptor,Endolysin,Endothelin B receptor, ... | Authors: | Nagiri, C, Shihoya, W, Nureki, O. | Deposit date: | 2019-05-11 | Release date: | 2019-07-17 | Method: | X-RAY DIFFRACTION (2.7 Å) | Cite: | Crystal structure of human endothelin ETBreceptor in complex with peptide inverse agonist IRL2500. Commun Biol, 2, 2019
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6KK7
| Structure of thermal-stabilised(M6) human GLP-1 receptor transmembrane domain | Descriptor: | Glucagon-like peptide 1 receptor,Endolysin,Glucagon-like peptide 1 receptor, N-{4-[(R)-(3,3-dimethylcyclobutyl)({6-[4-(trifluoromethyl)-1H-imidazol-1-yl]pyridin-3-yl}amino)methyl]benzene-1-carbonyl}-beta-alanine | Authors: | Song, G. | Deposit date: | 2019-07-23 | Release date: | 2019-11-13 | Last modified: | 2023-11-22 | Method: | X-RAY DIFFRACTION (3.1 Å) | Cite: | Mutagenesis facilitated crystallization of GLP-1R. Iucrj, 6, 2019
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6ZG9
| Structure of M1-StaR-T4L in complex with GSK1034702 at 2.5A | Descriptor: | 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, 7-fluoranyl-5-methyl-3-[1-(oxan-4-yl)piperidin-4-yl]-1~{H}-benzimidazol-2-one, Muscarinic acetylcholine receptor M1,Endolysin,Muscarinic acetylcholine receptor M1, ... | Authors: | Rucktooa, P, Cooke, R.M. | Deposit date: | 2020-06-18 | Release date: | 2021-10-06 | Last modified: | 2024-01-24 | Method: | X-RAY DIFFRACTION (2.5 Å) | Cite: | From structure to clinic: Design of a muscarinic M1 receptor agonist with potential to treatment of Alzheimer's disease. Cell, 184, 2021
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