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Page 1
Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors.
Zhang J, Adrián FJ, Jahnke W, Cowan-Jacob SW, Li AG, Iacob RE, Sim T, Powers J, Dierks C, Sun F, Guo GR, Ding Q, Okram B, Choi Y, Wojciechowski A, Deng X, Liu G, Fendrich G, Strauss A, Vajpai N, Grzesiek S, Tuntland T, Liu Y, Bursulaya B, Azam M, Manley PW, Engen JR, Daley GQ, Warmuth M, Gray NS. Zhang J, et al. Among authors: warmuth m. Nature. 2010 Jan 28;463(7280):501-6. doi: 10.1038/nature08675. Epub 2010 Jan 13. Nature. 2010. PMID: 20072125 Free PMC article.
The allosteric inhibitor ABL001 enables dual targeting of BCR-ABL1.
Wylie AA, Schoepfer J, Jahnke W, Cowan-Jacob SW, Loo A, Furet P, Marzinzik AL, Pelle X, Donovan J, Zhu W, Buonamici S, Hassan AQ, Lombardo F, Iyer V, Palmer M, Berellini G, Dodd S, Thohan S, Bitter H, Branford S, Ross DM, Hughes TP, Petruzzelli L, Vanasse KG, Warmuth M, Hofmann F, Keen NJ, Sellers WR. Wylie AA, et al. Among authors: warmuth m. Nature. 2017 Mar 30;543(7647):733-737. doi: 10.1038/nature21702. Epub 2017 Mar 22. Nature. 2017. PMID: 28329763
Inhibitors of the Abl kinase directed at either the ATP- or myristate-binding site.
Fabbro D, Manley PW, Jahnke W, Liebetanz J, Szyttenholm A, Fendrich G, Strauss A, Zhang J, Gray NS, Adrian F, Warmuth M, Pelle X, Grotzfeld R, Berst F, Marzinzik A, Cowan-Jacob SW, Furet P, Mestan J. Fabbro D, et al. Among authors: warmuth m. Biochim Biophys Acta. 2010 Mar;1804(3):454-62. doi: 10.1016/j.bbapap.2009.12.009. Biochim Biophys Acta. 2010. PMID: 20152788
A general strategy for creating "inactive-conformation" abl inhibitors.
Okram B, Nagle A, Adrián FJ, Lee C, Ren P, Wang X, Sim T, Xie Y, Wang X, Xia G, Spraggon G, Warmuth M, Liu Y, Gray NS. Okram B, et al. Among authors: warmuth m. Chem Biol. 2006 Jul;13(7):779-86. doi: 10.1016/j.chembiol.2006.05.015. Chem Biol. 2006. PMID: 16873026
Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1.
Schoepfer J, Jahnke W, Berellini G, Buonamici S, Cotesta S, Cowan-Jacob SW, Dodd S, Drueckes P, Fabbro D, Gabriel T, Groell JM, Grotzfeld RM, Hassan AQ, Henry C, Iyer V, Jones D, Lombardo F, Loo A, Manley PW, Pellé X, Rummel G, Salem B, Warmuth M, Wylie AA, Zoller T, Marzinzik AL, Furet P. Schoepfer J, et al. Among authors: warmuth m. J Med Chem. 2018 Sep 27;61(18):8120-8135. doi: 10.1021/acs.jmedchem.8b01040. Epub 2018 Sep 7. J Med Chem. 2018. PMID: 30137981
Ba/F3 cells and their use in kinase drug discovery.
Warmuth M, Kim S, Gu XJ, Xia G, Adrián F. Warmuth M, et al. Curr Opin Oncol. 2007 Jan;19(1):55-60. doi: 10.1097/CCO.0b013e328011a25f. Curr Opin Oncol. 2007. PMID: 17133113 Review.
87 results