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Page 1
Discovery of selective aminothiazole aurora kinase inhibitors.
Andersen CB, Wan Y, Chang JW, Riggs B, Lee C, Liu Y, Sessa F, Villa F, Kwiatkowski N, Suzuki M, Nallan L, Heald R, Musacchio A, Gray NS. Andersen CB, et al. Among authors: lee c. ACS Chem Biol. 2008 Mar 20;3(3):180-92. doi: 10.1021/cb700200w. Epub 2008 Feb 29. ACS Chem Biol. 2008. PMID: 18307303
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: lee c. Chem Biol. 2006 Jul;13(7):779-86. doi: 10.1016/j.chembiol.2006.05.015. Chem Biol. 2006. PMID: 16873026
Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 2.
Choi HS, Wang Z, Richmond W, He X, Yang K, Jiang T, Karanewsky D, Gu XJ, Zhou V, Liu Y, Che J, Lee CC, Caldwell J, Kanazawa T, Umemura I, Matsuura N, Ohmori O, Honda T, Gray N, He Y. Choi HS, et al. Among authors: lee cc. Bioorg Med Chem Lett. 2006 May 15;16(10):2689-92. doi: 10.1016/j.bmcl.2006.02.032. Epub 2006 Mar 9. Bioorg Med Chem Lett. 2006. PMID: 16524731
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: lee cc. J Med Chem. 2013 Jul 25;56(14):5675-90. doi: 10.1021/jm400402q. Epub 2013 Jun 26. J Med Chem. 2013. PMID: 23742252
Design and synthesis of novel selective anaplastic lymphoma kinase inhibitors.
Michellys PY, Chen B, Jiang T, Jin Y, Lu W, Marsilje TH, Pei W, Uno T, Zhu X, Wu B, Nguyen TN, Bursulaya B, Lee C, Li N, Kim S, Tuntland T, Liu B, Sun F, Steffy A, Hood T. Michellys PY, et al. Among authors: lee c. Bioorg Med Chem Lett. 2016 Feb 1;26(3):1090-1096. doi: 10.1016/j.bmcl.2015.11.049. Epub 2015 Nov 17. Bioorg Med Chem Lett. 2016. PMID: 26750252
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: lee cc. 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.
Orally bioavailable Syk inhibitors with activity in a rat PK/PD model.
Thoma G, Veenstra S, Strang R, Blanz J, Vangrevelinghe E, Berghausen J, Lee CC, Zerwes HG. Thoma G, et al. Among authors: lee cc. Bioorg Med Chem Lett. 2015 Oct 15;25(20):4642-7. doi: 10.1016/j.bmcl.2015.08.037. Epub 2015 Aug 18. Bioorg Med Chem Lett. 2015. PMID: 26320624
Syk inhibitors with high potency in presence of blood.
Thoma G, Blanz J, Bühlmayer P, Drückes P, Kittelmann M, Smith AB, van Eis M, Vangrevelinghe E, Zerwes HG, Che JJ, He X, Jin Y, Lee CC, Michellys PY, Uno T, Liu H. Thoma G, et al. Among authors: lee cc. Bioorg Med Chem Lett. 2014 May 15;24(10):2278-82. doi: 10.1016/j.bmcl.2014.03.075. Epub 2014 Apr 3. Bioorg Med Chem Lett. 2014. PMID: 24726806
Structure-Based Design of Selective LONP1 Inhibitors for Probing In Vitro Biology.
Kingsley LJ, He X, McNeill M, Nelson J, Nikulin V, Ma Z, Lu W, Zhou VW, Manuia M, Kreusch A, Gao MY, Witmer D, Vaillancourt MT, Lu M, Greenblatt S, Lee C, Vashisht A, Bender S, Spraggon G, Michellys PY, Jia Y, Haling JR, Lelais G. Kingsley LJ, et al. Among authors: lee c. J Med Chem. 2021 Apr 22;64(8):4857-4869. doi: 10.1021/acs.jmedchem.0c02152. Epub 2021 Apr 6. J Med Chem. 2021. PMID: 33821636
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