-
1
-
-
42149181885
-
Structural diversity of G protein-coupled receptors and significance for drug discovery
-
Lagerström, M. C.; Schiöth, H. B. Structural diversity of G protein-coupled receptors and significance for drug discovery Nature Rev. Drug Discovery 2008, 7, 339-357
-
(2008)
Nature Rev. Drug Discovery
, vol.7
, pp. 339-357
-
-
Lagerström, M.C.1
Schiöth, H.B.2
-
2
-
-
0036258990
-
G Protein-receptor coupling allosterism and complexing
-
Christopoulos, A.; Kenakin, T. G Protein-receptor coupling allosterism and complexing Pharmacol. Rev. 2002, 54, 323-374
-
(2002)
Pharmacol. Rev.
, vol.54
, pp. 323-374
-
-
Christopoulos, A.1
Kenakin, T.2
-
3
-
-
0036490942
-
Allosteric binding sites on cell-surface receptors: Novel targets for drug discovery
-
Christopoulos, A. Allosteric binding sites on cell-surface receptors: novel targets for drug discovery Nature Rev. Drug Discovery 2002, 1, 198-210
-
(2002)
Nature Rev. Drug Discovery
, vol.1
, pp. 198-210
-
-
Christopoulos, A.1
-
4
-
-
33847122495
-
Allosteric modulation of G protein-coupled receptors
-
May, L. T.; Leach, K.; Sexton, P. M.; Christopoulos, A. Allosteric modulation of G protein-coupled receptors Annu. Rev. Pharmacol. Toxicol. 2007, 47, 1-51
-
(2007)
Annu. Rev. Pharmacol. Toxicol.
, vol.47
, pp. 1-51
-
-
May, L.T.1
Leach, K.2
Sexton, P.M.3
Christopoulos, A.4
-
5
-
-
58149193205
-
Allosteric modulation of GPCRs: A novel approach for the treatment of CNS disorders
-
Conn, J. P.; Christopoulos, A.; Lindsley, C. W. Allosteric modulation of GPCRs: a novel approach for the treatment of CNS disorders Nature Rev. Drug Discovery 2009, 8, 41-54
-
(2009)
Nature Rev. Drug Discovery
, vol.8
, pp. 41-54
-
-
Conn, J.P.1
Christopoulos, A.2
Lindsley, C.W.3
-
6
-
-
0025603686
-
1 receptor binding and function by 2-amino-3-benzoylthiophenes
-
1 receptor binding and function by 2-amino-3-benzoylthiophenes Mol. Pharmacol. 1990, 38, 939-949
-
(1990)
Mol. Pharmacol.
, vol.38
, pp. 939-949
-
-
Bruns, R.F.1
Fergus, J.H.2
-
7
-
-
0025638880
-
Structure-activity relationships for enhancement of adenosine A1 receptor binding by 2-amino-3-benzoylthiophenes
-
Bruns, R. F.; Fergus, J. H.; Coughenour, L. L.; Courtland, G. G.; Pugsley, T. A.; Dodd, J. H.; Tinney, F. J. Structure-activity relationships for enhancement of adenosine A1 receptor binding by 2-amino-3-benzoylthiophenes Mol. Pharmacol. 1990, 38, 950-958
-
(1990)
Mol. Pharmacol.
, vol.38
, pp. 950-958
-
-
Bruns, R.F.1
Fergus, J.H.2
Coughenour, L.L.3
Courtland, G.G.4
Pugsley, T.A.5
Dodd, J.H.6
Tinney, F.J.7
-
8
-
-
0033539111
-
1 Receptor. Synthesis and Biological Evaluation of Novel 2-Amino-3-benzoylthiophenes as Allosteric Enhancers of Agonist Binding
-
1 Receptor. Synthesis and Biological Evaluation of Novel 2-Amino-3-benzoylthiophenes as Allosteric Enhancers of Agonist Binding J. Med. Chem. 1999, 42, 3629-3635
-
(1999)
J. Med. Chem.
, vol.42
, pp. 3629-3635
-
-
Van Der Klein, P.A.M.1
Kourounakis, A.P.2
Ijzerman, A.P.3
-
9
-
-
0034605224
-
1-adenosine receptor
-
1-adenosine receptor Bioorg. Med. Chem. Lett. 2000, 10, 1953-1957
-
(2000)
Bioorg. Med. Chem. Lett.
, vol.10
, pp. 1953-1957
-
-
Baraldi, P.G.1
Zaid, A.Z.2
Lampronti, I.3
Fruttarolo, F.F.4
Pavani, M.G.5
Tabrizi, M.A.6
Shyrock, J.C.S.7
Leung, E.8
Romagnoli, R.9
-
10
-
-
0346996805
-
1 adenosine receptors increase receptor-G protein coupling and counteract guanine nucleotide effects on agonist binding
-
1 adenosine receptors increase receptor-G protein coupling and counteract guanine nucleotide effects on agonist binding Mol. Pharmacol. 2003, 64, 1557-1564
-
(2003)
Mol. Pharmacol.
, vol.64
, pp. 1557-1564
-
-
Figler, H.1
Olsson, R.A.2
Linden, J.3
-
11
-
-
3142576214
-
1 Adenosine Agonist Binding: New 3-, 4-, and 5-Modifications
-
1 Adenosine Agonist Binding: New 3-, 4-, and 5-Modifications J. Med. Chem. 2003, 46, 1870-1877
-
(2003)
J. Med. Chem.
, vol.46
, pp. 1870-1877
-
-
Lütjens, H.1
Zickgraf, A.2
Figler, H.3
Linden, J.4
Olsson, R.A.5
Scammells, P.J.6
-
13
-
-
38849185360
-
5-Substituted 2-aminothiophenes as A1 adenosine receptor allosteric enhancers
-
Aurelio, L.; Figler, H.; Flynn, B. L.; Linden, J.; Scammells, P. J. 5-Substituted 2-aminothiophenes as A1 adenosine receptor allosteric enhancers Bioorg. Med. Chem. 2008, 16, 1319-1327
-
(2008)
Bioorg. Med. Chem.
, vol.16
, pp. 1319-1327
-
-
Aurelio, L.1
Figler, H.2
Flynn, B.L.3
Linden, J.4
Scammells, P.J.5
-
14
-
-
71749111336
-
1 adenosine receptor allosteric modulators and antagonists
-
1 adenosine receptor allosteric modulators and antagonists Bioorg. Med. Chem. 2009, 17, 7353-7361
-
(2009)
Bioorg. Med. Chem.
, vol.17
, pp. 7353-7361
-
-
Aurelio, L.1
Valant, C.2
Figler, H.3
Flynn, B.L.4
Linden, J.5
Sexton, P.M.6
Christopoulos, A.7
Scammells, P.J.8
-
15
-
-
67650756920
-
1 Receptor: Synthesis and Pharmacological Evaluation of 4-Substituted 2-Amino-3-benzoylthiophenes
-
1 Receptor: Synthesis and Pharmacological Evaluation of 4-Substituted 2-Amino-3- benzoylthiophenes J. Med. Chem. 2009, 52, 4543-4547
-
(2009)
J. Med. Chem.
, vol.52
, pp. 4543-4547
-
-
Aurelio, L.1
Valant, C.2
Flynn, B.L.3
Sexton, P.M.4
Christopoulos, A.5
Scammells, P.J.6
-
16
-
-
77956730941
-
1 Adenosine Receptor Modulation
-
1 Adenosine Receptor Modulation J. Med. Chem. 2010, 53, 6550-6559
-
(2010)
J. Med. Chem.
, vol.53
, pp. 6550-6559
-
-
Aurelio, L.1
Valant, C.2
Flynn, B.L.3
Sexton, P.M.4
White, J.M.5
Christopoulos, A.6
Scammells, P.J.7
-
17
-
-
79957800958
-
1 adenosine receptor
-
1 adenosine receptor Bioorg. Med. Chem. Lett. 2011, 21, 3704-3707
-
(2011)
Bioorg. Med. Chem. Lett.
, vol.21
, pp. 3704-3707
-
-
Aurelio, L.1
Christopoulos, A.2
Flynn, B.L.3
Scammells, P.J.4
Sexton, P.M.5
Valant, C.6
-
18
-
-
33845903110
-
Functional selectivity and classical concepts of quantitative pharmacology
-
Urban, J. D.; Clarke, W. P.; von Zastrow, M.; Nichols, D. E.; Kobilka, B.; Weinstein, H.; Javitch, J. A.; Roth, B. L.; Christopoulos, A.; Sexton, P. M.; Miller, K. J.; Spedding, M.; Mailman, R. B. Functional selectivity and classical concepts of quantitative pharmacology J. Pharmacol. Exp. Ther. 2007, 320, 1-13
-
(2007)
J. Pharmacol. Exp. Ther.
, vol.320
, pp. 1-13
-
-
Urban, J.D.1
Clarke, W.P.2
Von Zastrow, M.3
Nichols, D.E.4
Kobilka, B.5
Weinstein, H.6
Javitch, J.A.7
Roth, B.L.8
Christopoulos, A.9
Sexton, P.M.10
Miller, K.J.11
Spedding, M.12
Mailman, R.B.13
-
19
-
-
79960502280
-
Ligand functional selectivity and quantitative pharmacology at G protein-coupled receptors
-
Stallaert, W.; Christopoulos, A.; Bouvier, M. Ligand functional selectivity and quantitative pharmacology at G protein-coupled receptors Expert Opin. Drug Discovery 2011, 6, 811-825
-
(2011)
Expert Opin. Drug Discovery
, vol.6
, pp. 811-825
-
-
Stallaert, W.1
Christopoulos, A.2
Bouvier, M.3
-
21
-
-
77956245258
-
Delineating the mode of action of adenosine A1 receptor allosteric modulators
-
Valant, C.; Aurelio, L.; Urmaliya, V. B.; White, P.; Scammells, P. J.; Sexton, P. M.; Christopoulos, A. Delineating the mode of action of adenosine A1 receptor allosteric modulators Mol. Pharmacol. 2010, 78, 444-455
-
(2010)
Mol. Pharmacol.
, vol.78
, pp. 444-455
-
-
Valant, C.1
Aurelio, L.2
Urmaliya, V.B.3
White, P.4
Scammells, P.J.5
Sexton, P.M.6
Christopoulos, A.7
-
22
-
-
0037122790
-
1 adenosine receptors
-
1 adenosine receptors J. Med. Chem. 2002, 45, 382-389
-
(2002)
J. Med. Chem.
, vol.45
, pp. 382-389
-
-
Tranberg, C.E.1
Zickgraf, A.2
Giunta, B.N.3
Lütjens, H.4
Figler, H.5
Falke, R.6
Fleischer, H.7
Linden, J.8
Scammells, P.J.9
Olsson, R.A.10
-
23
-
-
77951223981
-
Identification of Orthosteric and Allosteric Site Mutations in M2 Muscarinic Acetylcholine Receptors That Contribute to Ligand-Selective Signaling Bias
-
Gregory, K. J.; Hall, N. E.; Tobin, A. B.; Sexton, P. M.; Christopoulos, A. Identification of Orthosteric and Allosteric Site Mutations in M2 Muscarinic Acetylcholine Receptors That Contribute to Ligand-Selective Signaling Bias J. Biol. Chem. 2010, 285, 7459-7474
-
(2010)
J. Biol. Chem.
, vol.285
, pp. 7459-7474
-
-
Gregory, K.J.1
Hall, N.E.2
Tobin, A.B.3
Sexton, P.M.4
Christopoulos, A.5
-
24
-
-
77956249652
-
Allosteric ligands of the glucagon-like peptide 1 receptor (GLP-1R) differentially modulate endogenous and exogenous peptide responses in a pathway-selective manner: Implications for drug screening
-
Koole, C.; Wootten, D.; Simms, J.; Valant, C.; Sridhar, R.; Woodman, O. L.; Miller, L. J.; Summers, R. J.; Christopoulos, A.; Sexton, P. M. Allosteric ligands of the glucagon-like peptide 1 receptor (GLP-1R) differentially modulate endogenous and exogenous peptide responses in a pathway-selective manner: implications for drug screening Mol. Pharmacol. 2010, 78, 465-465
-
(2010)
Mol. Pharmacol.
, vol.78
, pp. 465-465
-
-
Koole, C.1
Wootten, D.2
Simms, J.3
Valant, C.4
Sridhar, R.5
Woodman, O.L.6
Miller, L.J.7
Summers, R.J.8
Christopoulos, A.9
Sexton, P.M.10
-
25
-
-
78751538699
-
Quantification of functional selectivity at the human α1A-adrenoceptor
-
Evans, B. A.; Broxton, N.; Merlin, J.; Sato, M.; Hutchinson, D. S.; Christopoulos, A.; Summers, R. J. Quantification of functional selectivity at the human α1A-adrenoceptor Mol. Pharmacol. 2011, 79, 298-307
-
(2011)
Mol. Pharmacol.
, vol.79
, pp. 298-307
-
-
Evans, B.A.1
Broxton, N.2
Merlin, J.3
Sato, M.4
Hutchinson, D.S.5
Christopoulos, A.6
Summers, R.J.7
-
26
-
-
78149496159
-
Allosteric modulation of G protein-coupled receptors: A pharmacological perspective
-
Keov, P.; Sexton, P. M.; Christopoulos, A. Allosteric modulation of G protein-coupled receptors: a pharmacological perspective Neuropharmacology 2011, 60, 24-35
-
(2011)
Neuropharmacology
, vol.60
, pp. 24-35
-
-
Keov, P.1
Sexton, P.M.2
Christopoulos, A.3
-
27
-
-
84855290525
-
A Monod-Wyman-Changeux Mechanism Can Explain G Protein-Coupled Receptor (GPCR) Allosteric Modulation
-
Canals, M.; Lane, J. R.; Wen, A.; Scammells, P. J.; Sexton, P. M.; Christopoulos, A. A Monod-Wyman-Changeux Mechanism Can Explain G Protein-Coupled Receptor (GPCR) Allosteric Modulation J. Biol. Chem. 2012, 287, 650-659
-
(2012)
J. Biol. Chem.
, vol.287
, pp. 650-659
-
-
Canals, M.1
Lane, J.R.2
Wen, A.3
Scammells, P.J.4
Sexton, P.M.5
Christopoulos, A.6
-
28
-
-
34447632041
-
Allosteric GPCR modulators: Taking advantage of permissive receptor pharmacology
-
Leach, K.; Sexton, P. M.; Christopoulos, A. Allosteric GPCR modulators: taking advantage of permissive receptor pharmacology Trends Pharmacol. Sci. 2007, 28, 382-389
-
(2007)
Trends Pharmacol. Sci.
, vol.28
, pp. 382-389
-
-
Leach, K.1
Sexton, P.M.2
Christopoulos, A.3
-
29
-
-
84863408610
-
Measurement of ligand-G protein-coupled receptor interactions
-
In; Poyner, D. R. Wheatley, M. Wiley-Blackwell: Oxford, UK
-
Leach, K.; Valant, C.; Sexton, P. M.; Christopoulos, A. Measurement of ligand-G protein-coupled receptor interactions. In G Protein-Coupled Receptors; Poyner, D. R.; Wheatley, M., Eds.; Wiley-Blackwell: Oxford, UK, 2010; pp 1-29.
-
(2010)
G Protein-Coupled Receptors
, pp. 1-29
-
-
Leach, K.1
Valant, C.2
Sexton, P.M.3
Christopoulos, A.4
-
32
-
-
33646767009
-
ORTEP-3 for windows-a version of ORTEP-III with a graphical user interface (GUI)
-
Farrugia, L. J. ORTEP-3 for windows-a version of ORTEP-III with a graphical user interface (GUI) J. Appl. Crystallogr. 1997, 30, 565
-
(1997)
J. Appl. Crystallogr.
, vol.30
, pp. 565
-
-
Farrugia, L.J.1
-
33
-
-
0141452964
-
WinGX suite for small-molecule single-crystal crystallography
-
Farrugia, L. J. WinGX suite for small-molecule single-crystal crystallography J. Appl. Crystallogr. 1999, 32, 837-838
-
(1999)
J. Appl. Crystallogr.
, vol.32
, pp. 837-838
-
-
Farrugia, L.J.1
|