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Items: 39

1.

Utility of an "Allosteric Site-Impaired" M2 Muscarinic Acetylcholine Receptor as a Novel Construct for Validating Mechanisms of Action of Synthetic and Putative Endogenous Allosteric Modulators.

Von Moo E, Sexton PM, Christopoulos A, Valant C.

Mol Pharmacol. 2018 Nov;94(5):1298-1309. doi: 10.1124/mol.118.112490. Epub 2018 Sep 13.

PMID:
30213802
2.

Probing the binding site of novel selective positive allosteric modulators at the M1 muscarinic acetylcholine receptor.

Khajehali E, Valant C, Jörg M, Tobin AB, Conn PJ, Lindsley CW, Sexton PM, Scammells PJ, Christopoulos A.

Biochem Pharmacol. 2018 Aug;154:243-254. doi: 10.1016/j.bcp.2018.05.009. Epub 2018 May 17.

3.

Assessment of the Molecular Mechanisms of Action of Novel 4-Phenylpyridine-2-One and 6-Phenylpyrimidin-4-One Allosteric Modulators at the M1 Muscarinic Acetylcholine Receptors.

van der Westhuizen ET, Spathis A, Khajehali E, Jörg M, Mistry SN, Capuano B, Tobin AB, Sexton PM, Scammells PJ, Valant C, Christopoulos A.

Mol Pharmacol. 2018 Jul;94(1):770-783. doi: 10.1124/mol.118.111633. Epub 2018 Apr 24.

PMID:
29691279
4.

Synthesis and Pharmacological Evaluation of Heterocyclic Carboxamides: Positive Allosteric Modulators of the M1 Muscarinic Acetylcholine Receptor with Weak Agonist Activity and Diverse Modulatory Profiles.

Dallagnol JCC, Khajehali E, van der Westhuizen ET, Jörg M, Valant C, Gonçalves AG, Capuano B, Christopoulos A, Scammells PJ.

J Med Chem. 2018 Apr 12;61(7):2875-2894. doi: 10.1021/acs.jmedchem.7b01812. Epub 2018 Mar 23.

PMID:
29544056
5.

Structure-based discovery of selective positive allosteric modulators of antagonists for the M2 muscarinic acetylcholine receptor.

Korczynska M, Clark MJ, Valant C, Xu J, Moo EV, Albold S, Weiss DR, Torosyan H, Huang W, Kruse AC, Lyda BR, May LT, Baltos JA, Sexton PM, Kobilka BK, Christopoulos A, Shoichet BK, Sunahara RK.

Proc Natl Acad Sci U S A. 2018 Mar 6;115(10):E2419-E2428. doi: 10.1073/pnas.1718037115. Epub 2018 Feb 16.

6.

A Structure-Activity Relationship Study of Bitopic N6-Substituted Adenosine Derivatives as Biased Adenosine A1 Receptor Agonists.

Aurelio L, Baltos JA, Ford L, Nguyen ATN, Jörg M, Devine SM, Valant C, White PJ, Christopoulos A, May LT, Scammells PJ.

J Med Chem. 2018 Mar 8;61(5):2087-2103. doi: 10.1021/acs.jmedchem.8b00047. Epub 2018 Feb 23.

PMID:
29446948
7.

Structure-Based Design and Discovery of New M2 Receptor Agonists.

Fish I, Stößel A, Eitel K, Valant C, Albold S, Huebner H, Möller D, Clark MJ, Sunahara RK, Christopoulos A, Shoichet BK, Gmeiner P.

J Med Chem. 2017 Nov 22;60(22):9239-9250. doi: 10.1021/acs.jmedchem.7b01113. Epub 2017 Nov 13.

PMID:
29094937
8.

Accelerated structure-based design of chemically diverse allosteric modulators of a muscarinic G protein-coupled receptor.

Miao Y, Goldfeld DA, Moo EV, Sexton PM, Christopoulos A, McCammon JA, Valant C.

Proc Natl Acad Sci U S A. 2016 Sep 20;113(38):E5675-84. doi: 10.1073/pnas.1612353113. Epub 2016 Sep 6.

9.

Label-Free Kinetics: Exploiting Functional Hemi-Equilibrium to Derive Rate Constants for Muscarinic Receptor Antagonists.

Riddy DM, Valant C, Rueda P, Charman WN, Sexton PM, Summers RJ, Christopoulos A, Langmead CJ.

Mol Pharmacol. 2015 Oct;88(4):779-90. doi: 10.1124/mol.115.100545. Epub 2015 Aug 4.

10.

Synthesis and pharmacological evaluation of M4 muscarinic receptor positive allosteric modulators derived from VU10004.

Huynh T, Valant C, Crosby IT, Sexton PM, Christopoulos A, Capuano B.

ACS Chem Neurosci. 2015 Jun 17;6(6):838-44. doi: 10.1021/acschemneuro.5b00035. Epub 2015 Apr 17.

PMID:
25857219
11.

Endogenous allosteric modulators of G protein-coupled receptors.

van der Westhuizen ET, Valant C, Sexton PM, Christopoulos A.

J Pharmacol Exp Ther. 2015 May;353(2):246-60. doi: 10.1124/jpet.114.221606. Epub 2015 Feb 3. Review.

12.

Molecular mechanisms of bitopic ligand engagement with the M1 muscarinic acetylcholine receptor.

Keov P, López L, Devine SM, Valant C, Lane JR, Scammells PJ, Sexton PM, Christopoulos A.

J Biol Chem. 2014 Aug 22;289(34):23817-37. doi: 10.1074/jbc.M114.582874. Epub 2014 Jul 8.

13.

Synthesis and pharmacological evaluation of analogues of benzyl quinolone carboxylic acid (BQCA) designed to bind irreversibly to an allosteric site of the M ₁ muscarinic acetylcholine receptor.

Davie BJ, Valant C, White JM, Sexton PM, Capuano B, Christopoulos A, Scammells PJ.

J Med Chem. 2014 Jun 26;57(12):5405-18. doi: 10.1021/jm500556a. Epub 2014 Jun 5.

PMID:
24856614
14.

Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist.

Valant C, May LT, Aurelio L, Chuo CH, White PJ, Baltos JA, Sexton PM, Scammells PJ, Christopoulos A.

Proc Natl Acad Sci U S A. 2014 Mar 25;111(12):4614-9. doi: 10.1073/pnas.1320962111. Epub 2014 Mar 11.

15.

Activation and allosteric modulation of a muscarinic acetylcholine receptor.

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.

Nature. 2013 Dec 5;504(7478):101-6. doi: 10.1038/nature12735. Epub 2013 Nov 20.

16.

Structural basis for modulation of a G-protein-coupled receptor by allosteric drugs.

Dror RO, Green HF, Valant C, Borhani DW, Valcourt JR, Pan AC, Arlow DH, Canals M, Lane JR, Rahmani R, Baell JB, Sexton PM, Christopoulos A, Shaw DE.

Nature. 2013 Nov 14;503(7475):295-9. doi: 10.1038/nature12595. Epub 2013 Oct 13.

PMID:
24121438
17.

Probing structural requirements of positive allosteric modulators of the M4 muscarinic receptor.

Huynh T, Valant C, Crosby IT, Sexton PM, Christopoulos A, Capuano B.

J Med Chem. 2013 Oct 24;56(20):8196-200. doi: 10.1021/jm401032k. Epub 2013 Oct 11.

PMID:
24074052
18.

Reverse engineering of the selective agonist TBPB unveils both orthosteric and allosteric modes of action at the M₁ muscarinic acetylcholine receptor.

Keov P, Valant C, Devine SM, Lane JR, Scammells PJ, Sexton PM, Christopoulos A.

Mol Pharmacol. 2013 Sep;84(3):425-37. doi: 10.1124/mol.113.087320. Epub 2013 Jun 24.

19.

Synthesis and pharmacological profiling of analogues of benzyl quinolone carboxylic acid (BQCA) as allosteric modulators of the M1 muscarinic receptor.

Mistry SN, Valant C, Sexton PM, Capuano B, Christopoulos A, Scammells PJ.

J Med Chem. 2013 Jun 27;56(12):5151-72. doi: 10.1021/jm400540b. Epub 2013 Jun 17.

PMID:
23718562
20.

Allosteric modulation of endogenous metabolites as an avenue for drug discovery.

Wootten D, Savage EE, Valant C, May LT, Sloop KW, Ficorilli J, Showalter AD, Willard FS, Christopoulos A, Sexton PM.

Mol Pharmacol. 2012 Aug;82(2):281-90. doi: 10.1124/mol.112.079319. Epub 2012 May 10.

21.

Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1,2,3,6-tetrahydropyridines as 5-HT₂C agonists.

Conway RJ, Valant C, Christopoulos A, Robertson AD, Capuano B, Crosby IT.

Bioorg Med Chem Lett. 2012 Apr 1;22(7):2560-4. doi: 10.1016/j.bmcl.2012.01.122. Epub 2012 Feb 9.

PMID:
22381048
22.

Fluorescent derivatives of AC-42 to probe bitopic orthosteric/allosteric binding mechanisms on muscarinic M1 receptors.

Daval SB, Valant C, Bonnet D, Kellenberger E, Hibert M, Galzi JL, Ilien B.

J Med Chem. 2012 Mar 8;55(5):2125-43. doi: 10.1021/jm201348t. Epub 2012 Feb 27.

PMID:
22329602
23.

Synthesis and characterization of novel 2-amino-3-benzoylthiophene derivatives as biased allosteric agonists and modulators of the adenosine A(1) receptor.

Valant C, Aurelio L, Devine SM, Ashton TD, White JM, Sexton PM, Christopoulos A, Scammells PJ.

J Med Chem. 2012 Mar 8;55(5):2367-75. doi: 10.1021/jm201600e. Epub 2012 Feb 17.

PMID:
22315963
24.

Positive and negative allosteric modulators promote biased signaling at the calcium-sensing receptor.

Davey AE, Leach K, Valant C, Conigrave AD, Sexton PM, Christopoulos A.

Endocrinology. 2012 Mar;153(3):1232-41. doi: 10.1210/en.2011-1426. Epub 2011 Dec 30.

PMID:
22210744
25.

Probe dependence in the allosteric modulation of a G protein-coupled receptor: implications for detection and validation of allosteric ligand effects.

Valant C, Felder CC, Sexton PM, Christopoulos A.

Mol Pharmacol. 2012 Jan;81(1):41-52. doi: 10.1124/mol.111.074872. Epub 2011 Oct 11.

26.

The best of both worlds? Bitopic orthosteric/allosteric ligands of g protein-coupled receptors.

Valant C, Robert Lane J, Sexton PM, Christopoulos A.

Annu Rev Pharmacol Toxicol. 2012;52:153-78. doi: 10.1146/annurev-pharmtox-010611-134514. Epub 2011 Sep 9. Review.

PMID:
21910627
27.

Polymorphism and ligand dependent changes in human glucagon-like peptide-1 receptor (GLP-1R) function: allosteric rescue of loss of function mutation.

Koole C, Wootten D, Simms J, Valant C, Miller LJ, Christopoulos A, Sexton PM.

Mol Pharmacol. 2011 Sep;80(3):486-97. doi: 10.1124/mol.111.072884. Epub 2011 May 26. Erratum in: Mol Pharmacol. 2012 Jul;82(1):142.

28.

The synthesis and biological evaluation of 2-amino-4,5,6,7,8,9-hexahydrocycloocta[b]thiophenes as allosteric modulators of the A1 adenosine receptor.

Aurelio L, Christopoulos A, Flynn BL, Scammells PJ, Sexton PM, Valant C.

Bioorg Med Chem Lett. 2011 Jun 15;21(12):3704-7. doi: 10.1016/j.bmcl.2011.04.080. Epub 2011 May 4.

PMID:
21612922
29.

Effects of conformational restriction of 2-amino-3-benzoylthiophenes on A(1) adenosine receptor modulation.

Aurelio L, Valant C, Flynn BL, Sexton PM, White JM, Christopoulos A, Scammells PJ.

J Med Chem. 2010 Sep 23;53(18):6550-9. doi: 10.1021/jm1008538.

PMID:
20806896
30.

Delineating the mode of action of adenosine A1 receptor allosteric modulators.

Valant C, Aurelio L, Urmaliya VB, White P, Scammells PJ, Sexton PM, Christopoulos A.

Mol Pharmacol. 2010 Sep;78(3):444-55. doi: 10.1124/mol.110.064568. Epub 2010 Jun 14.

31.

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 OL, Miller LJ, Summers RJ, Christopoulos A, Sexton PM.

Mol Pharmacol. 2010 Sep;78(3):456-65. doi: 10.1124/mol.110.065664. Epub 2010 Jun 14.

32.

3- and 6-Substituted 2-amino-4,5,6,7-tetrahydrothieno[2,3-c]pyridines as A1 adenosine receptor allosteric modulators and antagonists.

Aurelio L, Valant C, Figler H, Flynn BL, Linden J, Sexton PM, Christopoulos A, Scammells PJ.

Bioorg Med Chem. 2009 Oct 15;17(20):7353-61. doi: 10.1016/j.bmc.2009.08.024. Epub 2009 Aug 20.

33.

Allosteric functional switch of neurokinin A-mediated signaling at the neurokinin NK2 receptor: structural exploration.

Valant C, Maillet E, Bourguignon JJ, Bucher B, Utard V, Galzi JL, Hibert M.

J Med Chem. 2009 Oct 8;52(19):5999-6011. doi: 10.1021/jm900671k.

PMID:
19746979
34.

Determination of adenosine A1 receptor agonist and antagonist pharmacology using Saccharomyces cerevisiae: implications for ligand screening and functional selectivity.

Stewart GD, Valant C, Dowell SJ, Mijaljica D, Devenish RJ, Scammells PJ, Sexton PM, Christopoulos A.

J Pharmacol Exp Ther. 2009 Oct;331(1):277-86. doi: 10.1124/jpet.109.158667. Epub 2009 Jul 29.

35.

Orthosteric/allosteric bitopic ligands: going hybrid at GPCRs.

Valant C, Sexton PM, Christopoulos A.

Mol Interv. 2009 Jun;9(3):125-35. doi: 10.1124/mi.9.3.6. Review.

PMID:
19592673
36.

Allosteric modulators of the adenosine A1 receptor: synthesis and pharmacological evaluation of 4-substituted 2-amino-3-benzoylthiophenes.

Aurelio L, Valant C, Flynn BL, Sexton PM, Christopoulos A, Scammells PJ.

J Med Chem. 2009 Jul 23;52(14):4543-7. doi: 10.1021/jm9002582.

PMID:
19514747
37.

2-aminothienopyridazines as novel adenosine A1 receptor allosteric modulators and antagonists.

Ferguson GN, Valant C, Horne J, Figler H, Flynn BL, Linden J, Chalmers DK, Sexton PM, Christopoulos A, Scammells PJ.

J Med Chem. 2008 Oct 9;51(19):6165-72. doi: 10.1021/jm800557d. Epub 2008 Sep 5.

38.

A novel mechanism of G protein-coupled receptor functional selectivity. Muscarinic partial agonist McN-A-343 as a bitopic orthosteric/allosteric ligand.

Valant C, Gregory KJ, Hall NE, Scammells PJ, Lew MJ, Sexton PM, Christopoulos A.

J Biol Chem. 2008 Oct 24;283(43):29312-21. doi: 10.1074/jbc.M803801200. Epub 2008 Aug 22.

39.

A novel, conformation-specific allosteric inhibitor of the tachykinin NK2 receptor (NK2R) with functionally selective properties.

Maillet EL, Pellegrini N, Valant C, Bucher B, Hibert M, Bourguignon JJ, Galzi JL.

FASEB J. 2007 Jul;21(9):2124-34. Epub 2007 Mar 19.

PMID:
17371796

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