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Synthesis and optimization of thiadiazole derivatives as a novel class of substrate competitive c-Jun N-terminal kinase inhibitors.
De SK, Chen V, Stebbins JL, Chen LH, Cellitti JF, Machleidt T, Barile E, Riel-Mehan M, Dahl R, Yang L, Emdadi A, Murphy R, Pellecchia M. De SK, et al. Among authors: machleidt t. Bioorg Med Chem. 2010 Jan 15;18(2):590-6. doi: 10.1016/j.bmc.2009.12.013. Epub 2009 Dec 11. Bioorg Med Chem. 2010. PMID: 20045647 Free PMC article.
Identification of a new JNK inhibitor targeting the JNK-JIP interaction site.
Stebbins JL, De SK, Machleidt T, Becattini B, Vazquez J, Kuntzen C, Chen LH, Cellitti JF, Riel-Mehan M, Emdadi A, Solinas G, Karin M, Pellecchia M. Stebbins JL, et al. Among authors: machleidt t. Proc Natl Acad Sci U S A. 2008 Oct 28;105(43):16809-13. doi: 10.1073/pnas.0805677105. Epub 2008 Oct 15. Proc Natl Acad Sci U S A. 2008. PMID: 18922779 Free PMC article.
Design, synthesis, and structure-activity relationship of substrate competitive, selective, and in vivo active triazole and thiadiazole inhibitors of the c-Jun N-terminal kinase.
De SK, Stebbins JL, Chen LH, Riel-Mehan M, Machleidt T, Dahl R, Yuan H, Emdadi A, Barile E, Chen V, Murphy R, Pellecchia M. De SK, et al. Among authors: machleidt t. J Med Chem. 2009 Apr 9;52(7):1943-52. doi: 10.1021/jm801503n. J Med Chem. 2009. PMID: 19271755 Free PMC article.
Discovery of potent and selective covalent inhibitors of JNK.
Zhang T, Inesta-Vaquera F, Niepel M, Zhang J, Ficarro SB, Machleidt T, Xie T, Marto JA, Kim N, Sim T, Laughlin JD, Park H, LoGrasso PV, Patricelli M, Nomanbhoy TK, Sorger PK, Alessi DR, Gray NS. Zhang T, et al. Among authors: machleidt t. Chem Biol. 2012 Jan 27;19(1):140-54. doi: 10.1016/j.chembiol.2011.11.010. Chem Biol. 2012. PMID: 22284361 Free PMC article.
Quantitative, Wide-Spectrum Kinase Profiling in Live Cells for Assessing the Effect of Cellular ATP on Target Engagement.
Vasta JD, Corona CR, Wilkinson J, Zimprich CA, Hartnett JR, Ingold MR, Zimmerman K, Machleidt T, Kirkland TA, Huwiler KG, Ohana RF, Slater M, Otto P, Cong M, Wells CI, Berger BT, Hanke T, Glas C, Ding K, Drewry DH, Huber KVM, Willson TM, Knapp S, Müller S, Meisenheimer PL, Fan F, Wood KV, Robers MB. Vasta JD, et al. Among authors: machleidt t. Cell Chem Biol. 2018 Feb 15;25(2):206-214.e11. doi: 10.1016/j.chembiol.2017.10.010. Epub 2017 Nov 22. Cell Chem Biol. 2018. PMID: 29174542 Free PMC article.
72 results