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Inhibition of HSP90 by AT13387 delays the emergence of resistance to BRAF inhibitors and overcomes resistance to dual BRAF and MEK inhibition in melanoma models.
Smyth T, Paraiso KHT, Hearn K, Rodriguez-Lopez AM, Munck JM, Haarberg HE, Sondak VK, Thompson NT, Azab M, Lyons JF, Smalley KSM, Wallis NG. Smyth T, et al. Mol Cancer Ther. 2014 Dec;13(12):2793-2804. doi: 10.1158/1535-7163.MCT-14-0452. Epub 2014 Oct 27. Mol Cancer Ther. 2014. PMID: 25349308 Free PMC article.
Second-Generation HSP90 Inhibitor Onalespib Blocks mRNA Splicing of Androgen Receptor Variant 7 in Prostate Cancer Cells.
Ferraldeschi R, Welti J, Powers MV, Yuan W, Smyth T, Seed G, Riisnaes R, Hedayat S, Wang H, Crespo M, Nava Rodrigues D, Figueiredo I, Miranda S, Carreira S, Lyons JF, Sharp S, Plymate SR, Attard G, Wallis N, Workman P, de Bono JS. Ferraldeschi R, et al. Among authors: smyth t. Cancer Res. 2016 May 1;76(9):2731-42. doi: 10.1158/0008-5472.CAN-15-2186. Cancer Res. 2016. PMID: 27197266 Free PMC article.
ASTX660, a Novel Non-peptidomimetic Antagonist of cIAP1/2 and XIAP, Potently Induces TNFα-Dependent Apoptosis in Cancer Cell Lines and Inhibits Tumor Growth.
Ward GA, Lewis EJ, Ahn JS, Johnson CN, Lyons JF, Martins V, Munck JM, Rich SJ, Smyth T, Thompson NT, Williams PA, Wilsher NE, Wallis NG, Chessari G. Ward GA, et al. Among authors: smyth t. Mol Cancer Ther. 2018 Jul;17(7):1381-1391. doi: 10.1158/1535-7163.MCT-17-0848. Epub 2018 Apr 25. Mol Cancer Ther. 2018. PMID: 29695633
A Fragment-Derived Clinical Candidate for Antagonism of X-Linked and Cellular Inhibitor of Apoptosis Proteins: 1-(6-[(4-Fluorophenyl)methyl]-5-(hydroxymethyl)-3,3-dimethyl-1 H,2 H,3 H-pyrrolo[3,2- b]pyridin-1-yl)-2-[(2 R,5 R)-5-methyl-2-([(3R)-3-methylmorpholin-4-yl]methyl)piperazin-1-yl]ethan-1-one (ASTX660).
Johnson CN, Ahn JS, Buck IM, Chiarparin E, Day JEH, Hopkins A, Howard S, Lewis EJ, Martins V, Millemaggi A, Munck JM, Page LW, Peakman T, Reader M, Rich SJ, Saxty G, Smyth T, Thompson NT, Ward GA, Williams PA, Wilsher NE, Chessari G. Johnson CN, et al. Among authors: smyth t. J Med Chem. 2018 Aug 23;61(16):7314-7329. doi: 10.1021/acs.jmedchem.8b00900. Epub 2018 Aug 9. J Med Chem. 2018. PMID: 30091600
205 results