Glycoprotein Hormone Receptors - TSHR, FSHR, LHCGR (LHR)

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Hormones

Hormones

Jiang X, Liu H, Chen X, Chen PH, Fischer D, Sriraman V, Yu HN, Arkinstall S, He X
Structure of follicle-stimulating hormone in complex with the entire ectodomain of its receptor.
Proc Natl Acad Sci U S A. 2012 Jul 31;109(31):12491-6.
PDB: 4AY9

Fan QR, Hendrickson WA
Structure of human follicle-stimulating hormone in complex with its receptor.
Nature. 2005 Jan 20;433(7023):269-77.
PDB: 1XWD

Fox KM, Dias JA, Van Roey P
Three-dimensional structure of human follicle-stimulating hormone
Mol Endocrinol. 2001 Mar;15(3):378-89
PDB: 1FL7

Tegoni M, Spinelli S, Verhoeyen M, Davis P, Cambillau C
Crystal structure of a ternary complex between human chorionic gonadotropin (hCG) and two Fv fragments specific for the alpha and beta-subunits
J Mol Biol. 1999 Jun 25;289(5):1375-85
PDB: 1QFW

Lapthorn AJ, Harris DC, Littlejohn A, Lustbader JW, Canfield RE, Machin KJ, Morgan FJ, Isaacs NW
Crystal structure of human chorionic gonadotropin
Nature. 1994 Jun 9;369(6480):455-61
PDB: 1HRP

Serpentine domain (Rhodopsin)

Serpentine domain (Rhodopsin)

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. v372 pp. 1179, 2007
PDB: 2J4Y

Salom, D., Lodowski, D.T., Stenkamp, R.E., Trong, I.L., Golczak, M., Jastrzebska, B., Harris, T., Ballesteros, J.A., Palczewski, K
Crystal structure of a photoactivated deprotonated intermediate of rhodopsin.
Proc.Natl.Acad.Sci.Usa v103 pp. 16123-16128, 2006
PDB: 2I35

Okada T, Sugihara M, Bondar AN, 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 Sep 10;342(2):571-83
PDB: 1U19

Li J, Edwards PC, Burghammer M, Villa C, Schertler GF
Structure of bovine rhodopsin in a trigonal crystal form
J Mol Biol. 2004 Nov 5;343(5):1409-38
PDB: 1GZM

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 v40 pp. 7761-7772, 2001
PDB: 1HZX

Palczewski K, Kumasaka T, Hori T, Behnke CA, Motoshima H, Fox BA, Le Trong I, Teller DC, Okada T, Stenkamp RE, Yamamoto M, Miyano M
Crystal structure of rhodopsin: A G protein-coupled receptor
Science. 2000 Aug 4;289(5480):739-45
PDB: 1F88

Serpentine domain (Metarhodopsin II)

Serpentine domain (Metarhodopsin II)

Choe HW, Kim YJ, Park JH, Morizumi T, Pai EF, Krauss N, Hofmann KP, Scheerer P, Ernst OP
Crystal structure of metarhodopsin II.
Nature. 2011 Mar 31;471(7340):651-5.
PDB: 3PQR

Choe HW, Kim YJ, Park JH, Morizumi T, Pai EF, Krauss N, Hofmann KP, Scheerer P, Ernst OP
Crystal structure of metarhodopsin II.
Nature. 2011 Mar 31;471(7340):651-5.
PDB: 3PXO

Serpentine domain (Opsin)

Serpentine domain (Opsin)

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
(2008) Nature 455: 497-502
PDB: 3DQB

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
(2008) Nature 454: 183-187
PDB: 3CAP

Serpentine domain (Adenosine receptor)

Serpentine domain (Adenosine receptor)

Lebon G, Warne T, Edwards PC, Bennett K, Langmead CJ, Leslie AG, Tate CG
Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation.
Nature. 2011 May 18;474(7352):521-5.
PDB: 2YDV

Lebon G, Warne T, Edwards PC, Bennett K, Langmead CJ, Leslie AG, Tate CG
Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation.
Nature. 2011 May 18;474(7352):521-5.
PDB: 2YDO

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
(2008) Science 322: 1211-1217
PDB: 3EML

Serpentine domain (beta(1)-adrenergic receptor)

Serpentine domain (beta(1)-adrenergic receptor)

Moukhametzianov R, Warne T, Edwards PC, Serrano-Vega MJ, Leslie AG, Tate CG, Schertler GF
Two distinct conformations of helix 6 observed in antagonist-bound structures of a beta1-adrenergic receptor.
Proc Natl Acad Sci U S A. 2011 May 17;108(20):8228-32.
PDB: 2YCX

Warne T, Moukhametzianov R, Baker JG, Nehmé R, Edwards PC, Leslie AG, Schertler GF, Tate CG
The structural basis for agonist and partial agonist action on a β(1)-adrenergic receptor.
Nature. 2011 Jan 13;469(7329):241-4.
PDB: 2Y02

Moukhametzianov R, Warne T, Edwards PC, Serrano-Vega MJ, Leslie AG, Tate CG, Schertler GF
Two distinct conformations of helix 6 observed in antagonist-bound structures of a beta1-adrenergic receptor.
Proc Natl Acad Sci U S A. 2011 May 17;108(20):8228-32.
PDB: 2YCZ

Warne T, Moukhametzianov R, Baker JG, Nehmé R, Edwards PC, Leslie AG, Schertler GF, Tate CG
The structural basis for agonist and partial agonist action on a β(1)-adrenergic receptor.
Nature. 2011 Jan 13;469(7329):241-4.
PDB: 2Y04

Warne T, Moukhametzianov R, Baker JG, Nehmé R, Edwards PC, Leslie AG, Schertler GF, Tate CG
The structural basis for agonist and partial agonist action on a β(1)-adrenergic receptor.
Nature. 2011 Jan 13;469(7329):241-4.
PDB: 2Y01

Warne T, Moukhametzianov R, Baker JG, Nehmé R, Edwards PC, Leslie AG, Schertler GF, Tate CG
The structural basis for agonist and partial agonist action on a β(1)-adrenergic receptor.
Nature. 2011 Jan 13;469(7329):241-4.
PDB: 2Y00

Moukhametzianov R, Warne T, Edwards PC, Serrano-Vega MJ, Leslie AG, Tate CG, Schertler GF
Two distinct conformations of helix 6 observed in antagonist-bound structures of a beta1-adrenergic receptor.
Proc Natl Acad Sci U S A. 2011 May 17;108(20):8228-32.
PDB: 2YCY

Warne T, Moukhametzianov R, Baker JG, Nehmé R, Edwards PC, Leslie AG, Schertler GF, Tate CG
The structural basis for agonist and partial agonist action on a β(1)-adrenergic receptor.
Nature. 2011 Jan 13;469(7329):241-4.
PDB: 2Y03

Moukhametzianov R, Warne T, Edwards PC, Serrano-Vega MJ, Leslie AG, Tate CG, Schertler GF
Two distinct conformations of helix 6 observed in antagonist-bound structures of a beta1-adrenergic receptor.
Proc Natl Acad Sci U S A. 2011 May 17;108(20):8228-32.
PDB: 2YCW

Warne, A., Serrano-Vega, M.J., Baker, J.G., Moukhametzianov, R., Edwards, P.C., Henderson, R., Leslie, A.G.W., Tate, C.G., Schertler, G.F.X.
Structure of the Beta1-Adrenergic G Protein-Coupled Receptor
(2008) Nature 454: 486
PDB: 2VT4

Serpentine domain (beta(2)-adrenergic receptor)

Serpentine domain (beta(2)-adrenergic receptor)

Rosenbaum DM, Zhang C, Lyons JA, Holl R, Aragao D, Arlow DH, Rasmussen SG, Choi HJ, Devree BT, Sunahara RK, Chae PS, Gellman SH, Dror RO, Shaw DE, Weis WI, Caffrey M, Gmeiner P, Kobilka BK
Structure and function of an irreversible agonist-β(2) adrenoceptor complex.
Nature. 2011 Jan 13;469(7329):236-40.
PDB: 3PDS

Rasmussen SG, Choi HJ, Fung JJ, Pardon E, Casarosa P, Chae PS, Devree BT, Rosenbaum DM, Thian FS, Kobilka TS, Schnapp A, Konetzki I, Sunahara RK, Gellman SH, Pautsch A, Steyaert J, Weis WI, Kobilka BK
Structure of a nanobody-stabilized active state of the β(2) adrenoceptor.
Nature. 2011 Jan 13;469(7329):175-80.
PDB: 3P0G

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 beta(2) adrenergic G-protein-coupled receptor.
Nature, 2007
PDB: 2R4R

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 {beta}2-Adrenergic G Protein Coupled Receptor.
Science, 2007
PDB: 2RH1

Serpentine domain (Chemokine receptor)

Serpentine domain (Chemokine receptor)

Wu B, Chien EY, Mol CD, Fenalti G, Liu W, Katritch V, Abagyan R, Brooun A, Wells P, Bi FC, Hamel DJ, Kuhn P, Handel TM, Cherezov V, Stevens RC
Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists.
Science. 2010 Nov 19;330(6007):1066-71.
PDB: 3ODU

Wu B, Chien EY, Mol CD, Fenalti G, Liu W, Katritch V, Abagyan R, Brooun A, Wells P, Bi FC, Hamel DJ, Kuhn P, Handel TM, Cherezov V, Stevens RC
Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists.
Science. 2010 Nov 19;330(6007):1066-71.
PDB: 3OE8

Wu B, Chien EY, Mol CD, Fenalti G, Liu W, Katritch V, Abagyan R, Brooun A, Wells P, Bi FC, Hamel DJ, Kuhn P, Handel TM, Cherezov V, Stevens RC
Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists.
Science. 2010 Nov 19;330(6007):1066-71.
PDB: 3OE0

Wu B, Chien EY, Mol CD, Fenalti G, Liu W, Katritch V, Abagyan R, Brooun A, Wells P, Bi FC, Hamel DJ, Kuhn P, Handel TM, Cherezov V, Stevens RC
Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists.
Science. 2010 Nov 19;330(6007):1066-71.
PDB: 3OE6

Wu B, Chien EY, Mol CD, Fenalti G, Liu W, Katritch V, Abagyan R, Brooun A, Wells P, Bi FC, Hamel DJ, Kuhn P, Handel TM, Cherezov V, Stevens RC
Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists.
Science. 2010 Nov 19;330(6007):1066-71.
PDB: 3OE9

Serpentine domain (Dopamine receptor)

Serpentine domain (Dopamine receptor)

Chien EY, Liu W, Zhao Q, Katritch V, Han GW, Hanson MA, Shi L, Newman AH, Javitch JA, Cherezov V, Stevens RC
Structure of the human dopamine D3 receptor in complex with a D2/D3 selective antagonist.
Science. 2010 Nov 19;330(6007):1091-5.
PDB: 3PBL

Structure of the GPHR Leucine-rich repeat domain in complex with different ligands

Structure of the GPHR Leucine-rich repeat domain in complex with different ligands

Jiang X, Liu H, Chen X, Chen PH, Fischer D, Sriraman V, Yu HN, Arkinstall S, He X
Structure of follicle-stimulating hormone in complex with the entire ectodomain of its receptor.
Proc Natl Acad Sci U S A. 2012 Jul 31;109(31):12491-6.
PDB: 4AY9

Sanders P, Young S, Sanders J, Kabelis K, Baker S, Sullivan A, Evans M, Clark J, Wilmot J, Hu X, Roberts E, Powell M, Núñez Miguel R, Furmaniak J, Rees Smith B
Crystal structure of the TSH receptor (TSHR) bound to a blocking-type TSHR autoantibody.
J Mol Endocrinol. 2011;46(2):81-99.
PDB: 2XWT

Sanders, J., Chirgadze, D.Y., Sanders, P., Baker, S., Sullivan, A., Bhardwaja, A., Bolton, J., Reeve, M., Nakatake, N., Evans, M., Richards, T., Powell, M., Miguel, R.N., Blundell, T.L., Furmaniak, J., Smith, B.R.
Crystal structure of the TSH receptor in complex with a thyroid-stimulating autoantibody
Thyroid. 2007 May;17(5):395-410.
PDB: 3G04

Fan QR, Hendrickson WA
Structure of human follicle-stimulating hormone in complex with its receptor
Nature. 2005 Jan 20;433(7023):269-77
PDB: 1XWD

G-Proteins (Gi, Gs)

G-Proteins (Gi, Gs)

Sunahara, R. K., Tesmer, J. J., Gilman, A. G., Sprang, S. R.
Crystal structure of the adenylyl cyclase activator Gsalpha
Science 278 pp. 1943 (1997)
PDB: 1AZT

Wall, M. A., Coleman, D. E., Lee, E., Iniguez-Lluhi, J. A., Posner, B. A., Gilman, A. G., Sprang, S. R.
The structure of the G protein heterotrimer Gi alpha 1 beta 1 gamma 2
Cell 83 pp. 1047 (1995)
PDB: 1GP2

Wall, M. A., Coleman, D. E., Lee, E., Iniguez-Lluhi, J. A., Posner, B. A., Gilman, A. G., Sprang, S. R.
The structure of the G protein heterotrimer Gi alpha 1 beta 1 gamma 2
Cell 83 pp. 1047 (1995)
PDB: 1GG2