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Identification of a Potent, Selective, and Brain-Penetrant Rho Kinase Inhibitor and its Activity in a Mouse Model of Huntington's Disease.
Ladduwahetty T, Lee MR, Maillard MC, Cachope R, Todd D, Barnes M, Beaumont V, Chauhan A, Gallati C, Haughan AF, Kempf G, Luckhurst CA, Matthews K, McAllister G, Mitchell P, Patel H, Rose M, Saville-Stones E, Steinbacher S, Stott AJ, Thatcher E, Tierney J, Urbonas L, Munoz-Sanjuan I, Dominguez C. Ladduwahetty T, et al. Among authors: beaumont v. J Med Chem. 2022 Jul 28;65(14):9819-9845. doi: 10.1021/acs.jmedchem.2c00474. Epub 2022 Jul 11. J Med Chem. 2022. PMID: 35816678
Design, synthesis, and biological evaluation of potent and selective class IIa histone deacetylase (HDAC) inhibitors as a potential therapy for Huntington's disease.
Bürli RW, Luckhurst CA, Aziz O, Matthews KL, Yates D, Lyons KA, Beconi M, McAllister G, Breccia P, Stott AJ, Penrose SD, Wall M, Lamers M, Leonard P, Müller I, Richardson CM, Jarvis R, Stones L, Hughes S, Wishart G, Haughan AF, O'Connell C, Mead T, McNeil H, Vann J, Mangette J, Maillard M, Beaumont V, Munoz-Sanjuan I, Dominguez C. Bürli RW, et al. Among authors: beaumont v. J Med Chem. 2013 Dec 27;56(24):9934-54. doi: 10.1021/jm4011884. Epub 2013 Dec 5. J Med Chem. 2013. PMID: 24261862
Development and characterization of a CNS-penetrant benzhydryl hydroxamic acid class IIa histone deacetylase inhibitor.
Luckhurst CA, Aziz O, Beaumont V, Bürli RW, Breccia P, Maillard MC, Haughan AF, Lamers M, Leonard P, Matthews KL, Raphy G, Stott AJ, Munoz-Sanjuan I, Thomas B, Wall M, Wishart G, Yates D, Dominguez C. Luckhurst CA, et al. Among authors: beaumont v. Bioorg Med Chem Lett. 2019 Jan 1;29(1):83-88. doi: 10.1016/j.bmcl.2018.11.009. Epub 2018 Nov 13. Bioorg Med Chem Lett. 2019. PMID: 30463802
Evaluation of 5-(Trifluoromethyl)-1,2,4-oxadiazole-Based Class IIa HDAC Inhibitors for Huntington's Disease.
Stott AJ, Maillard MC, Beaumont V, Allcock D, Aziz O, Borchers AH, Blackaby W, Breccia P, Creighton-Gutteridge G, Haughan AF, Jarvis RE, Luckhurst CA, Matthews KL, McAllister G, Pollack S, Saville-Stones E, Van de Poël AJ, Vater HD, Vann J, Williams R, Yates D, Muñoz-Sanjuán I, Dominguez C. Stott AJ, et al. Among authors: beaumont v. ACS Med Chem Lett. 2021 Feb 11;12(3):380-388. doi: 10.1021/acsmedchemlett.0c00532. eCollection 2021 Mar 11. ACS Med Chem Lett. 2021. PMID: 33738065 Free PMC article.
Developing HDAC4-Selective Protein Degraders To Investigate the Role of HDAC4 in Huntington's Disease Pathology.
Macabuag N, Esmieu W, Breccia P, Jarvis R, Blackaby W, Lazari O, Urbonas L, Eznarriaga M, Williams R, Strijbosch A, Van de Bospoort R, Matthews K, Clissold C, Ladduwahetty T, Vater H, Heaphy P, Stafford DG, Wang HJ, Mangette JE, McAllister G, Beaumont V, Vogt TF, Wilkinson HA, Doherty EM, Dominguez C. Macabuag N, et al. Among authors: beaumont v. J Med Chem. 2022 Sep 22;65(18):12445-12459. doi: 10.1021/acs.jmedchem.2c01149. Epub 2022 Sep 13. J Med Chem. 2022. PMID: 36098485 Free PMC article.
Oral administration of the pimelic diphenylamide HDAC inhibitor HDACi 4b is unsuitable for chronic inhibition of HDAC activity in the CNS in vivo.
Beconi M, Aziz O, Matthews K, Moumné L, O'Connell C, Yates D, Clifton S, Pett H, Vann J, Crowley L, Haughan AF, Smith DL, Woodman B, Bates GP, Brookfield F, Bürli RW, McAllister G, Dominguez C, Munoz-Sanjuan I, Beaumont V. Beconi M, et al. Among authors: beaumont v. PLoS One. 2012;7(9):e44498. doi: 10.1371/journal.pone.0044498. Epub 2012 Sep 4. PLoS One. 2012. PMID: 22973455 Free PMC article.
Unravelling and Exploiting Astrocyte Dysfunction in Huntington's Disease.
Khakh BS, Beaumont V, Cachope R, Munoz-Sanjuan I, Goldman SA, Grantyn R. Khakh BS, et al. Among authors: beaumont v. Trends Neurosci. 2017 Jul;40(7):422-437. doi: 10.1016/j.tins.2017.05.002. Epub 2017 May 31. Trends Neurosci. 2017. PMID: 28578789 Free PMC article. Review.
The novel KMO inhibitor CHDI-340246 leads to a restoration of electrophysiological alterations in mouse models of Huntington's disease.
Beaumont V, Mrzljak L, Dijkman U, Freije R, Heins M, Rassoulpour A, Tombaugh G, Gelman S, Bradaia A, Steidl E, Gleyzes M, Heikkinen T, Lehtimäki K, Puoliväli J, Kontkanen O, Javier RM, Neagoe I, Deisemann H, Winkler D, Ebneth A, Khetarpal V, Toledo-Sherman L, Dominguez C, Park LC, Munoz-Sanjuan I. Beaumont V, et al. Exp Neurol. 2016 Aug;282:99-118. doi: 10.1016/j.expneurol.2016.05.005. Epub 2016 May 6. Exp Neurol. 2016. PMID: 27163548
The PDE1/5 Inhibitor SCH-51866 Does Not Modify Disease Progression in the R6/2 Mouse Model of Huntington's Disease.
Beaumont V, Park L, Rassoulpour A, Dijkman U, Heikkinen T, Lehtimaki K, Kontkanen O, Al Nackkash R, Bates GP, Gleyzes M, Steidl E, Ramboz S, Murphy C, Beconi MG, Dominguez C, Munoz-Sanjuan I. Beaumont V, et al. PLoS Curr. 2014 Feb 13;6:ecurrents.hd.3304e87e460b4bb0dc519a29f4deccca. doi: 10.1371/currents.hd.3304e87e460b4bb0dc519a29f4deccca. PLoS Curr. 2014. PMID: 24558637 Free PMC article.
138 results