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Design, synthesis and evaluation of novel 2-phenyl-3-(1H-pyrazol-4-yl)pyridine positive allosteric modulators for the M4 mAChR.
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. Jörg M, et al. Among authors: van der westhuizen et. Eur J Med Chem. 2023 Oct 5;258:115588. doi: 10.1016/j.ejmech.2023.115588. Epub 2023 Jul 1. Eur J Med Chem. 2023. PMID: 37423123 Free PMC article.
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. Dallagnol JCC, et al. Among authors: van der westhuizen et. J Med Chem. 2018 Apr 12;61(7):2875-2894. doi: 10.1021/acs.jmedchem.7b01812. Epub 2018 Mar 23. J Med Chem. 2018. PMID: 29544056
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. Jörg M, et al. Among authors: van der westhuizen et. ACS Chem Neurosci. 2019 Mar 20;10(3):1099-1114. doi: 10.1021/acschemneuro.8b00613. Epub 2018 Dec 28. ACS Chem Neurosci. 2019. PMID: 30547573 Free PMC article.
Development of Novel 4-Arylpyridin-2-one and 6-Arylpyrimidin-4-one Positive Allosteric Modulators of the M1 Muscarinic Acetylcholine Receptor.
Jörg M, Khajehali E, van der Westhuizen ET, C Choy KH, Shackleford DM, Tobin AB, Sexton PM, Valant C, Capuano B, Christopoulos A, Scammells PJ. Jörg M, et al. Among authors: van der westhuizen et. ChemMedChem. 2021 Jan 8;16(1):216-233. doi: 10.1002/cmdc.202000540. Epub 2020 Sep 25. ChemMedChem. 2021. PMID: 32851779 Free PMC article.
Endogenous allosteric modulators of G protein-coupled receptors.
van der Westhuizen ET, Valant C, Sexton PM, Christopoulos A. van der Westhuizen ET, et al. J Pharmacol Exp Ther. 2015 May;353(2):246-60. doi: 10.1124/jpet.114.221606. Epub 2015 Feb 3. J Pharmacol Exp Ther. 2015. PMID: 25650376 Review.
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. van der Westhuizen ET, et al. Mol Pharmacol. 2018 Jul;94(1):770-783. doi: 10.1124/mol.118.111633. Epub 2018 Apr 24. Mol Pharmacol. 2018. PMID: 29691279 Free PMC article.
Crystal structure of the M5 muscarinic acetylcholine receptor.
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, Christopoulos A, Thal DM. Vuckovic Z, et al. Among authors: van der westhuizen et. Proc Natl Acad Sci U S A. 2019 Dec 17;116(51):26001-26007. doi: 10.1073/pnas.1914446116. Epub 2019 Nov 26. Proc Natl Acad Sci U S A. 2019. PMID: 31772027 Free PMC article.
Restoring Agonist Function at a Chemogenetically Modified M1 Muscarinic Acetylcholine Receptor.
Khajehali E, Bradley S, van der Westhuizen ET, Molloy C, Valant C, Finlayson L, Lindsley CW, Sexton PM, Tobin AB, Christopoulos A. Khajehali E, et al. Among authors: van der westhuizen et. ACS Chem Neurosci. 2020 Dec 16;11(24):4270-4279. doi: 10.1021/acschemneuro.0c00540. Epub 2020 Nov 16. ACS Chem Neurosci. 2020. PMID: 33196174 Free PMC article.
Identification of a Novel Allosteric Site at the M5 Muscarinic Acetylcholine Receptor.
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. Burger WAC, et al. Among authors: van der westhuizen et. ACS Chem Neurosci. 2021 Aug 18;12(16):3112-3123. doi: 10.1021/acschemneuro.1c00383. Epub 2021 Aug 5. ACS Chem Neurosci. 2021. PMID: 34351123 Free PMC article.
28 results