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Items: 16

1.

6-Phenylpyrimidin-4-ones as Positive Allosteric Modulators at the M1 mAChR: The Determinants of Allosteric Activity.

Jörg M, van der Westhuizen ET, Khajehali E, Burger WAC, White JM, Choy KHC, Tobin AB, Sexton PM, Valant C, Capuano B, Christopoulos A, Scammells PJ.

ACS Chem Neurosci. 2019 Mar 20;10(3):1099-1114. doi: 10.1021/acschemneuro.8b00613. Epub 2018 Dec 28.

PMID:
30547573
2.

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
3.

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
4.

Purinergic Receptor Transactivation by the β2-Adrenergic Receptor Increases Intracellular Ca2+ in Nonexcitable Cells.

Stallaert W, van der Westhuizen ET, Schönegge AM, Plouffe B, Hogue M, Lukashova V, Inoue A, Ishida S, Aoki J, Le Gouill C, Bouvier M.

Mol Pharmacol. 2017 May;91(5):533-544. doi: 10.1124/mol.116.106419. Epub 2017 Mar 9.

PMID:
28280061
5.

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.

PMID:
25650376
6.

Quantification of ligand bias for clinically relevant β2-adrenergic receptor ligands: implications for drug taxonomy.

van der Westhuizen ET, Breton B, Christopoulos A, Bouvier M.

Mol Pharmacol. 2014 Mar;85(3):492-509. doi: 10.1124/mol.113.088880. Epub 2013 Dec 23.

PMID:
24366668
7.

Relaxin family peptides and their receptors.

Bathgate RA, Halls ML, van der Westhuizen ET, Callander GE, Kocan M, Summers RJ.

Physiol Rev. 2013 Jan;93(1):405-80. doi: 10.1152/physrev.00001.2012. Review.

8.

H2 relaxin is a biased ligand relative to H3 relaxin at the relaxin family peptide receptor 3 (RXFP3).

van der Westhuizen ET, Christopoulos A, Sexton PM, Wade JD, Summers RJ.

Mol Pharmacol. 2010 May;77(5):759-72. doi: 10.1124/mol.109.061432. Epub 2010 Feb 16.

PMID:
20159943
9.

Addition of a carboxy-terminal green fluorescent protein does not alter the binding and signaling properties of relaxin family Peptide receptor 3.

van der Westhuizen ET, Wade JD, Sexton PM, Summers RJ.

Ann N Y Acad Sci. 2009 Apr;1160:105-7. doi: 10.1111/j.1749-6632.2008.03818.x.

PMID:
19416168
10.

Roles of the receptor, the ligand, and the cell in the signal transduction pathways utilized by the relaxin family peptide receptors 1-3.

Summers RJ, Bathgate RA, Wade JD, van der Westhuizen ET, Halls ML.

Ann N Y Acad Sci. 2009 Apr;1160:99-104. doi: 10.1111/j.1749-6632.2009.03828.x.

PMID:
19416167
11.

Relaxin family peptide receptor (RXFP1) coupling to G(alpha)i3 involves the C-terminal Arg752 and localization within membrane Raft Microdomains.

Halls ML, van der Westhuizen ET, Wade JD, Evans BA, Bathgate RA, Summers RJ.

Mol Pharmacol. 2009 Feb;75(2):415-28. doi: 10.1124/mol.108.051227. Epub 2008 Nov 24.

PMID:
19029286
12.

Relaxin family peptide receptors--from orphans to therapeutic targets.

van der Westhuizen ET, Halls ML, Samuel CS, Bathgate RA, Unemori EN, Sutton SW, Summers RJ.

Drug Discov Today. 2008 Aug;13(15-16):640-51. doi: 10.1016/j.drudis.2008.04.002. Epub 2008 Jun 6. Review.

PMID:
18675759
13.

The relaxin family peptide receptor 3 activates extracellular signal-regulated kinase 1/2 through a protein kinase C-dependent mechanism.

van der Westhuizen ET, Werry TD, Sexton PM, Summers RJ.

Mol Pharmacol. 2007 Jun;71(6):1618-29. Epub 2007 Mar 9.

PMID:
17351017
14.

Relaxin family peptide receptors--former orphans reunite with their parent ligands to activate multiple signalling pathways.

Halls ML, van der Westhuizen ET, Bathgate RA, Summers RJ.

Br J Pharmacol. 2007 Mar;150(6):677-91. Epub 2007 Feb 12. Review.

15.

Relaxin receptors--new drug targets for multiple disease states.

Van Der Westhuizen ET, Summers RJ, Halls ML, Bathgate RA, Sexton PM.

Curr Drug Targets. 2007 Jan;8(1):91-104. Review.

PMID:
17266534
16.

Responses of GPCR135 to human gene 3 (H3) relaxin in CHO-K1 cells determined by microphysiometry.

Van der Westhuizen ET, Sexton PM, Bathgate RA, Summers RJ.

Ann N Y Acad Sci. 2005 May;1041:332-7.

PMID:
15956730

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