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Discovery of (2,4-dihydroxy-5-isopropylphenyl)-[5-(4-methylpiperazin-1-ylmethyl)-1,3-dihydroisoindol-2-yl]methanone (AT13387), a novel inhibitor of the molecular chaperone Hsp90 by fragment based drug design.
Woodhead AJ, Angove H, Carr MG, Chessari G, Congreve M, Coyle JE, Cosme J, Graham B, Day PJ, Downham R, Fazal L, Feltell R, Figueroa E, Frederickson M, Lewis J, McMenamin R, Murray CW, O'Brien MA, Parra L, Patel S, Phillips T, Rees DC, Rich S, Smith DM, Trewartha G, Vinkovic M, Williams B, Woolford AJ. Woodhead AJ, et al. Among authors: downham r. J Med Chem. 2010 Aug 26;53(16):5956-69. doi: 10.1021/jm100060b. J Med Chem. 2010. PMID: 20662534
1,2,4-Triazolo-[1,5-a]pyridine HIF Prolylhydroxylase Domain-1 (PHD-1) Inhibitors With a Novel Monodentate Binding Interaction.
Ahmed S, Ayscough A, Barker GR, Canning HE, Davenport R, Downham R, Harrison D, Jenkins K, Kinsella N, Livermore DG, Wright S, Ivetac AD, Skene R, Wilkens SJ, Webster NA, Hendrick AG. Ahmed S, et al. Among authors: downham r. J Med Chem. 2017 Jul 13;60(13):5663-5672. doi: 10.1021/acs.jmedchem.7b00352. Epub 2017 Jun 24. J Med Chem. 2017. PMID: 28594552
Preclinical trial of a MAP4K4 inhibitor to reduce infarct size in the pig: does cardioprotection in human stem cell-derived myocytes predict success in large mammals?
Te Lintel Hekkert M, Newton G, Chapman K, Aqil R, Downham R, Yan R, Merkus D, Whitlock G, Lane CAL, Cawkill D, Perrior T, Duncker DJ, Schneider MD. Te Lintel Hekkert M, et al. Among authors: downham r. Basic Res Cardiol. 2021 May 20;116(1):34. doi: 10.1007/s00395-021-00875-7. Basic Res Cardiol. 2021. PMID: 34018053 Free PMC article.
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