-
1
-
-
61649096359
-
G-protein-coupled receptor-focused drug discovery using a target class platform approach
-
Heilker R et al (2009) G-protein-coupled receptor-focused drug discovery using a target class platform approach. Drug Discov Today 14:231-240
-
(2009)
Drug Discov Today
, vol.14
, pp. 231-240
-
-
Heilker, R.1
-
2
-
-
66249144426
-
The structure and function of G-protein-coupled receptors
-
Rosenbaum DM, Rasmussen SGF, Kobilka BK (2009) The structure and function of G-protein-coupled receptors. Nature 459: 356-363
-
(2009)
Nature
, vol.459
, pp. 356-363
-
-
Rosenbaum, D.M.1
Sgf, R.2
Kobilka, B.K.3
-
3
-
-
67349250440
-
X-ray structure breakthroughs in the GPCR transmembrane region
-
Topiol S, Sabio M (2009) X-ray structure breakthroughs in the GPCR transmembrane region. Biochem Pharmacol 78:11-20
-
(2009)
Biochem Pharmacol
, vol.78
, pp. 11-20
-
-
Topiol, S.1
Sabio, M.2
-
4
-
-
78651390368
-
Cell signalling: Binding the receptor at both ends
-
Sprang SR (2011) Cell signalling: binding the receptor at both ends. Nature 469:172-173
-
(2011)
Nature
, vol.469
, pp. 172-173
-
-
Sprang, S.R.1
-
5
-
-
79954782236
-
Structure of an agonistbound human A2A adenosine receptor
-
Xu F et al (2011) Structure of an agonistbound human A2A adenosine receptor. Science 332(6027):322-327
-
(2011)
Science
, vol.332
, Issue.6027
, pp. 322-327
-
-
Xu, F.1
-
6
-
-
69049108756
-
Modern homology modeling of G-protein coupled receptors which structural template to use?
-
Mobarec JC, Sanchez R, Filizola M (2009) Modern homology modeling of G-protein coupled receptors: which structural template to use? J Med Chem 52:5207-5216
-
(2009)
J Med Chem
, vol.52
, pp. 5207-5216
-
-
Mobarec, J.C.1
Sanchez, R.2
Filizola, M.3
-
7
-
-
77954052042
-
Homology modeling of G-protein-coupled receptors with X-ray structures on the rise
-
Yarnitzky T, Levit A, Niv MY (2010) Homology modeling of G-protein-coupled receptors with X-ray structures on the rise. Curr Opin Drug Discov Devel 13:317-325
-
(2010)
Curr Opin Drug Discov Devel
, vol.13
, pp. 317-325
-
-
Yarnitzky, T.1
Levit, A.2
Niv, M.Y.3
-
8
-
-
71749086377
-
G Proteincoupled receptors: Target-based in silico screening
-
Senderowitz H, Marantz Y (2009) G Proteincoupled receptors: target-based in silico screening. Curr Pharm Des 15:4049-4068
-
(2009)
Curr Pharm des
, vol.15
, pp. 4049-4068
-
-
Senderowitz, H.1
Marantz, Y.2
-
9
-
-
71749112086
-
Customizing G Protein-coupled receptor models for structurebased virtual screening
-
de Graaf C, Rognan D (2009) Customizing G Protein-coupled receptor models for structurebased virtual screening. Curr Pharm Des 15: 4026-4048
-
(2009)
Curr Pharm des
, vol.15
, pp. 4026-4048
-
-
De Graaf, C.1
Rognan, D.2
-
10
-
-
69549096130
-
Molecular tuning of odorant receptors and its implication for odor signal processing
-
Reisert J, Restrepo D (2009) Molecular tuning of odorant receptors and its implication for odor signal processing. Chem Senses 34: 535-545
-
(2009)
Chem Senses
, vol.34
, pp. 535-545
-
-
Reisert, J.1
Restrepo, D.2
-
11
-
-
33751505567
-
The heterodimeric sweet taste receptor has multiple potential ligand binding sites
-
Cui M et al (2006) The heterodimeric sweet taste receptor has multiple potential ligand binding sites. Curr Pharm Des 12:4591-4600
-
(2006)
Curr Pharm des
, vol.12
, pp. 4591-4600
-
-
Cui, M.1
-
12
-
-
77954653331
-
Structural requirements of bitter taste receptor activation
-
Brockhoff A et al (2010) Structural requirements of bitter taste receptor activation. Proc Natl Acad Sci U S A 107:11110-11115
-
(2010)
Proc Natl Acad Sci U S A
, vol.107
, pp. 11110-11115
-
-
Brockhoff, A.1
-
13
-
-
42149181885
-
Structural diversity of G protein-coupled receptors and significance for drug discovery
-
Lagerstrom MC, Schioth HB (2008) Structural diversity of G protein-coupled receptors and significance for drug discovery. Nat Rev Drug Discov 7:339-357
-
(2008)
Nat Rev Drug Discov
, vol.7
, pp. 339-357
-
-
Lagerstrom, M.C.1
Schioth, H.B.2
-
14
-
-
58149183694
-
IUPHAR-DB: The IUPHAR database of G protein-coupled receptors and ion channels
-
Harmar AJ et al (2009) IUPHAR-DB: the IUPHAR database of G protein-coupled receptors and ion channels. Nucleic Acids Res 37:D680-D685
-
(2009)
Nucleic Acids Res
, vol.37
-
-
Harmar, A.J.1
-
15
-
-
2442548717
-
Positive and negative allosteric modulators of the Ca 2+ -sensing receptor interact within overlapping but not identical binding sites in the transmembrane domain
-
Petrel C et al (2004) Positive and negative allosteric modulators of the Ca 2+ -sensing receptor interact within overlapping but not identical binding sites in the transmembrane domain. J Biol Chem 279:18990-18997
-
(2004)
J Biol Chem
, vol.279
, pp. 18990-18997
-
-
Petrel, C.1
-
16
-
-
77955662759
-
Allosteric antagonist binding sites in class B GPCRs: Corticotropin receptor 1
-
Bhattacharya S et al (2010) Allosteric antagonist binding sites in class B GPCRs: corticotropin receptor 1. J Comput Aided Mol Des 24:659-674
-
(2010)
J Comput Aided Mol des
, vol.24
, pp. 659-674
-
-
Bhattacharya, S.1
-
17
-
-
34548671028
-
Modeling activated states of GPCRs: The rhodopsin template
-
Niv MY et al (2006) Modeling activated states of GPCRs: the rhodopsin template. J Comput Aided Mol Des 20:437-448
-
(2006)
J Comput Aided Mol des
, vol.20
, pp. 437-448
-
-
Niv, M.Y.1
-
18
-
-
41149141017
-
In fluence of oligomerization on the dynamics of G-proteincoupled receptors as assessed by normal mode analysis
-
Niv MY, Filizola M (2008) In fluence of oligomerization on the dynamics of G-proteincoupled receptors as assessed by normal mode analysis. Proteins 71:575-586
-
(2008)
Proteins
, vol.71
, pp. 575-586
-
-
Niv, M.Y.1
Filizola, M.2
-
19
-
-
66249129665
-
Evaluation of homology modeling of G-proteincoupled receptors in light of the A(2A) adenosine receptor crystallographic structure
-
Ivanov AA, Barak D, Jacobson KA (2009) Evaluation of homology modeling of G-proteincoupled receptors in light of the A(2A) adenosine receptor crystallographic structure. J Med Chem 52:3284-3292
-
(2009)
J Med Chem
, vol.52
, pp. 3284-3292
-
-
Ivanov, A.A.1
Barak, D.2
Jacobson, K.A.3
-
20
-
-
77955710004
-
Modulation of bitter taste perception by a small molecule hTAS2R antagonist
-
Slack JP et al (2010) Modulation of bitter taste perception by a small molecule hTAS2R antagonist. Curr Biol 20:1104-1109
-
(2010)
Curr Biol
, vol.20
, pp. 1104-1109
-
-
Slack, J.P.1
-
21
-
-
77957871915
-
Insights into the binding of phenyltiocarbamide (PTC) agonist to its target human TAS2R38 bitter receptor
-
Biarnes X et al (2010) Insights into the binding of phenyltiocarbamide (PTC) agonist to its target human TAS2R38 bitter receptor. PLoS One 5:e12394
-
(2010)
PLoS One
, vol.5
-
-
Biarnes, X.1
-
22
-
-
65549111760
-
Modeling small molecule-compound binding to G-protein-coupled receptors
-
Vaidehi N, Pease JE, Horuk R (2009) Modeling small molecule-compound binding to G-protein-coupled receptors. Methods Enzymol 460:263-288
-
(2009)
Methods Enzymol
, vol.460
, pp. 263-288
-
-
Vaidehi, N.1
Pease, J.E.2
Horuk, R.3
-
23
-
-
67650351973
-
Homology modeling of GPCRs
-
Simms J et al (2009) Homology modeling of GPCRs. Methods Mol Biol 552:97-113
-
(2009)
Methods Mol Biol
, vol.552
, pp. 97-113
-
-
Simms, J.1
-
24
-
-
74249106219
-
I-TASSER: Fully automated protein structure prediction in CASP8
-
Zhang Y (2009) I-TASSER: fully automated protein structure prediction in CASP8. Proteins 77(Suppl 9):100-113
-
(2009)
Proteins
, vol.77
, Issue.SUPPL 9
, pp. 100-113
-
-
Zhang, Y.1
-
25
-
-
77957055780
-
Integrated methods for the construction of three dimensional models and computational probing of structure function relations in G proteincoupled receptors
-
Ballesteros JA, Weinstein H (1995) Integrated methods for the construction of three dimensional models and computational probing of structure function relations in G proteincoupled receptors. Methods Neurosci 25: 366-428
-
(1995)
Methods Neurosci
, vol.25
, pp. 366-428
-
-
Ballesteros, J.A.1
Weinstein, H.2
-
26
-
-
38549164272
-
GLIDA: GPCR ligand database for chemical genomics drug discovery database and tools update
-
Okuno Y et al (2008) GLIDA: GPCR ligand database for chemical genomics drug discovery database and tools update. Nucleic Acids Res 36:D907-D912
-
(2008)
Nucleic Acids Res
, vol.36
-
-
Okuno, Y.1
-
27
-
-
77955249382
-
Mapping the druggable allosteric space of G-protein-coupled receptors: A fragment-based molecular dynamics approach
-
Ivetac A, McCammon JA (2010) Mapping the druggable allosteric space of G-protein-coupled receptors: a fragment-based molecular dynamics approach. Chem Biol Drug Des 76:201-217
-
(2010)
Chem Biol Drug des
, vol.76
, pp. 201-217
-
-
Ivetac, A.1
McCammon, J.A.2
-
28
-
-
0008600208
-
TinyGRAP database: A bioinformatics tool to mine G-proteincoupled receptor mutant data
-
Beukers MW et al (1999) TinyGRAP database: a bioinformatics tool to mine G-proteincoupled receptor mutant data. Trends Pharmacol Sci 20:475-477
-
(1999)
Trends Pharmacol Sci
, vol.20
, pp. 475-477
-
-
Beukers, M.W.1
-
29
-
-
1542400018
-
Automated extraction of mutation data from the literature: Application of MuteXt to G protein-coupled receptors and nuclear hormone receptors
-
Horn F, Lau AL, Cohen FE (2004) Automated extraction of mutation data from the literature: application of MuteXt to G protein-coupled receptors and nuclear hormone receptors. Bioinformatics 20:557-568
-
(2004)
Bioinformatics
, vol.20
, pp. 557-568
-
-
Horn, F.1
Lau, A.L.2
Cohen, F.E.3
-
30
-
-
43949095157
-
On the applicability of GPCR homology models to computer-aided drug discovery: A comparison between in silico and crystal structures of the beta2-adrenergic receptor
-
Costanzi S (2008) On the applicability of GPCR homology models to computer-aided drug discovery: a comparison between in silico and crystal structures of the beta2-adrenergic receptor. J Med Chem 51:2907-2914
-
(2008)
J Med Chem
, vol.51
, pp. 2907-2914
-
-
Costanzi, S.1
-
31
-
-
65049089399
-
Identifying conformational changes of the beta(2) adrenoceptor that enable accurate prediction of ligand/receptor interactions and screening for GPCR modulators
-
Reynolds KA, Katritch V, Abagyan R (2009) Identifying conformational changes of the beta(2) adrenoceptor that enable accurate prediction of ligand/receptor interactions and screening for GPCR modulators. J Comput Aided Mol Des 23:273-288
-
(2009)
J Comput Aided Mol des
, vol.23
, pp. 273-288
-
-
Reynolds, K.A.1
Katritch, V.2
Abagyan, R.3
-
32
-
-
18744394070
-
Q-SiteFinder: An energy-based method for the prediction of protein-ligand binding sites
-
Laurie AT, Jackson RM (2005) Q-SiteFinder: an energy-based method for the prediction of protein-ligand binding sites. Bioinformatics 21:1908-1916
-
(2005)
Bioinformatics
, vol.21
, pp. 1908-1916
-
-
Laurie, A.T.1
Jackson, R.M.2
-
33
-
-
36448995359
-
High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor
-
Cherezov V et al (2007) High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor. Science 318:1258-1265
-
(2007)
Science
, vol.318
, pp. 1258-1265
-
-
Cherezov, V.1
-
34
-
-
44649172481
-
A specific cholesterol binding site is established by the 2.8 A structure of the human beta2-adrenergic receptor
-
Hanson MA et al (2008) A specific cholesterol binding site is established by the 2.8 A structure of the human beta2-adrenergic receptor. Structure 16:897-905
-
(2008)
Structure
, vol.16
, pp. 897-905
-
-
Hanson, M.A.1
-
35
-
-
33749240615
-
Modeling the human PTC bitter-taste receptor interactions with bitter tastants
-
Floriano WB et al (2006) Modeling the human PTC bitter-taste receptor interactions with bitter tastants. J Mol Model 12:931-941
-
(2006)
J Mol Model
, vol.12
, pp. 931-941
-
-
Floriano, W.B.1
-
36
-
-
33845195004
-
Computational studies of ligand-receptor interactions in bitter taste receptors
-
Miguet L, Zhang Z, Grigorov MG (2006) Computational studies of ligand-receptor interactions in bitter taste receptors. J Recept Signal Transduct Res 26:611-630
-
(2006)
J Recept Signal Transduct Res
, vol.26
, pp. 611-630
-
-
Miguet, L.1
Zhang, Z.2
Grigorov, M.G.3
-
37
-
-
78651411166
-
Structure of a nanobody-stabilized active state of the beta (2) adrenoceptor
-
Rasmussen SG et al (2011) Structure of a nanobody-stabilized active state of the beta(2) adrenoceptor. Nature 469:175-180
-
(2011)
Nature
, vol.469
, pp. 175-180
-
-
Rasmussen, S.G.1
-
38
-
-
0037252680
-
GPCRDB information system for G protein-coupled receptors
-
Horn F et al (2003) GPCRDB information system for G protein-coupled receptors. Nucleic Acids Res 31:294-297
-
(2003)
Nucleic Acids Res
, vol.31
, pp. 294-297
-
-
Horn, F.1
-
39
-
-
0031552362
-
Development and validation of a genetic algorithm for flexible docking
-
Jones G et al (1997) Development and validation of a genetic algorithm for flexible docking. J Mol Biol 267:727-748
-
(1997)
J Mol Biol
, vol.267
, pp. 727-748
-
-
Jones, G.1
-
40
-
-
12144289984
-
Glide: A new approach for rapid, accurate docking and scoring. 1. Method and assessment of docking accuracy
-
Friesner RA et al (2004) Glide: a new approach for rapid, accurate docking and scoring. 1. Method and assessment of docking accuracy. J Med Chem 47:1739-1749
-
(2004)
J Med Chem
, vol.47
, pp. 1739-1749
-
-
Friesner, R.A.1
-
41
-
-
1642310340
-
Glide: A new approach for rapid, accurate docking and scoring. 2. Enrichment factors in database screening
-
Halgren TA et al (2004) Glide: a new approach for rapid, accurate docking and scoring. 2. Enrichment factors in database screening. J Med Chem 47:1750-1759
-
(2004)
J Med Chem
, vol.47
, pp. 1750-1759
-
-
Halgren, T.A.1
-
42
-
-
0037212102
-
LigandFit: A novel method for the shape-directed rapid docking of ligands to protein active sites
-
Venkatachalam CM et al (2003) LigandFit: a novel method for the shape-directed rapid docking of ligands to protein active sites. J Mol Graph Model 21:289-307
-
(2003)
J Mol Graph Model
, vol.21
, pp. 289-307
-
-
Venkatachalam, C.M.1
-
43
-
-
0041781898
-
Detailed analysis of gridbased molecular docking: A case study of CDOCKER-A CHARMm-based MD docking algorithm
-
Wu G et al (2003) Detailed analysis of gridbased molecular docking: a case study of CDOCKER-A CHARMm-based MD docking algorithm. J Comput Chem 24:1549-1562
-
(2003)
J Comput Chem
, vol.24
, pp. 1549-1562
-
-
Wu, G.1
-
44
-
-
0028922586
-
LIGPLOT: A program to generate schematic diagrams of protein-ligand interactions
-
Wallace AC, Laskowski RA, Thornton JM (1995) LIGPLOT: a program to generate schematic diagrams of protein-ligand interactions. Protein Eng 8:127-134
-
(1995)
Protein Eng
, vol.8
, pp. 127-134
-
-
Wallace, A.C.1
Laskowski, R.A.2
Thornton, J.M.3
-
45
-
-
0032957538
-
PCR-mediated recombination: A general method applied to construct chimeric infectious molecular clones of plasmaderived HIV-1 RNA
-
Fang G et al (1999) PCR-mediated recombination: a general method applied to construct chimeric infectious molecular clones of plasmaderived HIV-1 RNA. Nat Med 5:239-242
-
(1999)
Nat Med
, vol.5
, pp. 239-242
-
-
Fang, G.1
-
46
-
-
48249144782
-
Functions of human bitter taste receptors depend on N-glycosylation
-
Reichling C, Meyerhof W, Behrens M (2008) Functions of human bitter taste receptors depend on N-glycosylation. J Neurochem 106:1138-1148
-
(2008)
J Neurochem
, vol.106
, pp. 1138-1148
-
-
Reichling, C.1
Meyerhof, W.2
Behrens, M.3
-
47
-
-
11244259136
-
Molecular cloning and characterisation of DESC4, a new transmembrane serine protease
-
Behrens M et al (2004) Molecular cloning and characterisation of DESC4, a new transmembrane serine protease. Cell Mol Life Sci 61:2866-2877
-
(2004)
Cell Mol Life Sci
, vol.61
, pp. 2866-2877
-
-
Behrens, M.1
-
48
-
-
0024403619
-
Highresolution epitope mapping of hGH-receptor interactions by alanine-scanning mutagenesis
-
Cunningham BC, Wells JA (1989) Highresolution epitope mapping of hGH-receptor interactions by alanine-scanning mutagenesis. Science 244:1081-1085
-
(1989)
Science
, vol.244
, pp. 1081-1085
-
-
Cunningham, B.C.1
Wells, J.A.2
-
49
-
-
0042739015
-
Functional interaction between T2R taste receptors and G-protein alpha subunits expressed in taste receptor cells
-
Ueda T et al (2003) Functional interaction between T2R taste receptors and G-protein alpha subunits expressed in taste receptor cells. J Neurosci 23:7376-7380
-
(2003)
J Neurosci
, vol.23
, pp. 7376-7380
-
-
Ueda, T.1
-
50
-
-
0025216266
-
Inhibition of Fura-2 sequestration and secretion with organic anion transport blockers
-
Di Virgilio F, Steinberg TH, Silverstein SC (1990) Inhibition of Fura-2 sequestration and secretion with organic anion transport blockers. Cell Calcium 11:57-62
-
(1990)
Cell Calcium
, vol.11
, pp. 57-62
-
-
Di Virgilio, F.1
Steinberg, T.H.2
Silverstein, S.C.3
-
51
-
-
0036844351
-
The human TAS2R16 receptor mediates bitter taste in response to beta-glucopyranosides
-
Bufe B et al (2002) The human TAS2R16 receptor mediates bitter taste in response to beta-glucopyranosides. Nat Genet 32:397-401
-
(2002)
Nat Genet
, vol.32
, pp. 397-401
-
-
Bufe, B.1
-
52
-
-
2642511376
-
The human taste receptor hTAS2R14 responds to a variety of different bitter compounds
-
Behrens M et al (2004) The human taste receptor hTAS2R14 responds to a variety of different bitter compounds. Biochem Biophys Res Commun 319:479-485
-
(2004)
Biochem Biophys Res Commun
, vol.319
, pp. 479-485
-
-
Behrens, M.1
-
53
-
-
20844437913
-
Bitter taste receptors for saccharin and acesulfame K
-
Kuhn C et al (2004) Bitter taste receptors for saccharin and acesulfame K. J Neurosci 24:10260-10265
-
(2004)
J Neurosci
, vol.24
, pp. 10260-10265
-
-
Kuhn, C.1
-
54
-
-
77950896139
-
G protein coupled receptorsin silico drug discovery and design
-
Sela I et al (2010) G protein coupled receptorsin silico drug discovery and design. Curr Top Med Chem 10:638-656
-
(2010)
Curr Top Med Chem
, vol.10
, pp. 638-656
-
-
Sela, I.1
-
55
-
-
34547802810
-
Broad tuning of the human bitter taste receptor hTAS2R46 to various sesquiterpene lactones, clerodane and labdane diterpenoids, strychnine, and denatonium
-
Brockhoff A et al (2007) Broad tuning of the human bitter taste receptor hTAS2R46 to various sesquiterpene lactones, clerodane and labdane diterpenoids, strychnine, and denatonium. J Agric Food Chem 55:6236-6243
-
(2007)
J Agric Food Chem
, vol.55
, pp. 6236-6243
-
-
Brockhoff, A.1
-
56
-
-
41149156578
-
Molecular modeling of the second extracellular loop of G-protein coupled receptors and its implication on structurebased virtual screening
-
de Graaf C et al (2008) Molecular modeling of the second extracellular loop of G-protein coupled receptors and its implication on structurebased virtual screening. Proteins 71:599-620
-
(2008)
Proteins
, vol.71
, pp. 599-620
-
-
De Graaf, C.1
-
57
-
-
0347717582
-
The second extracellular loop of the dopamine D2 receptor lines the binding-site crevice
-
Shi L, Javitch JA (2004) The second extracellular loop of the dopamine D2 receptor lines the binding-site crevice. Proc Natl Acad Sci U S A 101:440-445
-
(2004)
Proc Natl Acad Sci U S A
, vol.101
, pp. 440-445
-
-
Shi, L.1
Javitch, J.A.2
-
58
-
-
58849094130
-
Topology of class A G protein-coupled receptors: Insights gained from crystal structures of rhodopsins, adrenergic and adenosine receptors
-
MustafiD, Palczewski K (2009) Topology of class A G protein-coupled receptors: insights gained from crystal structures of rhodopsins, adrenergic and adenosine receptors. Mol Pharmacol 75:1-12
-
(2009)
Mol Pharmacol
, vol.75
, pp. 1-12
-
-
Mustafi, D.1
Palczewski, K.2
-
59
-
-
73849149844
-
Ligand-specific regulation of the extracellular surface of a G-proteincoupled receptor
-
Bokoch MP et al (2010) Ligand-specific regulation of the extracellular surface of a G-proteincoupled receptor. Nature 463:108-112
-
(2010)
Nature
, vol.463
, pp. 108-112
-
-
Bokoch, M.P.1
-
60
-
-
59649112109
-
Helix movement is coupled to displacement of the second extracellular loop in rhodopsin activation
-
Ahuja S et al (2009) Helix movement is coupled to displacement of the second extracellular loop in rhodopsin activation. Nat Struct Mol Biol 16:168-175
-
(2009)
Nat Struct Mol Biol
, vol.16
, pp. 168-175
-
-
Ahuja, S.1
-
61
-
-
0036169280
-
The binding site of aminergic G protein-coupled receptors: The transmembrane segments and second extracellular loop
-
Shi L, Javitch JA (2002) The binding site of aminergic G protein-coupled receptors: the transmembrane segments and second extracellular loop. Annu Rev Pharmacol Toxicol 42:437-467
-
(2002)
Annu Rev Pharmacol Toxicol
, vol.42
, pp. 437-467
-
-
Shi, L.1
Javitch, J.A.2
-
62
-
-
52949146798
-
Identification of Tyr(290(6.58)) of the human gonadotropinreleasing hormone (GnRH) receptor as a contact residue for both GnRH i and GnRH II: Importance for high-affinity binding and receptor activation
-
Coetsee M et al (2008) Identification of Tyr(290(6.58)) of the human gonadotropinreleasing hormone (GnRH) receptor as a contact residue for both GnRH I and GnRH II: importance for high-affinity binding and receptor activation. Biochemistry 47:10305-10313
-
(2008)
Biochemistry
, vol.47
, pp. 10305-10313
-
-
Coetsee, M.1
-
63
-
-
8544242989
-
Identification of ligands for two human bitter T2R receptors
-
Pronin AN et al (2004) Identification of ligands for two human bitter T2R receptors. Chem Senses 29:583-593
-
(2004)
Chem Senses
, vol.29
, pp. 583-593
-
-
Pronin, A.N.1
-
64
-
-
77956243395
-
Characterization of the beta-D-glucopyranoside binding site of the human bitter taste receptor hTAS2R16
-
Sakurai T et al (2010) Characterization of the beta-D-glucopyranoside binding site of the human bitter taste receptor hTAS2R16. J Biol Chem 285(36):28373-28378
-
(2010)
J Biol Chem
, vol.285
, Issue.36
, pp. 28373-28378
-
-
Sakurai, T.1
-
65
-
-
66849115400
-
Elucidation of binding sites of dual antagonists in the human chemokine receptors CCR2 and CCR5
-
Hall SE et al (2009) Elucidation of binding sites of dual antagonists in the human chemokine receptors CCR2 and CCR5. Mol Pharmacol 75:1325-1336
-
(2009)
Mol Pharmacol
, vol.75
, pp. 1325-1336
-
-
Hall, S.E.1
-
66
-
-
77955779227
-
Conserved binding mode of human beta2 adrenergic receptor inverse agonists and antagonist revealed by X-ray crystallography
-
Wacker D et al (2010) Conserved binding mode of human beta2 adrenergic receptor inverse agonists and antagonist revealed by X-ray crystallography. J Am Chem Soc 132:11443-11445
-
(2010)
J Am Chem Soc
, vol.132
, pp. 11443-11445
-
-
Wacker, D.1
-
67
-
-
56749103466
-
The 2.6 Angstrom crystal structure of a human A2A adenosine receptor bound to an antagonist
-
Jaakola V-P et al (2008) The 2.6 Angstrom crystal structure of a human A2A adenosine receptor bound to an antagonist. Science 322:1211-1217
-
(2008)
Science
, vol.322
, pp. 1211-1217
-
-
Jaakola, V.-P.1
-
68
-
-
36349016730
-
Roof and floor of the muscarinic binding pocket: Variations in the binding modes of orthosteric ligands
-
Goodwin JA et al (2007) Roof and floor of the muscarinic binding pocket: variations in the binding modes of orthosteric ligands. Mol Pharmacol 72:1484-1496
-
(2007)
Mol Pharmacol
, vol.72
, pp. 1484-1496
-
-
Goodwin, J.A.1
-
69
-
-
77952356281
-
Evolution-guided discovery and recoding of allosteric pathway specificity determinants in psychoactive bioamine receptors
-
Rodriguez GJ et al (2010) Evolution-guided discovery and recoding of allosteric pathway specificity determinants in psychoactive bioamine receptors. Proc Natl Acad Sci U S A 107:7787-7792
-
(2010)
Proc Natl Acad Sci U S A
, vol.107
, pp. 7787-7792
-
-
Rodriguez, G.J.1
-
70
-
-
67650753759
-
Definition of the G protein-coupled receptor transmembrane bundle binding pocket and calculation of receptor similarities for drug design
-
Gloriam DE et al (2009) Definition of the G protein-coupled receptor transmembrane bundle binding pocket and calculation of receptor similarities for drug design. J Med Chem 52:4429-4442
-
(2009)
J Med Chem
, vol.52
, pp. 4429-4442
-
-
Gloriam, D.E.1
-
71
-
-
85027927015
-
Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists
-
Wu B et al (2010) Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists. Science 330: 1066-1071
-
(2010)
Science
, vol.330
, pp. 1066-1071
-
-
Wu, B.1
-
72
-
-
78651405537
-
The structural basis for agonist and partial agonist action on a beta (1)-adrenergic receptor
-
Warne T et al (2011) The structural basis for agonist and partial agonist action on a beta(1)-adrenergic receptor. Nature 469:241-244
-
(2011)
Nature
, vol.469
, pp. 241-244
-
-
Warne, T.1
-
73
-
-
78449305788
-
Structure of the human dopamine D3 receptor in complex with a D2/ D3 selective antagonist
-
Chien EY et al (2010) Structure of the human dopamine D3 receptor in complex with a D2/ D3 selective antagonist. Science 330:1091-1095
-
(2010)
Science
, vol.330
, pp. 1091-1095
-
-
Chien, E.Y.1
-
74
-
-
77951244300
-
Ligand binding and subtype selectivity of the human A(2A) adenosine receptor: Identification and characterization of essential amino acid residues
-
Jaakola VP et al (2010) Ligand binding and subtype selectivity of the human A(2A) adenosine receptor: identification and characterization of essential amino acid residues. J Biol Chem 285:13032-13044
-
(2010)
J Biol Chem
, vol.285
, pp. 13032-13044
-
-
Jaakola, V.P.1
-
75
-
-
70350362562
-
A G protein-coupled receptor at work: The rhodopsin model
-
Hofmann KP et al (2009) A G protein-coupled receptor at work: the rhodopsin model. Trends Biochem Sci 34:540-552
-
(2009)
Trends Biochem Sci
, vol.34
, pp. 540-552
-
-
Hofmann, K.P.1
-
76
-
-
50249156843
-
Selective structure-based virtual screening for full and partial agonists of the beta2 adrenergic receptor
-
de Graaf C, Rognan D (2008) Selective structure-based virtual screening for full and partial agonists of the beta2 adrenergic receptor. J Med Chem 51:4978-4985
-
(2008)
J Med Chem
, vol.51
, pp. 4978-4985
-
-
De Graaf, C.1
Rognan, D.2
-
77
-
-
78349305715
-
Dynamics and flexibility of G-protein-coupled receptor conformations and their relevance to drug design
-
Vaidehi N (2010) Dynamics and flexibility of G-protein-coupled receptor conformations and their relevance to drug design. Drug Discov Today 15(21-22):951-957
-
(2010)
Drug Discov Today
, vol.15
, Issue.21-22
, pp. 951-957
-
-
Vaidehi, N.1
-
78
-
-
77950823494
-
Computational mapping of the conformational transitions in agonist selective pathways of a G-protein coupled receptor
-
Bhattacharya S, Vaidehi N (2010) Computational mapping of the conformational transitions in agonist selective pathways of a G-protein coupled receptor. J Am Chem Soc 132: 5205-5214
-
(2010)
J Am Chem Soc
, vol.132
, pp. 5205-5214
-
-
Bhattacharya, S.1
Vaidehi, N.2
-
79
-
-
77956638608
-
Putative active states of a prototypic g-protein-coupled receptor from biased molecular dynamics
-
Provasi D, Filizola M (2010) Putative active states of a prototypic g-protein-coupled receptor from biased molecular dynamics. Biophys J 98:2347-2355
-
(2010)
Biophys J
, vol.98
, pp. 2347-2355
-
-
Provasi, D.1
Filizola, M.2
-
80
-
-
77956329606
-
Investigation of the histamine H3 receptor binding site. Design and synthesis of hybrid agonists with a lipophilic side chain
-
Ishikawa M et al (2010) Investigation of the histamine H3 receptor binding site. Design and synthesis of hybrid agonists with a lipophilic side chain. J Med Chem 53:6445-6456
-
(2010)
J Med Chem
, vol.53
, pp. 6445-6456
-
-
Ishikawa, M.1
-
81
-
-
0037192858
-
Evidence for a model of agonist-induced activation of 5-hydroxytryptamine 2A serotonin receptors that involves the disruption of a strong ionic interaction between helices 3 and 6
-
Shapiro DA et al (2002) Evidence for a model of agonist-induced activation of 5-hydroxytryptamine 2A serotonin receptors that involves the disruption of a strong ionic interaction between helices 3 and 6. J Biol Chem 277:11441-11449
-
(2002)
J Biol Chem
, vol.277
, pp. 11441-11449
-
-
Shapiro, D.A.1
-
82
-
-
0030796011
-
Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors
-
Jiang Q et al (1997) Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors. J Med Chem 40: 2588-2595
-
(1997)
J Med Chem
, vol.40
, pp. 2588-2595
-
-
Jiang, Q.1
-
83
-
-
0029043501
-
Site-directed mutagenesis identifies residues involved in ligand recognition in the human A2a adenosine receptor
-
Kim J et al (1995) Site-directed mutagenesis identifies residues involved in ligand recognition in the human A2a adenosine receptor. J Biol Chem 270:13987-13997
-
(1995)
J Biol Chem
, vol.270
, pp. 13987-13997
-
-
Kim, J.1
-
84
-
-
77955191993
-
Structural insights into conformational stability of wild-type and mutant beta1-adrenergic receptor
-
Balaraman GS, Bhattacharya S, Vaidehi N (2010) Structural insights into conformational stability of wild-type and mutant beta1-adrenergic receptor. Biophys J 99:568-577
-
(2010)
Biophys J
, vol.99
, pp. 568-577
-
-
Balaraman, G.S.1
Bhattacharya, S.2
Vaidehi, N.3
-
85
-
-
76249122268
-
An ensemble view of allostery
-
Hilser VJ (2010) An ensemble view of allostery. Science 327:653-654
-
(2010)
Science
, vol.327
, pp. 653-654
-
-
Hilser, V.J.1
-
86
-
-
67349088738
-
Community-wide assessment of GPCR structure modelling and ligand docking: GPCR Dock 2008
-
Michino M et al (2009) Community-wide assessment of GPCR structure modelling and ligand docking: GPCR Dock 2008. Nat Rev Drug Discov 8:455-463
-
(2009)
Nat Rev Drug Discov
, vol.8
, pp. 455-463
-
-
Michino, M.1
-
87
-
-
80051521545
-
Status of GPCR modeling and docking as re flected by communitywide GPCR dock 2010 Assessment
-
Kufareva I et al (2011) Status of GPCR modeling and docking as re flected by communitywide GPCR dock 2010 Assessment, Structure 19:1108-1126
-
(2011)
Structure
, vol.19
, pp. 1108-1126
-
-
Kufareva, I.1
-
88
-
-
84865228105
-
New insights for drug design from the X-ray crystallographic structures of GPCRs
-
doi:10.1124/mol.112.079335
-
Jacobson KA and Costanzi S (2012) New insights for drug design from the X-ray crystallographic structures of GPCRs. Mol Pharmacol doi:10.1124/mol.112. 079335 Forschungsgemeinschaft Forschungsgemeinschaft
-
(2012)
Mol Pharmacol
-
-
Jacobson, K.A.1
Costanzi, S.2
|