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Phase 1 and preclinical profiling of ESM-HDAC391, a myeloid-targeted histone deacetylase inhibitor, shows enhanced pharmacology and monocytopaenia.
Furze RC, Molnar J, Parr NJ, Ahmad F, Henry Y, Howe D, Singh R, Toal M, Bassil AK, Bernard SG, Davis RP, Gibson A, Maller NC, Sharp C, Tough DF, Prinjha RK, Lewis HD. Furze RC, et al. Among authors: bernard sg. Br J Clin Pharmacol. 2022 Dec;88(12):5238-5256. doi: 10.1111/bcp.15428. Epub 2022 Jul 11. Br J Clin Pharmacol. 2022. PMID: 35655123 Free PMC article. Clinical Trial.
Targeting Histone Deacetylases in Myeloid Cells Inhibits Their Maturation and Inflammatory Function With Limited Effects on Atherosclerosis.
Luque-Martin R, Van den Bossche J, Furze RC, Neele AE, van der Velden S, Gijbels MJJ, van Roomen CPPA, Bernard SG, de Jonge WJ, Rioja I, Prinjha RK, Lewis HD, Mander PK, de Winther MPJ. Luque-Martin R, et al. Among authors: bernard sg. Front Pharmacol. 2019 Oct 29;10:1242. doi: 10.3389/fphar.2019.01242. eCollection 2019. Front Pharmacol. 2019. PMID: 31736752 Free PMC article.
Discovery of a Novel Bromodomain and Extra Terminal Domain (BET) Protein Inhibitor, I-BET282E, Suitable for Clinical Progression.
Jones KL, Beaumont DM, Bernard SG, Bit RA, Campbell SP, Chung CW, Cutler L, Demont EH, Dennis K, Gordon L, Gray JR, Haase MV, Lewis AJ, McCleary S, Mitchell DJ, Moore SM, Parr N, Robb OJ, Smithers N, Soden PE, Suckling CJ, Taylor S, Walker AL, Watson RJ, Prinjha RK. Jones KL, et al. Among authors: bernard sg. J Med Chem. 2021 Aug 26;64(16):12200-12227. doi: 10.1021/acs.jmedchem.1c00855. Epub 2021 Aug 13. J Med Chem. 2021. PMID: 34387088
IFN-γ Drives Human Monocyte Differentiation into Highly Proinflammatory Macrophages That Resemble a Phenotype Relevant to Psoriasis.
Luque-Martin R, Angell DC, Kalxdorf M, Bernard S, Thompson W, Eberl HC, Ashby C, Freudenberg J, Sharp C, Van den Bossche J, de Jonge WJ, Rioja I, Prinjha RK, Neele AE, de Winther MPJ, Mander PK. Luque-Martin R, et al. J Immunol. 2021 Jul 15;207(2):555-568. doi: 10.4049/jimmunol.2001310. Epub 2021 Jul 7. J Immunol. 2021. PMID: 34233910
Pharmacological validation of targets regulating CD14 during macrophage differentiation.
Jimenez-Duran G, Luque-Martin R, Patel M, Koppe E, Bernard S, Sharp C, Buchan N, Rea C, de Winther MPJ, Turan N, Angell D, Wells CA, Cousins R, Mander PK, Masters SL. Jimenez-Duran G, et al. EBioMedicine. 2020 Nov;61:103039. doi: 10.1016/j.ebiom.2020.103039. Epub 2020 Oct 7. EBioMedicine. 2020. PMID: 33038762 Free PMC article.
Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype.
Wellaway CR, Bamborough P, Bernard SG, Chung CW, Craggs PD, Cutler L, Demont EH, Evans JP, Gordon L, Karamshi B, Lewis AJ, Lindon MJ, Mitchell DJ, Rioja I, Soden PE, Taylor S, Watson RJ, Willis R, Woolven JM, Wyspiańska BS, Kerr WJ, Prinjha RK. Wellaway CR, et al. Among authors: bernard sg. J Med Chem. 2020 Sep 10;63(17):9020-9044. doi: 10.1021/acs.jmedchem.0c00566. Epub 2020 Aug 3. J Med Chem. 2020. PMID: 32787145 Free article.