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A conserved salt bridge in the G loop of multiple protein kinases is important for catalysis and for in vivo Lyn function.
Barouch-Bentov R, Che J, Lee CC, Yang Y, Herman A, Jia Y, Velentza A, Watson J, Sternberg L, Kim S, Ziaee N, Miller A, Jackson C, Fujimoto M, Young M, Batalov S, Liu Y, Warmuth M, Wiltshire T, Cooke MP, Sauer K. Barouch-Bentov R, et al. Among authors: warmuth m. Mol Cell. 2009 Jan 16;33(1):43-52. doi: 10.1016/j.molcel.2008.12.024. Mol Cell. 2009. PMID: 19150426 Free PMC article.
Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.
Hur W, Velentza A, Kim S, Flatauer L, Jiang X, Valente D, Mason DE, Suzuki M, Larson B, Zhang J, Zagorska A, Didonato M, Nagle A, Warmuth M, Balk SP, Peters EC, Gray NS. Hur W, et al. Among authors: warmuth m. Bioorg Med Chem Lett. 2008 Nov 15;18(22):5916-9. doi: 10.1016/j.bmcl.2008.07.062. Epub 2008 Jul 18. Bioorg Med Chem Lett. 2008. PMID: 18667312 Free PMC article.
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.
Galkin AV, Melnick JS, Kim S, Hood TL, Li N, Li L, Xia G, Steensma R, Chopiuk G, Jiang J, Wan Y, Ding P, Liu Y, Sun F, Schultz PG, Gray NS, Warmuth M. Galkin AV, et al. Among authors: warmuth m. Proc Natl Acad Sci U S A. 2007 Jan 2;104(1):270-5. doi: 10.1073/pnas.0609412103. Epub 2006 Dec 21. Proc Natl Acad Sci U S A. 2007. PMID: 17185414 Free PMC article.
Allosteric inhibition of BCR-ABL.
Hassan AQ, Sharma SV, Warmuth M. Hassan AQ, et al. Among authors: warmuth m. Cell Cycle. 2010 Sep 15;9(18):3710-4. doi: 10.4161/cc.9.18.13232. Epub 2010 Sep 3. Cell Cycle. 2010. PMID: 20930519 Review.
Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials.
Marsilje TH, Pei W, Chen B, Lu W, Uno T, Jin Y, Jiang T, Kim S, Li N, Warmuth M, Sarkisova Y, Sun F, Steffy A, Pferdekamper AC, Li AG, Joseph SB, Kim Y, Liu B, Tuntland T, Cui X, Gray NS, Steensma R, Wan Y, Jiang J, Chopiuk G, Li J, Gordon WP, Richmond W, Johnson K, Chang J, Groessl T, He YQ, Phimister A, Aycinena A, Lee CC, Bursulaya B, Karanewsky DS, Seidel HM, Harris JL, Michellys PY. Marsilje TH, et al. Among authors: warmuth m. J Med Chem. 2013 Jul 25;56(14):5675-90. doi: 10.1021/jm400402q. Epub 2013 Jun 26. J Med Chem. 2013. PMID: 23742252
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
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
87 results