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ASTX029, a Novel Dual-mechanism ERK Inhibitor, Modulates Both the Phosphorylation and Catalytic Activity of ERK.
Munck JM, Berdini V, Bevan L, Brothwood JL, Castro J, Courtin A, East C, Ferraldeschi R, Heightman TD, Hindley CJ, Kucia-Tran J, Lyons JF, Martins V, Muench S, Murray CW, Norton D, O'Reilly M, Reader M, Rees DC, Rich SJ, Richardson CJ, Shah AD, Stanczuk L, Thompson NT, Wilsher NE, Woolford AJ, Wallis NG. Munck JM, et al. Among authors: thompson nt. Mol Cancer Ther. 2021 Oct;20(10):1757-1768. doi: 10.1158/1535-7163.MCT-20-0909. Epub 2021 Jul 30. Mol Cancer Ther. 2021. PMID: 34330842
The HSP90 inhibitor, AT13387, is effective against imatinib-sensitive and -resistant gastrointestinal stromal tumor models.
Smyth T, Van Looy T, Curry JE, Rodriguez-Lopez AM, Wozniak A, Zhu M, Donsky R, Morgan JG, Mayeda M, Fletcher JA, Schöffski P, Lyons J, Thompson NT, Wallis NG. Smyth T, et al. Among authors: thompson nt. Mol Cancer Ther. 2012 Aug;11(8):1799-808. doi: 10.1158/1535-7163.MCT-11-1046. Epub 2012 Jun 19. Mol Cancer Ther. 2012. PMID: 22714264 Free PMC article.
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. Among authors: thompson nt. 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.
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: thompson nt. 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
Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2.
Heightman TD, Berdini V, Braithwaite H, Buck IM, Cassidy M, Castro J, Courtin A, Day JEH, East C, Fazal L, Graham B, Griffiths-Jones CM, Lyons JF, Martins V, Muench S, Munck JM, Norton D, O'Reilly M, Palmer N, Pathuri P, Reader M, Rees DC, Rich SJ, Richardson C, Saini H, Thompson NT, Wallis NG, Walton H, Wilsher NE, Woolford AJ, Cooke M, Cousin D, Onions S, Shannon J, Watts J, Murray CW. Heightman TD, et al. Among authors: thompson nt. J Med Chem. 2018 Jun 14;61(11):4978-4992. doi: 10.1021/acs.jmedchem.8b00421. Epub 2018 May 31. J Med Chem. 2018. PMID: 29775310
AT7867 is a potent and oral inhibitor of AKT and p70 S6 kinase that induces pharmacodynamic changes and inhibits human tumor xenograft growth.
Grimshaw KM, Hunter LJ, Yap TA, Heaton SP, Walton MI, Woodhead SJ, Fazal L, Reule M, Davies TG, Seavers LC, Lock V, Lyons JF, Thompson NT, Workman P, Garrett MD. Grimshaw KM, et al. Among authors: thompson nt. Mol Cancer Ther. 2010 May;9(5):1100-10. doi: 10.1158/1535-7163.MCT-09-0986. Epub 2010 Apr 27. Mol Cancer Ther. 2010. PMID: 20423992 Free PMC article.
51 results