Centre Publications
The roles of RGS proteins in cardiometabolic disease.
McNeill SM, Zhao P (2024). Br J Pharmacol, 181(14): 2319-2337 (2024). doi: 10.1111/bph.16076.
Molecular insights into orphan G protein-coupled receptors relevant to schizophrenia.
Lu Y, Hatzipantelis CJ, Langmead CJ, Stewart GD (2024). Br J Pharmacol, 181(14): 2095-2113. doi: 10.1111/bph.16221.
The role of the adenosine system in epilepsy and its comorbidities.
Baltos J-A, Casillas-Espinosa PM, Rollo B, Gregory KJ, White, PJ, Christopoulos A, Kwan P, O’Brien TJ, May,LT (2024). Br J Pharmacol, 181(14): 2143-2157. doi: 10.1111/bph.16094.
Isoquinoline small molecule ligands are agonists and probe-dependent allosteric modulators of the glucagon subfamily of GPCRs.
Yuliante E, Trinh PNH, Hick C, Ebenhoch R, Nar H, Weichert D, Christopoulos, A, Sexton PM, Wootten D (2024). Biochem Pharmacol (in press). with industry partner Boehringer Ingelheim. [Preprint SSRN Elsevier (22 May 2024)] https://papers.ssrn.com/sol3/papers.cfm?abstract_id=4831303.
Discovery and development of macrocyclic peptide modulators of the cannabinoid 2 receptor.
Tomašević N, Emser FS, Muratspahić E, Gattringer J, Hasinger S, Hellinger R, Keov, P, Felkl M, Gertsch J, Becker CFW, Gruber CW (2024). J Biol Chem 300(6):107330 (2024). DOI: https://doi.org/10.1016/j.jbc.2024.107330
MORC2 phosphorylation fine tunes its DNA compaction activity.
Tan W, Park JV, Venugopal H, Lou JQ, Dias PS, Baldoni PL, Dite T, Moon K-W, Keenan CR, Gurzau AD, Leis A, Yousef J, Vaibhav V, Dagley LF, Ang C-S, Corso L, Davidovich C, Vervoort SJ, Smyth GS, Blewitt ME, Allan RS, Hinde H, D’Arcy S, Ryu J-K, Shakeel S. bioRxiv (28 June 2024) doi: https://doi.org/10.1101/2024.06.27.600912
Trace amine associated receptor 1: predicted effects of single nucleotide variants on structure-function in geographically diverse populations.
Shajan B, Marri S, Bastiampillai T, Gregory KJ, Hellyer SD, Nair PC (2024). Human Genomics, 18(1): 61. doi: 10.1186/s40246-024-00620-w.
Development of putative bivalent dicovalent ligands for the adenosine A1 receptor.
Payne CM, Baltos J-A, Langiu M, Lu CS, Tyndall JDA, Gregory KJ, May LT, Vernall AJ. ChemBioChem, 22 May 2024 online ahead of print. https://doi.org/10.1002/cbic.202400242
Discovery of 2-methyl-5-(1H-pyrazol-4-yl)pyridines and related heterocycles as promising M4 mAChR positive allosteric modulators for the treatment of neurocognitive disorders.
Liu B, Thompson G, Manuela J Barnes N, Thal D, Christopoulos A, Capuano B, Valant C, Scammells P. J Med Chem (accepted).
Development of a novel assay for direct assessment of selective amylin receptor activation reveals novel differences in behaviour of selective and non-selective peptide agonists.
Keov P, Christopoulos G, Hick CA, Glendorf T, Ballarín-González B, Wootten D, Sexton PM (2024). Mol Pharmacol 105(5): 359-373. with industry partner Novo Nordisk DOI: https://doi.org/10.1124/molpharm.123.000865