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Synthesis and SAR of novel GPR39 agonists and positive allosteric modulators.
Burley R, Hewer RC, Teall M, Dickson L, Ossola B, Russell S, Bender C, Cheung T, Powell JAC, Xu X, Brice NL, Otter L, Arimont M, Kidd SL, Vidal D, Dale JW, Mervin L, Sore HF, Mateu N, Lakshminarayana N, Dawson LA, Carlton M, Bürli RW. Burley R, et al. Among authors: cheung t. Bioorg Med Chem Lett. 2022 Apr 1;61:128607. doi: 10.1016/j.bmcl.2022.128607. Epub 2022 Feb 3. Bioorg Med Chem Lett. 2022. PMID: 35123006
Development of CVN424: A Selective and Novel GPR6 Inverse Agonist Effective in Models of Parkinson Disease.
Brice NL, Schiffer HH, Monenschein H, Mulligan VJ, Page K, Powell J, Xu X, Cheung T, Burley JR, Sun H, Dickson L, Murphy ST, Kaushal N, Sheardown S, Lawrence J, Chen Y, Bartkowski D, Kanta A, Russo J, Hosea N, Dawson LA, Hitchcock SH, Carlton MB. Brice NL, et al. Among authors: cheung t. J Pharmacol Exp Ther. 2021 Jun;377(3):407-416. doi: 10.1124/jpet.120.000438. Epub 2021 Apr 1. J Pharmacol Exp Ther. 2021. PMID: 33795395
Characterisation of C101248: A novel selective THIK-1 channel inhibitor for the modulation of microglial NLRP3-inflammasome.
Ossola B, Rifat A, Rowland A, Hunter H, Drinkall S, Bender C, Hamlischer M, Teall M, Burley R, Barker DF, Cadwalladr D, Dickson L, Lawrence JMK, Harvey JRM, Lizio M, Xu X, Kavanagh E, Cheung T, Sheardown S, Lawrence CB, Harte M, Brough D, Madry C, Matthews K, Doyle K, Page K, Powell J, Brice NL, Bürli RW, Carlton MB, Dawson LA. Ossola B, et al. Among authors: cheung t. Neuropharmacology. 2023 Feb 15;224:109330. doi: 10.1016/j.neuropharm.2022.109330. Epub 2022 Nov 12. Neuropharmacology. 2023. PMID: 36375694 Free PMC article.
Discovery of CVN636: A Highly Potent, Selective, and CNS Penetrant mGluR7 Allosteric Agonist.
Dickson L, Teall M, Chevalier E, Cheung T, Liwicki GM, Mack S, Stephenson A, White K, Fosbeary R, Harrison DC, Brice NL, Doyle K, Ciccocioppo R, Wu C, Almond S, Patel TR, Mitchell P, Barnes M, Ayscough AP, Dawson LA, Carlton M, Bürli RW. Dickson L, et al. Among authors: cheung t. ACS Med Chem Lett. 2023 Mar 2;14(4):442-449. doi: 10.1021/acsmedchemlett.2c00529. eCollection 2023 Apr 13. ACS Med Chem Lett. 2023. PMID: 37077399 Free PMC article.
Discovery and Characterization of Novel CNS-Penetrant GPR55 Agonists.
Hewer RC, Christie LA, Doyle KJ, Xu X, Roberts MJ, Dickson L, Cheung T, Cadwalladr DH, Pickford P, Teall M, Powell JAC, Sheardown S, Narayana L, Brice NL, Dawson LA, Carlton M, Bürli RW. Hewer RC, et al. Among authors: cheung t. J Med Chem. 2023 Sep 28;66(18):12858-12876. doi: 10.1021/acs.jmedchem.3c00784. Epub 2023 Sep 14. J Med Chem. 2023. PMID: 37708305
Mechanistic safety assessment via multi-omic characterisation of systemic pathway perturbations following in vivo MAT2A inhibition.
Fogal V, Michopoulos F, Jarnuczak AF, Hamza GM, Harlfinger S, Davey P, Hulme H, Atkinson SJ, Gabrowski P, Cheung T, Grondine M, Hoover C, Rose J, Bray C, Foster AJ, Askin S, Majumder MM, Fitzpatrick P, Miele E, Macdonald R, Keun HC, Coen M. Fogal V, et al. Among authors: cheung t. Arch Toxicol. 2024 May 17. doi: 10.1007/s00204-024-03771-w. Online ahead of print. Arch Toxicol. 2024. PMID: 38755480
1,339 results