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GPCR-EXP: a database of experimentally solved GPCR structure


[GPCR-I-TASSER] [GPCR-HGmod] [GPCR-RD]

Updated on August 13, 2015

Number PDB-ID Resolution Release date GPCR name Reference
1, Rhodopsin
1 1F88 2.80 Å 2000-08-04 bovine rhodopsin with 11-cis-retinal Palczewski, K.; Kumasaka, T.; Hori, T.; Behnke, C. A.; Motoshima, H.; Fox, B. A.; Le Trong, I.; Teller, D. C.; Okada, T.; Stenkamp, R. E.; Yamamoto, M.; Miyano, M. Crystal structure of rhodopsin: A G protein-coupled receptor. Science 2000, 289, 739 [Download PDF]
2 1HZX 2.80 Å 2001-07-04 bovine rhodopsin with 11-cis-retinal Teller, D. C.; Okada, T.; Behnke, C. A.; Palczewski, K.; Stenkamp, R. E. Advances in determination of a high-resolution three-dimensional structure of rhodopsin, a model of G-protein-coupled receptors (GPCRs). Biochemistry 2001, 40, 7761 [Download PDF]
3 1L9H 2.60 Å 2002-05-15 bovine rhodopsin with 11-cis-retinal Okada, T.; Fujiyoshi, Y.; Silow, M.; Navarro, J.; Landau, E. M.; Shichida, Y. Functional role of internal water molecules in rhodopsin revealed by X-ray crystallography Proc. Natl. Acad. Sci. U.S.A. 2002, 99, 5982 [Download PDF]
4 1GZM 2.65 Å 2003-11-20 bovine rhodopsin with 11-cis-retinal Li, J.; Edwards, P. C.; Burghammer, M.; Villa, C.; Schertler, G. F. Structure of bovine rhodopsin in a trigonal crystal form. J. Mol. Biol. 2004, 343, 1409 [Download PDF]
5 1U19 2.20 Å 2004-10-12 bovine rhodopsin with 11-cis-retinal Okada, T.; Sugihara, M.; Bondar, A. N.; Elstner, M.; Entel, P.; Buss, V. The retinal conformation and its environment in rhodopsin in light of a new 2.2 A crystal structure. J. Mol. Biol. 2004, 342, 571 [Download PDF]
6 2HPY 2.80 Å 2006-08-22 bovine lumirhodopsin with all-trans-retinal Nakamichi, H.; Okada, T. Local peptide movement in the photoreaction intermediate of rhodopsin. Proc. Natl. Acad. Sci. U.S.A. 2006, 103, 12729 [Download PDF]
7 2G87 2.60 Å 2006-09-02 bovine bathorhodopsin with all-trans-retinal Nakamichi, H.; Okada, T. Crystallographic analysis of primary visual photochemistry. Angew. Chem., Int. Ed. Engl. 2006, 45, 4270 [Download PDF]
8 2I35 3.80 Å 2006-10-17 bovine rhodopsin with 11-cis-retinal Salom, D.; Lodowski, D. T.; Stenkamp, R. E.; Le Trong, I.; Golczak, M.; Jastrzebska, B.; Harris, T.; Ballesteros, J. A.; Palczewski, K. Crystal structure of a photoactivated deprotonated intermediate of rhodopsin. Proc. Natl. Acad. Sci. U.S.A. 2006, 103, 16123 [Download PDF]
9 2I36 4.10 Å 2006-10-17 bovine rhodopsin with 11-cis-retinala Salom, D.; Lodowski, D. T.; Stenkamp, R. E.; Le Trong, I.; Golczak, M.; Jastrzebska, B.; Harris, T.; Ballesteros, J. A.; Palczewski, K. Crystal structure of a photoactivated deprotonated intermediate of rhodopsin. Proc. Natl. Acad. Sci. U.S.A. 2006, 103, 16123 [Download PDF]
10 2I37 4.15 Å 2006-10-17 bovine rhodopsin with all-trans-retinala Salom, D.; Lodowski, D. T.; Stenkamp, R. E.; Le Trong, I.; Golczak, M.; Jastrzebska, B.; Harris, T.; Ballesteros, J. A.; Palczewski, K. Crystal structure of a photoactivated deprotonated intermediate of rhodopsin. Proc. Natl. Acad. Sci. U.S.A. 2006, 103, 16123 [Download PDF]
11 2J4Y 3.40 Å 2007-09-25 mutant bovine rhodopsin with 11-cis-retinal Standfuss, J.; Xie, G.; Edwards, P. C.; Burghammer, M.; Oprian, D. D.; Schertler, G. F. Crystal structure of a thermally stable rhodopsin mutant. J. Mol. Biol. 2007, 372, 1179 [Download PDF]
12 2PED 2.95 Å 2007-10-30 bovine rhodopsin with 9-cis-retinal Nakamichi, H.; Okada, T. Photochem. X-ray crystallographic analysis of 9-cis-rhodopsin, a model analogue visual pigment. Photobiol. 2007, 83, 232 [Download PDF]
13 3CAP 2.90 Å 2008-06-24 Native Opsin: the G Protein-Coupled Receptor rhodopsin in its ligand-free state Park, J. H.; Scheerer, P.; Hofmann, K. P.; Choe, H. W.; Ernst, O. P. Crystal structure of the ligand-free G-protein-coupled receptor opsin. Nature 2008, 454, 183 [Download PDF]
14 3C9L 2.65 Å 2008-08-05 bovine rhodopsin with 11-cis-retinal Stenkamp, R. E. Acta Crystallogr., Sect. D: Biol. Alternative models for two crystal structures of bovine rhodopsin. Crystallogr. 2008, D64, 902 [Download PDF]
15 3C9M 3.40 Å 2008-08-05 bovine rhodopsin with 11-cis-retinal Stenkamp, R. E. Acta Crystallogr., Sect. D: Biol. Alternative models for two crystal structures of bovine rhodopsin. Crystallogr. 2008, D64, 902 [Download PDF]
16 3DQB 3.20 Å 2008-09-23 bovine opsin (ligand-free form of the G-protein-coupled receptor rhodopsin) in complex with GtCT Scheerer, P.; Park, J. H.; Hildebrand, P. W.; Kim, Y. J.; Krauss, N.; Choe, H. W.; Hofmann, K. P.; Ernst, O. P. Crystal structure of opsin in its G-protein-interacting conformation. Nature 2008, 455, 497 [Download PDF]
17 3PXO 3.00 Å 2011-03-09 metarhodopsin II. Choe, H. W.; Kim, Y. J.; Park, J. H.; Morizumi, T.; Pai, E. F.; Krauss, N.; Hofmann, K. P.; Scheerer, P.; Ernst, O. P. Nature 2011, 471, 651 [Download PDF]
18 3PQR 2.85 Å 2011-03-09 metarhodopsin II. Choe, H. W.; Kim, Y. J.; Park, J. H.; Morizumi, T.; Pai, E. F.; Krauss, N.; Hofmann, K. P.; Scheerer, P.; Ernst, O. P. Crystal structure of metarhodopsin II. Nature 2011, 471, 651 [Download PDF]
19 2X72 3.00 Å 2011-03-16 constitutively active bovine rhodopsin mutant bound to GtCt Standfuss, J.; Edwards, P. C.; Du2019Antona, A.; Fransen, M.; Xie, G.; Oprian, D. D.; Schertler, G. F. Nature 2011, 471, 656 [Download PDF]
20 2ZIY 3.70 Å 2008-05-06 squid rhodopsin with 11-cis-retinal Shimamura, T.; Hiraki, K.; Takahashi, N.; Hori, T.; Ago, H.; Masuda, K.; Takio, K.; Ishiguro, M.; Miyano, M. The structural basis of agonist-induced activation in constitutively active rhodopsin. J. Biol. Chem. 2008, 283, 17753 [Download PDF]
21 2Z73 2.50 Å 2008-05-13 squid rhodopsin with 11-cis-retinal Murakami, M.; Kouyama, T. Crystal structure of squid rhodopsin. Nature 2008, 453, 363 [Download PDF]
22 3AYM 2.80 Å 2011-08-17 batho intermediate of squid rhodopsin Murakami M, Kouyama T. Crystallographic analysis of the primary photochemical reaction of squid rhodopsin. J Mol Biol. 2011 Oct 28;413(3):615-27. [Download PDF]
23 3AYN 2.70 Å 2011-08-17 batho intermediate of squid rhodopsin Murakami M, Kouyama T. Crystallographic analysis of the primary photochemical reaction of squid rhodopsin. J Mol Biol. 2011 Oct 28;413(3):615-27. [Download PDF]
24 3OAX 2.60 Å 2011-01-19 bovine rhodopsin with beta-ionone Makino CL, Riley CK, Looney J, Crouch RK, Okada T. Binding of more than one retinoid to visual opsins. Biophys J. 2010 Oct 6;99(7):2366-73. [Download PDF]
25 4BEY 2.90 Å 2013-05-08 night blindness causing G90D rhodopsin in complex with GaCT2 peptide Singhal A, Ostermaier MK, Vishnivetskiy SA, Panneels V, Homan KT, Tesmer JJ, Veprintsev D, Deupi X, Gurevich VV, Schertler GF, Standfuss J. Insights into congenital stationary night blindness based on the structure of G90D rhodopsin. EMBO Rep. 2013 Jun;14(6):520-6. [Download PDF]
26 4BEZ 3.30 Å 2013-04-24 night blindness causing G90D rhodopsin in the active conformation Singhal A, Ostermaier MK, Vishnivetskiy SA, Panneels V, Homan KT, Tesmer JJ, Veprintsev D, Deupi X, Gurevich VV, Schertler GF, Standfuss J. Insights into congenital stationary night blindness based on the structure of G90D rhodopsin. EMBO Rep. 2013 Jun;14(6):520-6. [Download PDF]
27 4A4M 3.30 Å 2012-01-25 light-activated constitutively active N2C, M257Y,D282C rhodopsin mutant in complex with a peptide resembling the C-terminus of the Galpha-protein subunit Deupi X, Edwards P, Singhal A, Nickle B, Oprian D, Schertler G, Standfuss J. Stabilized G protein binding site in the structure of constitutively active metarhodopsin-II. Proc Natl Acad Sci U S A. 2012 Jan 3;109(1):119-24. [Download PDF]
28 4J4Q 2.65 Å 2013-10-30 Active conformation of rhodopsin stabilized by octylglucoside Park JH, Morizumi T, Li Y, Hong JE, Pai EF, Hofmann KP, Choe HW, Ernst OP., Opsin, a structural model for olfactory receptors? Angew Chem Int Ed Engl. 2013 Oct 11;52(42):11021-4. [Download PDF]
29 4PXF 2.75 Å 2014-09-17 bovine rhodopsin in complex with the finger-loop peptide Szczepek M, Beyrière F, Hofmann KP, Elgeti M, Kazmin R, Rose A, Bartl FJ, von Stetten D, Heck M, Sommer ME, Hildebrand PW, Scheerer P. Crystal structure of a common GPCR-binding interface for G protein and arrestin. Nat Commun. 2014 Sep 10;5:4801. [PubMed]
30 4S0V 2.5 Å 2015-01-14 human OX2 orexin receptor (OX2R, belongs to the beta branch of the rhodopsin family of GPCRs) bound to the insomnia drug Suvorexant Yin J, Mobarec JC, Kolb P, Rosenbaum DM. Nature. 2015 Mar 12;519(7542):247-50. [PubMed]
31 4WW3 2.8 Å 2015-06-17 Crystal structure of the lumi intermediate of squid rhodopsin Murakami M, Kouyama T. PLoS One. 2015 May 29;10(5):e0126970. [PubMed]
2, Human Beta2-adrenergic-aceptor (B2AR)
32 2RH1 2.40 Å 2007-10-30 human B2AR with the inverse agonist carazolol Cherezov, V.; Rosenbaum, D. M.; Hanson, M. A.; Rasmussen, S. G.; Thian, F. S.; Kobilka, T. S.; Choi, H. J.; Kuhn, P.; Weis, W. I.; Kobilka, B. K.; Stevens, R. C. High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor. Science 2007, 318, 1258 [Download PDF]
33 2R4R 3.40 Å 2007-11-06 human B2AR with the inverse agonist carazolola Rasmussen, S. G.; 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. Crystal structure of the human beta2 adrenergic G-protein-coupled receptor. Nature 2007, 450, 383 [Download PDF]
34 2R4S 3.40 Å 2007-11-06 human B2AR with the inverse agonist carazolola Rasmussen, S. G.; 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. Crystal structure of the human beta2 adrenergic G-protein-coupled receptor. Nature 2007, 450, 383 [Download PDF]
35 3D4S 2.80 Å 2008-06-17 human B2AR with the inverse agonist timolol Hanson, M. A.; Cherezov, V.; Griffith, M. T.; Roth, C. B.; Jaakola, V. P.; Chien, E. Y.; Velasquez, J.; Kuhn, P.; Stevens, R. C. A specific cholesterol binding site is established by the 2.8 A structure of the human beta2-adrenergic receptor. Structure 2008, 16, 897 [Download PDF]
36 3NY8 2.84 Å 2010-08-11 human B2AR with the inverse agonist ICI 118,551 Wacker, D.; Fenalti, G.; Brown, M. A.; Katritch, V.; Abagyan, R.; Cherezov, V.; Stevens, R. C. Conserved binding mode of human beta2 adrenergic receptor inverse agonists and antagonist revealed by X-ray crystallography. J. Am. Chem. Soc. 2010, 132, 11443 [Download PDF]
37 3NY9 2.84 Å 2010-08-11 human B2AR with a novel inverse agonist Wacker, D.; Fenalti, G.; Brown, M. A.; Katritch, V.; Abagyan, R.; Cherezov, V.; Stevens, R. C. Conserved binding mode of human beta2 adrenergic receptor inverse agonists and antagonist revealed by X-ray crystallography. J. Am. Chem. Soc. 2010, 132, 11443 [Download PDF]
38 3NYA 3.16 Å 2010-08-11 human B2AR with the antagonist alprenolol Wacker, D.; Fenalti, G.; Brown, M. A.; Katritch, V.; Abagyan, R.; Cherezov, V.; Stevens, R. C. Conserved binding mode of human beta2 adrenergic receptor inverse agonists and antagonist revealed by X-ray crystallography. J. Am. Chem. Soc. 2010, 132, 11443 [Download PDF]
39 3PDS 3.50 Å 2011-01-12 human B2AR with an irreversible agonist Rosenbaum, D. M.; Zhang, C.; Lyons, J. A.; Holl, R.; Aragao, D.; Arlow, D. H.; Rasmussen, S. G.; 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. Structure and function of an irreversible agonist-beta2 adrenoceptor complex. Nature 2011, 469, 236 [Download PDF]
40 3P0G 3.50 Å 2011-01-19 nanobody-stabilized active state of the B2AR Rasmussen, S. G.; 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. Structure of a nanobody-stabilized active state of the beta2 adrenoceptor. Nature 2011, 469, 175 [Download PDF]
41 3SN6 3.20 Å 2011-07-20 human B2AR in complex with heterotrimeric Gs Rasmussen, S. G.; 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.; Lyons, J. A.; Caffrey, M.; Gellman, S. H.; Steyaert, J.; Skiniotis, G.; Weis, W. I.; Sunahara, R. K.; Kobilka, B. K. Crystal structure of the beta2 adrenergic receptor-Gs protein complex. Nature 2011, 477, 549 [Download PDF]
42 3KJ6 3.40 Å 2010-02-16 methylated B2AR-fab complex Bokoch MP, Zou Y, Rasmussen SG, Liu CW, Nygaard R, Rosenbaum DM, Fung JJ, Choi HJ, Thian FS, Kobilka TS, Puglisi JD, Weis WI, Pardo L, Prosser RS, Mueller L, Kobilka BK. Ligand-specific regulation of the extracellular surface of a G-protein-coupled receptor. Nature. 2010 Jan 7;463(7277):108-12. [Download PDF]
43 4GBR 3.99 Å 2012-10-24 N-terminal T4 lysozyme fusion facilitates crystallization of B2AR Zou Y, Weis WI, Kobilka BK. N-terminal T4 lysozyme fusion facilitates crystallization of a G protein coupled receptor. PLoS One. 2012;7(10):e46039. [Download PDF]
44 4LDE 2.79 Å 2013-09-25 B2AR bound to BI167107 and an engineered nanobody Ring AM, Manglik A, Kruse AC, Enos MD, Weis WI, Garcia KC, Kobilka BK.,Adrenaline-activated structure of β2-adrenoceptor stabilized by an engineered nanobody. Nature. 2013 Oct 24;502(7472):575-9. [Download PDF]
45 4LDL 3.10 Å 2013-09-25 B2AR bound to hydroxybenzylisoproterenol and an engineered nanobody Ring AM, Manglik A, Kruse AC, Enos MD, Weis WI, Garcia KC, Kobilka BK.,Adrenaline-activated structure of β2-adrenoceptor stabilized by an engineered nanobody. Nature. 2013 Oct 24;502(7472):575-9. [Download PDF]
46 4LDO 3.20 Å 2013-09-25 B2AR bound to adrenaline and an engineered nanobody Ring AM, Manglik A, Kruse AC, Enos MD, Weis WI, Garcia KC, Kobilka BK.,Adrenaline-activated structure of β2-adrenoceptor stabilized by an engineered nanobody. Nature. 2013 Oct 24;502(7472):575-9. [Download PDF]
47 4QKX 3.30 Å 2014-07-23 hman B2AR bound to a covalent agonist and an engineered nanobody Weichert D, Kruse AC, Manglik A, Hiller C, Zhang C, Hubner H, Kobilka BK, Gmeiner P. Covalent agonists for studying G protein-coupled receptor activation. Proc Natl Acad Sci U S A. 2014 Jul 8 [PubMed]
3, Turkey Beta1-Adrenergic-aceptor (B1AR)
48 2VT4 2.70 Å 2008-06-24 turkey B1AR with the antagonist cyanopindolol Warne, T.; Serrano-Vega, M. J.; Baker, J. G.; Moukhametzianov, R.; Edwards, P. C.; Henderson, R.; Leslie, A. G.; Tate, C. G.; Schertler, G. F. Structure of a beta1-adrenergic G-protein-coupled receptor. Nature 2008, 454, 486 [Download PDF]
49 2Y00 2.50 Å 2011-01-12 turkey B1AR with the partial agonist dobutamine Warne, T.; Moukhametzianov, R.; Baker, J. G.; Nehme, R.; Edwards, P. C.; Leslie, A. G.; Schertler, G. F.; Tate, C. G. Structure of a beta1-adrenergic G-protein-coupled receptor. Nature 2011, 469, 241 [Download PDF]
50 2Y02 2.60 Å 2011-01-12 turkey B1AR with the agonist carmoterol Warne, T.; Moukhametzianov, R.; Baker, J. G.; Nehme, R.; Edwards, P. C.; Leslie, A. G.; Schertler, G. F.; Tate, C. G. Structure of a beta1-adrenergic G-protein-coupled receptor. Nature 2011, 469, 241 [Download PDF]
51 2Y03 2.85 Å 2011-01-12 turkey B1AR with the agonist isoprenaline Warne, T.; Moukhametzianov, R.; Baker, J. G.; Nehme, R.; Edwards, P. C.; Leslie, A. G.; Schertler, G. F.; Tate, C. G. Structure of a beta1-adrenergic G-protein-coupled receptor. Nature 2011, 469, 241 [Download PDF]
52 2Y04 3.05 Å 2011-01-12 turkey B1AR with the partial agonist salbutamol Warne, T.; Moukhametzianov, R.; Baker, J. G.; Nehme, R.; Edwards, P. C.; Leslie, A. G.; Schertler, G. F.; Tate, C. G. Structure of a beta1-adrenergic G-protein-coupled receptor. Nature 2011, 469, 241 [Download PDF]
53 2Y01 2.60 Å 2011-03-30 turkey B1AR with the partial agonist dobutamine Warne, T.; Moukhametzianov, R.; Baker, J. G.; Nehme, R.; Edwards, P. C.; Leslie, A. G.; Schertler, G. F.; Tate, C. G. Structure of a beta1-adrenergic G-protein-coupled receptor. Nature 2011, 469, 241 [Download PDF]
54 2YCW 3.00 Å 2011-06-01 turkey B1AR with the antagonist carazolol Moukhametzianov, R.; Warne, T.; Edwards, P. C.; Serrano-Vega, M. J.; Leslie, A. G.; Tate, C. G.; Schertler, G. F. Two distinct conformations of helix 6 observed in antagonist-bound structures of a beta1-adrenergic receptor. Proc. Natl. Acad. Sci. U.S.A. 2011, 108, 8228 [Download PDF]
55 2YCX 3.25 Å 2011-06-01 turkey B1AR with the antagonist cyanopindolol Moukhametzianov, R.; Warne, T.; Edwards, P. C.; Serrano-Vega, M. J.; Leslie, A. G.; Tate, C. G.; Schertler, G. F. Two distinct conformations of helix 6 observed in antagonist-bound structures of a beta1-adrenergic receptor. Proc. Natl. Acad. Sci. U.S.A. 2011, 108, 8228 [Download PDF]
56 2YCZ 3.65 Å 2011-06-01 turkey B1AR with the antagonist iodocyanopindolol Moukhametzianov, R.; Warne, T.; Edwards, P. C.; Serrano-Vega, M. J.; Leslie, A. G.; Tate, C. G.; Schertler, G. F. Two distinct conformations of helix 6 observed in antagonist-bound structures of a beta1-adrenergic receptor. Proc. Natl. Acad. Sci. U.S.A. 2011, 108, 8228 [Download PDF]
57 2YCY 3.15 Å 2011-06-08 turkey B1AR with the antagonist cyanopindolol Moukhametzianov, R.; Warne, T.; Edwards, P. C.; Serrano-Vega, M. J.; Leslie, A. G.; Tate, C. G.; Schertler, G. F. Two distinct conformations of helix 6 observed in antagonist-bound structures of a beta1-adrenergic receptor. Proc. Natl. Acad. Sci. U.S.A. 2011, 108, 8228 [Download PDF]
58 4AMI 3.20 Å 2012-05-23 turkey B1AR with stabilising mutations and bound biased agonist bucindolol Warne T, Edwards PC, Leslie AG, Tate CG. Crystal structures of a stabilized β1-adrenoceptor bound to the biased agonists bucindolol and carvedilol. Structure. 2012 May 9;20(5):841-9. [Download PDF]
59 4AMJ 2.30 Å 2012-05-23 turkey B1AR with stabilising mutations and bound biased agonist carvedilol Warne T, Edwards PC, Leslie AG, Tate CG. Crystal structures of a stabilized β1-adrenoceptor bound to the biased agonists bucindolol and carvedilol. Structure. 2012 May 9;20(5):841-9. [Download PDF]
60 4GPO 3.50 Å 2013-02-27 oligomeic turkey B1AR Huang JJ, Chen S, Zhang JJ, Huang X-Y. Crystal structure of oligomeric Beta1-adrenergic G protein coupled receptors in ligand-free basal state. Nat Struct Mol Biol. 2013 Apr;20(4):419-25. [Download PDF]
61 3ZPR 2.70 Å 2013-04-03 Thermostabilised turkey B1AR with 4-methyl-2-(piperazin-1-yl) quinoline bound Christopher JA, Brown J, Dore AS, Errey JC, Koglin M, Marshall FH, Myszka DG, Rich RL, Tate CG, Tehan B, Warne T, Congreve M. Biophysical fragment screening of the β1-adrenergic receptor: identification of high affinity arylpiperazine leads using structure-based drug design. J Med Chem. 2013 May 9;56(9):3446-55. [Download PDF]
62 3ZPQ 2.80 Å 2013-04-03 Thermostabilised turkey B1AR with 4-methyl-2-(piperazin-1-yl) quinoline bound Christopher JA, Brown J, Dore AS, Errey JC, Koglin M, Marshall FH, Myszka DG, Rich RL, Tate CG, Tehan B, Warne T, Congreve M. Biophysical fragment screening of the β1-adrenergic receptor: identification of high affinity arylpiperazine leads using structure-based drug design. J Med Chem. 2013 May 9;56(9):3446-55. [Download PDF]
63 4BVN 2.10 Å 2014-04-02 beta1-adrenoceptor (B1AR) with cyanopindolol bound Miller-Gallacher JL, Nehme R, Warne T, Edwards PC, Schertler GF, Leslie AG, Tate CG. The 2.1 A Resolution Structure of Cyanopindolol-Bound β1-Adrenoceptor Identifies an Intramembrane Na+ Ion that Stabilises the Ligand-Free Receptor. PLoS One. 2014 Mar 24;9(3):e92727 [PubMed]
4, Human Alpha2 Adenosine receptor (A2AR)
64 3EML 2.60 Å 2008-10-14 human A2AR with the antagonist ZM241385 Jaakola, V. P.; Griffith, M. T.; Hanson, M. A.; Cherezov, V.; Chien, E. Y.; Lane, J. R.; Ijzerman, A. P.; Stevens, R. C. The 2.6 Angstrom Crystal Structure of a Human A2A Adenosine Receptor Bound to an Antagonist Science 2008, 322, 1211 [Download PDF]
65 3QAK 2.71 Å 2011-03-09 human A2AR with the agonist UKA Xu, F.; Wu, H.; Katritch, V.; Han, G. W.; Jacobson, K. A.; Gao, Z. G.; Cherezov, V.; Stevens, R. C. Structure of an agonist-bound human A2A adenosine receptor. Science 2011, 332, 322 [Download PDF]
66 2YDO 3.00 Å 2011-05-18 human A2AR with the agonist adenosine Lebon, G.; Warne, T.; Edwards, P. C.; Bennett, K.; Langmead, C. J.; Leslie, A. G.; Tate, C. G. Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation. Nature 2011, 474, 521 [Download PDF]
67 2YDV 2.60 Å 2011-05-18 human A2AR with the agonist NECA Lebon, G.; Warne, T.; Edwards, P. C.; Bennett, K.; Langmead, C. J.; Leslie, A. G.; Tate, C. G. Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation. Nature 2011, 474, 521 [Download PDF]
68 3PWH 3.30 Å 2011-09-07 thermostabilized A2AR Dore AS, Robertson N, Errey JC, Ng I, Hollenstein K, Tehan B, Hurrell E, Bennett K, Congreve M, Magnani F, Tate CG, Weir M, Marshall FH. Structure of the adenosine A(2A) receptor in complex with ZM241385 and the xanthines XAC and caffeine. Structure. 2011 Sep 7;19(9):1283-93. [PubMed]
69 3REY 3.31 Å 2011-09-07 thermostabilized A2AR Dore AS, Robertson N, Errey JC, Ng I, Hollenstein K, Tehan B, Hurrell E, Bennett K, Congreve M, Magnani F, Tate CG, Weir M, Marshall FH. Structure of the adenosine A(2A) receptor in complex with ZM241385 and the xanthines XAC and caffeine. Structure. 2011 Sep 7;19(9):1283-93. [PubMed]
70 3RFM 3.60 Å 2011-09-07 thermostabilized A2AR Dore AS, Robertson N, Errey JC, Ng I, Hollenstein K, Tehan B, Hurrell E, Bennett K, Congreve M, Magnani F, Tate CG, Weir M, Marshall FH. Structure of the adenosine A(2A) receptor in complex with ZM241385 and the xanthines XAC and caffeine. Structure. 2011 Sep 7;19(9):1283-93. [PubMed]
71 3UZA 3.27 Å 2012-03-21 Thermostabilised A2AR in complex with T4G Congreve M, Andrews SP, Dore AS, Hollenstein K, Hurrell E, Langmead CJ, Mason JS, Ng IW, Tehan B, Zhukov A, Weir M, Marshall FH. Discovery of 1,2,4-triazine derivatives as adenosine A(2A) antagonists using structure based drug design. J Med Chem. 2012 Mar 8;55(5):1898-903. [Download PDF]
72 3UZC 3.34 Å 2012-03-21 Thermostabilised A2AR in complex with T4E Congreve M, Andrews SP, Dore AS, Hollenstein K, Hurrell E, Langmead CJ, Mason JS, Ng IW, Tehan B, Zhukov A, Weir M, Marshall FH. Discovery of 1,2,4-triazine derivatives as adenosine A(2A) antagonists using structure based drug design. J Med Chem. 2012 Mar 8;55(5):1898-903. [Download PDF]
73 3VG9 2.70 Å 2012-02-01 human A2AR with an allosteric inverse-agonist antibody 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 AD, Kobayashi T, Hamakubo T, Iwata S, Murata T. G-protein-coupled receptor inactivation by an allosteric inverse-agonist antibody. Nature. 2012 Jan 29;482(7384):237-40. [Download PDF]
74 3VGA 3.10 Å 2012-02-01 human A2AR with an allosteric inverse-agonist antibody 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 AD, Kobayashi T, Hamakubo T, Iwata S, Murata T. G-protein-coupled receptor inactivation by an allosteric inverse-agonist antibody. Nature. 2012 Jan 29;482(7384):237-40. [Download PDF]
75 4EIY 1.80 Å 2012-07-25 chimeric protein of A2aAR-BRIL in complex with ZM241385 Liu W, Chun E, Thompson AA, Chubukov P, Xu F, Katritch V, Han GW, Roth CB, Heitman LH, IJzerman AP, Cherezov V, Stevens RC. Structural basis for allosteric regulation of GPCRs by sodium ions. Science. 2012 Jul 13;337(6091):232-6. [Download PDF]
76 4UG2 2.6 Å 2015-04-08 Thermostabilised human A2a Receptor with CGS21680 bound Lebon G, Edwards PC, Leslie AG, Tate CG. Mol Pharmacol. 2015 Jun;87(6):907-15. [PubMed]
77 4UHR 2.6 Å 2015-04-08 Thermostabilised human A2a Receptor with CGS21680 bound Lebon G, Edwards PC, Leslie AG, Tate CG. Mol Pharmacol. 2015 Jun;87(6):907-15. [PubMed]
5, Human Chemokine receptor type 4 (CXCR4)
78 3OE0 2.90 Å 2010-10-27 human CXCR4 with the peptide antagonist CVX15 Wu, B.; Chien, E. Y.; Mol, C. D.; Fenalti, G.; Liu, W.; Katritch, V.; Abagyan, R.; Brooun, A.; Wells, P.; Bi, F. C.; Hamel, D. J.; Kuhn, P.; Handel, T. M.; Cherezov, V.; Stevens, R. C. Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists. Science 2010, 330, 1066 [Download PDF]
79 3OE6 3.20 Å 2010-10-27 human CXCR4 with the small ligand antagonist IT1t Wu, B.; Chien, E. Y.; Mol, C. D.; Fenalti, G.; Liu, W.; Katritch, V.; Abagyan, R.; Brooun, A.; Wells, P.; Bi, F. C.; Hamel, D. J.; Kuhn, P.; Handel, T. M.; Cherezov, V.; Stevens, R. C. Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists. Science 2010, 330, 1066 [Download PDF]
80 3OE8 3.10 Å 2010-10-27 human CXCR4 with the small ligand antagonist IT1t Wu, B.; Chien, E. Y.; Mol, C. D.; Fenalti, G.; Liu, W.; Katritch, V.; Abagyan, R.; Brooun, A.; Wells, P.; Bi, F. C.; Hamel, D. J.; Kuhn, P.; Handel, T. M.; Cherezov, V.; Stevens, R. C. Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists. Science 2010, 330, 1066 [Download PDF]
81 3OE9 3.10 Å 2010-10-27 human CXCR4 with the small ligand antagonist IT1t Wu, B.; Chien, E. Y.; Mol, C. D.; Fenalti, G.; Liu, W.; Katritch, V.; Abagyan, R.; Brooun, A.; Wells, P.; Bi, F. C.; Hamel, D. J.; Kuhn, P.; Handel, T. M.; Cherezov, V.; Stevens, R. C. Science 2010, 330, 1066 [Download PDF]
82 3ODU 2.50 Å 2010-10-27 human CXCR4 with the small ligand antagonist IT1t Wu, B.; Chien, E. Y.; Mol, C. D.; Fenalti, G.; Liu, W.; Katritch, V.; Abagyan, R.; Brooun, A.; Wells, P.; Bi, F. C.; Hamel, D. J.; Kuhn, P.; Handel, T. M.; Cherezov, V.; Stevens, R. C. Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists. Science 2010, 330, 1066 [Download PDF]
83 4RWS 3.1 Å 2015-02-11 CXCR4 and viral chemokine antagonist vMIP-II complex Qin L, Kufareva I, Holden LG, Wang C, Zheng Y, Zhao C, Fenalti G, Wu H, Han GW, Cherezov V, Abagyan R, Stevens RC, Handel TM. Science. 2015 Mar 6;347(6226):1117-22. [PubMed]
6, Human Dopamine Receptor 3 (D3R)
84 3PBL 2.89 Å 2010-11-03 human D3R with the antagonist eticlopride Chien, E. Y.; Liu, W.; Zhao, Q.; Katritch, V.; Han, G. W.; Hanson, M. A.; Shi, L.; Newman, A. H.; Javitch, J. A.; Cherezov, V.; Stevens, R. C. Structure of the Human Dopamine D3 Receptor in Complex with a D2/D3 Selective Antagonist. Science 2010, 330, 1091 [Download PDF]
7, Human Histamine receptor 1 (H1R)
85 3RZE 3.10 Å 2011-06-15 human H1R with the antagonist doxamine Shimamura, T.; Shiroishi, M.; Weyand, S.; Tsujimoto, H.; Winter, G.; Katritch, V.; Abagyan, R.; Cherezov, V.; Liu, W.; Han, G. W.; Kobayashi, T.; Stevens, R. C.; Iwata, S. Structure of the human histamine H1 receptor complex with doxepin. Nature 2011, 475, 65 [Download PDF]
8, Human M3 muscarinic acetylcholine receptor (CHRM3)
86 4DAJ 3.40 Å 2012-02-22 human M3 muscarinic acetylcholine receptor Kruse AC, Hu J, Pan AC, Arlow DH, Rosenbaum DM, Rosemond E, Green HF, Liu T, Chae PS, Dror RO, Shaw DE, Weis WI, Wess J, Kobilka BK. Structure and dynamics of the M3 muscarinic acetylcholine receptor. Nature. 2012 Feb 22;482(7386):552-6. doi: 10.1038/nature10867. [Download PDF]
87 4U14 3.57 Å 2014-11-26 rat M3 muscarinic acetylcholine receptor bound to the antagonist tiotropium crystallized with disulfide-stabilized T4 lysozyme T.S.THORSEN,R.A.MATT,W.I.WEIS,B.K.KOBILKA, Modified T4 lysozyme fusion proteins facilitate G protein-coupled receptor crystallogenesis, Structure 22: 1657-1664, 2014. [PubMed]
88 4U15 2.80 Å 2014-11-26 rat M3 muscarinic acetylcholine-mT4L receptor bound to tiotropium T.S.THORSEN,R.A.MATT,W.I.WEIS,B.K.KOBILKA, Modified T4 lysozyme fusion proteins facilitate G protein-coupled receptor crystallogenesis, Structure 22: 1657-1664, 2014. [PubMed]
89 4U16 3.70 Å 2014-11-26 rat M3 muscarinic acetylcholine-mT4L receptor bound to NMS T.S.THORSEN,R.A.MATT,W.I.WEIS,B.K.KOBILKA, Modified T4 lysozyme fusion proteins facilitate G protein-coupled receptor crystallogenesis, Structure 22: 1657-1664, 2014. [PubMed]
9, Human opioid receptor (OPRK1)
90 4DJH 2.90 Å 2012-03-21 human kappa opioid receptor with JDTic H. Wu, D. Wacker, M. Mileni, V. Katritch, G. W. Han, E. Vardy, W. Liu, A. A. Thompson, X. P. Huang, F. I. Carroll, S. W. Mascarella, R. B. Westkaemper, P. D. Mosier, B. L. Roth, V. Cherezov and R. C. Stevens (2012) Structure of the human kappa-opioid receptor in complex with JDTic. Nature 485: 327-332 [Download PDF]
91 4DKL 2.80 Å 2012-03-21 mu-opioid receptor bound to a morphinan antagonist Manglik A, Kruse AC, Kobilka TS, Thian FS, Mathiesen JM, Sunahara RK, Pardo L, Weis WI, Kobilka BK, Granier S. Crystal structure of the mu-opioid receptor bound to a morphinan antagonist. Nature. 2012 Mar 21;485(7398):321-6. [Download PDF]
92 4EJ4 3.40 Å 2012-05-16 delta opioid receptor bound to naltrindole Granier S, Manglik A, Kruse AC, Kobilka TS, Thian FS, Weis WI, Kobilka BK. Structure of the delta-opioid receptor bound to naltrindole.Nature. 2012 May 16;485(7398):400-4. [Download PDF]
93 4N6H 1.80 Å 2013-12-25 human delta opioid 7TM receptor Fenalti G, Giguere PM, Katritch V, Huang XP, Thompson AA, Cherezov V, Roth BL, Stevens RC, Molecular Control of delta-Opioid Receptor Signaling. Nature. 2014 Feb 13;506(7487):191-6 [PubMed]
94 4RWA 3.28 Å 2015-01-14 delta opioid receptor in complex with a bifunctional peptide Fenalti G, Zatsepin NA, Betti C, Giguere P, Han GW, Ishchenko A, Liu W, Guillemyn K, Zhang H, James D, Wang D, Weierstall U, Spence JC, Boutet S, Messerschmidt M, Williams GJ, Gati C, Yefanov OM, White TA, Oberthuer D, Metz M, Yoon CH, Barty A, Chapman HN, Basu S, Coe J, Conrad CE, Fromme R, Fromme P, Tourwé, Schiller PW, Roth BL, Ballet S, Katritch V, Stevens RC, Cherezov V. Nat Struct Mol Biol. 2015 Mar;22(3):265-8. [PubMed]
10, Human Nociceptin/orphanin FQ receptor (KOR3)
95 4EA3 3.01 Å 2012-04-25 nociceptin/orphanin FQ receptor with a peptide mimetic A. A. Thompson, W. Liu, E. Chun, V. Katritch, H. Wu, E. Vardy, X. P. Huang, C. Trapella, R. Guerrini, G. Calo, B. L. Roth, V. Cherezov and R. C. Stevens (2012) Structure of the nociceptin/orphanin FQ receptor in complex with a peptide mimetic. Nature 485: 395-399 [Download PDF]
11, Human protease-activated receptor 1 (PAR1)
96 3VW7 2.2 Å 2012-12-12 human protease-activated receptor 1 Zhang C, Srinivasan Y, Arlow DH, Fung JJ, Palmer D, Zheng Y, Green HF, Pandey A, Dror RO, Shaw DE, Weis WI, Coughlin SR, Kobilka BK (2012) High-resolution crystal structure of human protease-activated receptor 1. Nature. 492:387-92. [Download PDF]
12, Neurotensin receptor
97 4GRV 2.8 Å 2012-10-17 Neurotensin receptor White JF, Noinaj N, Shibata Y, Love J, Kloss B, Xu F, Gvozdenovic-Jeremic J, Shah P, Shiloach J, Tate CG, Grisshammer R. Structure of the agonist-bound neurotensin receptor. Nature. 2012 Oct 25;490(7421):508-13. [Download PDF]
98 3ZEV 3.00 Å 2014-01-29 thermostable agonist-bound neurotensin receptor 1 mutant without lysozyme fusion Egloff et al, Structure of signaling-competent neurotensin receptor 1 obtained by directed evolution in Escherichia coli. Proc Natl Acad Sci USA. 2014 Feb 11;111(6):E655-62 [PubMed]
99 4BUO 2.75 Å 2014-01-29 Thermostable Agonist-bound Neurotensin Receptor 1 Mutant without Lysozyme Fusion Egloff et al, Structure of signaling-competent neurotensin receptor 1 obtained by directed evolution in Escherichia coli. Proc Natl Acad Sci USA. 2014 Feb 11;111(6):E655-62 [PubMed]
100 4BV0 3.10 Å 2014-01-29 evolved agonist-bound neurotensin receptor 1 mutant without lysozyme fusion Egloff et al, Structure of signaling-competent neurotensin receptor 1 obtained by directed evolution in Escherichia coli. Proc Natl Acad Sci USA. 2014 Feb 11;111(6):E655-62 [PubMed]
101 4BWB 3.57 Å 2014-01-29 thermostable agonist-bound neurotensin receptor 1 mutant without lysozyme fusion Egloff et al, Structure of signaling-competent neurotensin receptor 1 obtained by directed evolution in Escherichia coli. Proc Natl Acad Sci USA. 2014 Feb 11;111(6):E655-62 [PubMed]
13, Human Chemokine receptor type 1 (CXCR1)
102 2LNL NMR Å 2012-10-17 human CXCR1 in phospholipid bilayers Park SH, Das BB, Casagrande F, Tian Y, Nothnagel HJ, Chu M, Kiefer H, Maier K, De Angelis AA, Marassi FM, Opella SJ. Structure of the chemokine receptor CXCR1 in phospholipid bilayers. Nature. 2012 Nov 29;491(7426):779-83. [Download PDF]
14, Human M2 muscarinic acetylcholine receptor (CHRM2)
103 3UON 3.00 Å 2012-02-01 human M2 muscarinic acetylcholine receptor bound to an antagonis Haga K, Kruse AC, Asada H, Yurugi-Kobayashi T, Shiroishi M, Zhang C, Weis WI, Okada T, Kobilka BK, Haga T, Kobayashi T. Structure of the human M2 muscarinic acetylcholine receptor bound to an antagonist. Nature. 2012 Jan 25;482(7386):547-51. [Download PDF]
104 4MQS 3.50 Å 2013-11-27 active human M2 muscarinic acetylcholine receptor bound to the agonist iperoxo Kruse AC, Ring AM, Manglik A, Hu J, Hu K, Eitel K, Hübner H, Pardon E, Valant C, Sexton PM, Christopoulos A, Felder CC, Gmeiner P, Steyaert J, Weis WI, Garcia KC, Wess J, Kobilka BK., Activation and allosteric modulation of a muscarinic acetylcholine receptor. Nature 2013; 504:101–106. [PubMed]
105 4MQT 3.70 Å 2013-11-27 active human M2 muscarinic acetylcholine receptor bound to the agonist iperoxo and allosteric modulator LY2119620 Kruse AC, Ring AM, Manglik A, Hu J, Hu K, Eitel K, Hübner H, Pardon E, Valant C, Sexton PM, Christopoulos A, Felder CC, Gmeiner P, Steyaert J, Weis WI, Garcia KC, Wess J, Kobilka BK., Activation and allosteric modulation of a muscarinic acetylcholine receptor. Nature 2013; 504:101–106. [PubMed]
15, Sphingosine 1-phosphate receptor
106 3V2W 3.35 Å 2012-02-15 sphingosine 1-phosphate receptor Hanson MA, Roth CB, Jo E, Griffith MT, Scott FL, Reinhart G, Desale H, Clemons B, Cahalan SM, Schuerer SC, Sanna MG, Han GW, Kuhn P, Rosen H, Stevens RC. Crystal structure of a lipid G protein-coupled receptor. Science. 2012 Feb 17;335(6070):851-5. [Download PDF]
107 3V2Y 2.80 Å 2012-02-15 sphingosine 1-phosphate receptor Hanson MA, Roth CB, Jo E, Griffith MT, Scott FL, Reinhart G, Desale H, Clemons B, Cahalan SM, Schuerer SC, Sanna MG, Han GW, Kuhn P, Rosen H, Stevens RC. Crystal structure of a lipid G protein-coupled receptor. Science. 2012 Feb 17;335(6070):851-5. [Download PDF]
16, Class B GPCR
108 4K5Y 2.98 Å 2013-07-17 class B GPCR corticotropin releasing factor receptor 1 Hollenstein K, Kean J, Bortolato A, Cheng RK, Dore AS, Jazayeri A, Cooke RM, Weir M, Marshall FH. Structure of class B GPCR corticotropin-releasing factor receptor 1. Nature. 2013 Jul 25;499(7459):438-43. [Download PDF]
109 4L6R 3.30 Å 2013-07-24 human glucagon class B G-protein-coupled receptor Siu FY, He M, de Graaf C, Han GW, Yang D, Zhang Z, Zhou C, Xu Q, Wacker D, Joseph JS, Liu W, Lau J, Cherezov V, Katritch V, Wang MW, Stevens RC. Structure of the human glucagon class B G-protein-coupled receptor. Nature. 2013 Jul 25;499(7459):444-9. [Download PDF]
17, human smoothened receptor (SMO)
110 4JKV 2.45 Å 2013-05-29 human smoothened 7TM receptor in complex with an antitumor agent Wang C, Wu H, Katritch V, Han GW, Huang XP, Liu W, Siu FY, Roth BL, Cherezov V, Stevens RC. Structure of the human smoothened receptor bound to an antitumour agent. Nature. 2013 May 16;497(7449):338-43. [Download PDF]
111 4N4W 2.80 Å 2014-01-22 human smoothened receptor in complex with SANT-1 Wang C, Wu H, Evron T, Vardy E, Han GW, Huang XP, Hufeisen SJ, Mangano TJ, Urban DJ, Katritch V, Cherezov V, Caron MG, Roth BL, Stevens RC. Structural basis for Smoothened receptor modulation and chemoresistance to anticancer drugs, Nat Commun. 2014 Jul 10;5:4355 [PubMed]
112 4O9R 3.20 Å 2014-03-05 human smoothened receptor structure in complex with cyclopamine Weierstall et al, Lipidic cubic phase injector facilitates membrane protein serial femtosecond crystallography. Nat Commun. 2014 Feb 14;5:3309. [PubMed]
113 4QIM 2.60 Å 2014-07-23 human smoothened receptor in complex with ANTA XV Wang C, Wu H, Evron T, Vardy E, Han GW, Huang XP, Hufeisen SJ, Mangano TJ, Urban DJ, Katritch V, Cherezov V, Caron MG, Roth BL, Stevens RC. Structural basis for Smoothened receptor modulation and chemoresistance to anticancer drugs, Nat Commun. 2014 Jul 10;5:4355 [PubMed]
114 4QIN 2.60 Å 2014-07-23 human smoothened receptor in complex with SAG1.5 Wang C, Wu H, Evron T, Vardy E, Han GW, Huang XP, Hufeisen SJ, Mangano TJ, Urban DJ, Katritch V, Cherezov V, Caron MG, Roth BL, Stevens RC. Structural basis for Smoothened receptor modulation and chemoresistance to anticancer drugs, Nat Commun. 2014 Jul 10;5:4355 [PubMed]
18, 5-hydroxytryptamine (5-HT) receptor
115 4IB4 2.70 Å 2013-03-13 chimeric protein of 5-HT2B-BRIL in complex with ergotamine Wacker D, Wang C, Katritch V, Han GW, Huang XP, Vardy E, McCorvy JD, Jiang Y, Chu M, Siu FY, Liu W, Xu HE, Cherezov V, Roth BL, Stevens RC. Structural features for functional selectivity at serotonin receptors. Science. 2013 May 3;340(6132):615-9. [Download PDF]
116 4IAR 2.70 Å 2013-03-13 chimeric protein of 5-HT1B-BRIL in complex with ergotamine Wang C, Jiang Y, Ma J, Wu H, Wacker D, Katritch V, Han GW, Liu W, Huang XP, Vardy E, McCorvy JD, Gao X, Zhou XE, Melcher K, Zhang C, Bai F, Yang H, Yang L, Jiang H, Roth BL, Cherezov V, Stevens RC, Xu HE. Structural basis for molecular recognition at serotonin receptors. Science. 2013 May 3;340(6132):610-4. [Download PDF]
117 4IAQ 2.80 Å 2013-03-13 chimeric protein of 5-HT1B-BRIL in complex with dihydroergotamine Wang C, Jiang Y, Ma J, Wu H, Wacker D, Katritch V, Han GW, Liu W, Huang XP, Vardy E, McCorvy JD, Gao X, Zhou XE, Melcher K, Zhang C, Bai F, Yang H, Yang L, Jiang H, Roth BL, Cherezov V, Stevens RC, Xu HE. Structural basis for molecular recognition at serotonin receptors. Science. 2013 May 3;340(6132):610-4. [Download PDF]
118 4NC3 2.80 Å 2013-12-18 5-HT2B receptor solved using serial femtosecond crystallography in lipidic cubic phase Liu W, Wacker D, Gati C, Han GW, James D, Wang D, Nelson G, Weierstall U, Katritch V, Barty A, Zatsepin NA, Li D, Messerschmidt M, Boutet S, Williams GJ, Koglin JE, Seibert MM, Wang C, Shah ST, Basu S, Fromme R, Kupitz C, Rendek KN, Grotjohann I, Fromme P, Kirian RA, Beyerlein KR, White TA, Chapman HN, Caffrey M, Spence JC, Stevens RC, Cherezov V. Serial femtosecond crystallography of G protein-coupled receptors. Science. 2013 Dec 20;342(6165):1521-4. [PubMed]
19, CCR5 Chemokine receptor
119 4MBS 2.71 Å 2013-09-11 CCR5 Chemokine Receptor Tan Q, Zhu Y, Li J, Chen Z, Han GW, Kufareva I, Li T, Ma L, Fenalti G, Li J, Zhang W, Xie X, Yang H, Jiang H, Cherezov V, Liu H, Stevens RC, Zhao Q, Wu B. Structure of the CCR5 chemokine receptor-HIV entry inhibitor maraviroc complex. Science. 2013 Sep 20;341(6152):1387-90. [Download PDF]
20, Class C G protein-coupled metabotropic glutamate receptor
120 4OR2 2.80 Å 2014-03-19 human class C G protein-coupled metabotropic glutamate receptor 1 Wu et al, Human class C G protein-coupled metabotropic glutamate receptor 1 in complex with a negative allosteric modulator. To be published, 2014. [PubMed]
121 4OO9 2.60 Å 2014-07-02 human class C GPCR metabotropic glutamate receptor 5 transmembrane domain Dore AS, Okrasa K, Patel JC, Serrano-Vega M, Bennett K, Cooke RM, Errey JC, Jazayeri A, Khan S, Tehan B, Weir M, Wiggin GR, Marshall FH. Structure of class C GPCR metabotropic glutamate receptor 5 transmembrane domain. Nature. 2014 Jul 31;511(7511):557-62 [PubMed]
21, P2Y purinoceptor 12 (P2Y12)
122 4NTJ 2.62 Å 2014-03-26 human P2Y12 receptor in complex with an antithrombotic drug Zhang K, Zhang J, Gao ZG, Zhang D, Zhu L, Han GW, Moss SM, Paoletta S, Kiselev E, Lu W, Fenalti G, Zhang W, Müller CE, Yang H, Jiang H, Cherezov V, Katritch V, Jacobson KA, Stevens RC, Wu B, Zhao Q. Structure of the human P2Y12 receptor in complex with an antithrombotic drug. Nature. 2014 May 1;509(7498):115-8 [PubMed]
123 4PXZ 2.50 Å 2014-04-30 P2Y12 receptor in complex with 2MeSADP Zhang J, Zhang K, Gao ZG, Paoletta S, Zhang D, Han GW, Li T, Ma L, Zhang W, Muller CE, Yang H, Jiang H, Cherezov V, Katritch V, Jacobson KA, Stevens RC, Wu B, Zhao Q. Agonist-bound structure of the human P2Y12 receptor. Nature. 2014 May 1;509(7498):119-22. [PubMed]
124 4PY0 3.10 Å 2014-04-30 P2Y12 receptor in complex with 2MeSATP Zhang J, Zhang K, Gao ZG, Paoletta S, Zhang D, Han GW, Li T, Ma L, Zhang W, Muller CE, Yang H, Jiang H, Cherezov V, Katritch V, Jacobson KA, Stevens RC, Wu B, Zhao Q. Agonist-bound structure of the human P2Y12 receptor. Nature. 2014 May 1;509(7498):119-22. [PubMed]
22, Free fatty acid receptor 1 (FFAR1)
125 4PHU 2.33 Å 2014-07-16 human GPR40 (FFAR1) bound to allosteric agonist TAK-875 Srivastava A, Yano J, Hirozane Y, Kefala G, Gruswitz F, Snell G, Lane W, Ivetac A, Aertgeerts K, Nguyen J, Jennings A, Okada K. High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875. Nature. 2014 Sep 4;513(7516):124-7 [PubMed]

References:

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