Year |
Citation |
Score |
2023 |
Jörg M, van der Westhuizen ET, Lu Y, Christopher Choy KH, Shackleford DM, Khajehali E, Tobin AB, Thal DM, Capuano B, Christopoulos A, Valant C, Scammells PJ. Design, synthesis and evaluation of novel 2-phenyl-3-(1H-pyrazol-4-yl)pyridine positive allosteric modulators for the M mAChR. European Journal of Medicinal Chemistry. 258: 115588. PMID 37423123 DOI: 10.1016/j.ejmech.2023.115588 |
0.337 |
|
2023 |
Vuckovic Z, Wang J, Pham V, Mobbs JI, Belousoff MJ, Bhattarai A, Burger WAC, Thompson G, Yeasmin M, Nawaratne V, Leach K, van der Westhuizen ET, Khajehali E, Liang YL, Glukhova A, et al. Pharmacological hallmarks of allostery at the M4 muscarinic receptor elucidated through structure and dynamics. Elife. 12. PMID 37248726 DOI: 10.7554/eLife.83477 |
0.392 |
|
2022 |
Nguyen HTM, van der Westhuizen ET, Langmead CJ, Tobin AB, Sexton PM, Christopoulos A, Valant C. Opportunities and challenges for the development of M1 muscarinic receptor positive allosteric modulators in the treatment for neurocognitive deficits. British Journal of Pharmacology. PMID 36355830 DOI: 10.1111/bph.15982 |
0.493 |
|
2022 |
McDonald JK, van der Westhuizen ET, Pham V, Thompson G, Felder CC, Paul SM, Thal DM, Christopoulos A, Valant C. Biased Profile of Xanomeline at the Recombinant Human M Muscarinic Acetylcholine Receptor. Acs Chemical Neuroscience. PMID 35380782 DOI: 10.1021/acschemneuro.1c00827 |
0.627 |
|
2021 |
Burger WAC, Gentry PR, Berizzi AE, Vuckovic Z, van der Westhuizen ET, Thompson G, Yeasmin M, Lindsley CW, Sexton PM, Langmead CJ, Tobin AB, Christopoulos A, Valant C, Thal DM. Identification of a Novel Allosteric Site at the M Muscarinic Acetylcholine Receptor. Acs Chemical Neuroscience. PMID 34351123 DOI: 10.1021/acschemneuro.1c00383 |
0.513 |
|
2020 |
van der Westhuizen ET, Choy KHC, Valant C, McKenzie-Nickson S, Bradley SJ, Tobin AB, Sexton PM, Christopoulos A. Fine Tuning Muscarinic Acetylcholine Receptor Signaling Through Allostery and Bias. Frontiers in Pharmacology. 11: 606656. PMID 33584282 DOI: 10.3389/fphar.2020.606656 |
0.609 |
|
2020 |
Khajehali E, Bradley S, van der Westhuizen ET, Molloy C, Valant C, Finlayson L, Lindsley CW, Sexton PM, Tobin AB, Christopoulos A. Restoring Agonist Function at a Chemogenetically Modified M Muscarinic Acetylcholine Receptor. Acs Chemical Neuroscience. PMID 33196174 DOI: 10.1021/acschemneuro.0c00540 |
0.575 |
|
2020 |
Scammells PJ, Jörg M, Khajehali E, van der Westhuizen ET, Choy KHC, Shackleford D, Tobin AB, Sexton PM, Valant C, Capuano B, Christopoulos A. Development of Novel 4-Arylpyridin-2-one and 6-Arylpyrimidin-4-one Positive Allosteric Modulators of the M1 Muscarinic Acetylcholine Receptor. Chemmedchem. PMID 32851779 DOI: 10.1002/cmdc.202000540 |
0.55 |
|
2020 |
Benredjem B, Gallion J, Pelletier D, Dallaire P, Charbonneau J, Cawkill D, Nagi K, Gosink M, Lukasheva V, Jenkinson S, Ren Y, Somps C, Murat B, Van Der Westhuizen E, Le Gouill C, et al. Author Correction: Exploring use of unsupervised clustering to associate signaling profiles of GPCR ligands to clinical response. Nature Communications. 11: 1929. PMID 32300106 DOI: 10.1038/S41467-020-15945-Y |
0.727 |
|
2019 |
Vuckovic Z, Gentry PR, Berizzi AE, Hirata K, Varghese S, Thompson G, van der Westhuizen ET, Burger WAC, Rahmani R, Valant C, Langmead CJ, Lindsley CW, Baell JB, Tobin AB, Sexton PM, et al. Crystal structure of the M muscarinic acetylcholine receptor. Proceedings of the National Academy of Sciences of the United States of America. PMID 31772027 DOI: 10.2210/Pdb6Ol9/Pdb |
0.572 |
|
2019 |
Benredjem B, Gallion J, Pelletier D, Dallaire P, Charbonneau J, Cawkill D, Nagi K, Gosink M, Lukasheva V, Jenkinson S, Ren Y, Somps C, Murat B, Van Der Westhuizen E, Le Gouill C, et al. Exploring use of unsupervised clustering to associate signaling profiles of GPCR ligands to clinical response. Nature Communications. 10: 4075. PMID 31501422 DOI: 10.1038/S41467-019-11875-6 |
0.755 |
|
2018 |
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. 6-Phenylpyrimidin-4-ones as Positive Allosteric Modulators at the M1 mAChR: The Determinants of Allosteric Activity. Acs Chemical Neuroscience. PMID 30547573 DOI: 10.1021/acschemneuro.8b00613 |
0.561 |
|
2018 |
Masureel M, Zou Y, Picard LP, van der Westhuizen E, Mahoney JP, Rodrigues JPGLM, Mildorf TJ, Dror RO, Shaw DE, Bouvier M, Pardon E, Steyaert J, Sunahara RK, Weis WI, Zhang C, et al. Publisher Correction: Structural insights into binding specificity, efficacy and bias of a βAR partial agonist. Nature Chemical Biology. PMID 30504785 DOI: 10.1038/S41589-018-0182-5 |
0.717 |
|
2018 |
Masureel M, Zou Y, Picard LP, van der Westhuizen E, Mahoney JP, Rodrigues JPGLM, Mildorf TJ, Dror RO, Shaw DE, Bouvier M, Pardon E, Steyaert J, Sunahara RK, Weis WI, Zhang C, et al. Structural insights into binding specificity, efficacy and bias of a βAR partial agonist. Nature Chemical Biology. 14: 1059-1066. PMID 30327561 DOI: 10.1038/S41589-018-0145-X |
0.76 |
|
2018 |
van der Westhuizen ET, Spathis A, Khajehali E, Jörg M, Mistry SN, Capuano B, Tobin AB, Sexton PM, Scammells PJ, Valant C, Christopoulos A. Assessment of the Molecular Mechanisms of Action of Novel 4-Phenylpyridine-2-One and 6-Phenylpyrimidin-4-One Allosteric Modulators at the M Muscarinic Acetylcholine Receptors. Molecular Pharmacology. 94: 770-783. PMID 29691279 DOI: 10.1124/mol.118.111633 |
0.568 |
|
2018 |
Dallagnol JCC, Khajehali E, van der Westhuizen ET, Jörg M, Valant C, Gonçalves AG, Capuano B, Christopoulos A, Scammells PJ. Synthesis and Pharmacological Evaluation of Heterocyclic Carboxamides: Positive Allosteric Modulators of the M Muscarinic Acetylcholine Receptor with Weak Agonist Activity and Diverse Modulatory Profiles. Journal of Medicinal Chemistry. 61: 2875-2894. PMID 29544056 DOI: 10.1021/acs.jmedchem.7b01812 |
0.597 |
|
2017 |
Stallaert W, van der Westhuizen ET, Schonegge AM, Plouffe B, Hogue M, Lukashova V, Inoue A, Ishida S, Aoki J, Le Gouill C, Bouvier M. Purinergic receptor transactivation by the β2-adrenergic receptor increases intracellular Ca(2+) in non-excitable cells. Molecular Pharmacology. PMID 28280061 DOI: 10.1124/Mol.116.106419 |
0.738 |
|
2015 |
van der Westhuizen ET, Valant C, Sexton PM, Christopoulos A. Endogenous allosteric modulators of G protein-coupled receptors. The Journal of Pharmacology and Experimental Therapeutics. 353: 246-60. PMID 25650376 DOI: 10.1124/jpet.114.221606 |
0.59 |
|
2014 |
van der Westhuizen ET, Breton B, Christopoulos A, Bouvier M. Quantification of ligand bias for clinically relevant β2-adrenergic receptor ligands: implications for drug taxonomy. Molecular Pharmacology. 85: 492-509. PMID 24366668 DOI: 10.1124/Mol.113.088880 |
0.794 |
|
2012 |
Stallaert W, Dorn JF, van der Westhuizen E, Audet M, Bouvier M. Impedance responses reveal β₂-adrenergic receptor signaling pluridimensionality and allow classification of ligands with distinct signaling profiles. Plos One. 7: e29420. PMID 22242170 DOI: 10.1371/Journal.Pone.0029420 |
0.789 |
|
2010 |
van der Westhuizen ET, Christopoulos A, Sexton PM, Wade JD, Summers RJ. H2 relaxin is a biased ligand relative to H3 relaxin at the relaxin family peptide receptor 3 (RXFP3). Molecular Pharmacology. 77: 759-72. PMID 20159943 DOI: 10.1124/mol.109.061432 |
0.681 |
|
2009 |
van der Westhuizen ET, Wade JD, Sexton PM, Summers RJ. Addition of a carboxy-terminal green fluorescent protein does not alter the binding and signaling properties of relaxin family Peptide receptor 3. Annals of the New York Academy of Sciences. 1160: 105-7. PMID 19416168 DOI: 10.1111/j.1749-6632.2008.03818.x |
0.673 |
|
2009 |
Summers RJ, Bathgate RA, Wade JD, van der Westhuizen ET, Halls ML. Roles of the receptor, the ligand, and the cell in the signal transduction pathways utilized by the relaxin family peptide receptors 1-3. Annals of the New York Academy of Sciences. 1160: 99-104. PMID 19416167 DOI: 10.1111/j.1749-6632.2009.03828.x |
0.704 |
|
2009 |
Halls ML, van der Westhuizen ET, Wade JD, Evans BA, Bathgate RA, Summers RJ. Relaxin family peptide receptor (RXFP1) coupling to G(alpha)i3 involves the C-terminal Arg752 and localization within membrane Raft Microdomains. Molecular Pharmacology. 75: 415-28. PMID 19029286 DOI: 10.1124/mol.108.051227 |
0.599 |
|
2008 |
van der Westhuizen ET, Halls ML, Samuel CS, Bathgate RA, Unemori EN, Sutton SW, Summers RJ. Relaxin family peptide receptors--from orphans to therapeutic targets. Drug Discovery Today. 13: 640-51. PMID 18675759 DOI: 10.1016/j.drudis.2008.04.002 |
0.625 |
|
2007 |
van der Westhuizen ET, Werry TD, Sexton PM, Summers RJ. The relaxin family peptide receptor 3 activates extracellular signal-regulated kinase 1/2 through a protein kinase C-dependent mechanism. Molecular Pharmacology. 71: 1618-29. PMID 17351017 DOI: 10.1124/mol.106.032763 |
0.644 |
|
2007 |
Van Der Westhuizen ET, Summers RJ, Halls ML, Bathgate RA, Sexton PM. Relaxin receptors--new drug targets for multiple disease states. Current Drug Targets. 8: 91-104. PMID 17266534 DOI: 10.2174/138945007779315650 |
0.349 |
|
2005 |
Van der Westhuizen ET, Sexton PM, Bathgate RA, Summers RJ. Responses of GPCR135 to human gene 3 (H3) relaxin in CHO-K1 cells determined by microphysiometry. Annals of the New York Academy of Sciences. 1041: 332-7. PMID 15956730 DOI: 10.1196/annals.1282.053 |
0.543 |
|
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