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Design and synthesis of a series of bioavailable fatty acid synthase (FASN) KR domain inhibitors for cancer therapy.
Lu T, Schubert C, Cummings MD, Bignan G, Connolly PJ, Smans K, Ludovici D, Parker MH, Meyer C, Rocaboy C, Alexander R, Grasberger B, De Breucker S, Esser N, Fraiponts E, Gilissen R, Janssens B, Peeters D, Van Nuffel L, Vermeulen P, Bischoff J, Meerpoel L. Lu T, et al. Bioorg Med Chem Lett. 2018 Jul 1;28(12):2159-2164. doi: 10.1016/j.bmcl.2018.05.014. Epub 2018 May 8. Bioorg Med Chem Lett. 2018. PMID: 29779975
Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors.
Tomczuk B, Lu T, Soll RM, Fedde C, Wang A, Murphy L, Crysler C, Dasgupta M, Eisennagel S, Spurlino J, Bone R. Tomczuk B, et al. Among authors: lu t. Bioorg Med Chem Lett. 2003 Apr 17;13(8):1495-8. doi: 10.1016/s0960-894x(03)00125-2. Bioorg Med Chem Lett. 2003. PMID: 12668020
Discovery and cocrystal structure of benzodiazepinedione HDM2 antagonists that activate p53 in cells.
Grasberger BL, Lu T, Schubert C, Parks DJ, Carver TE, Koblish HK, Cummings MD, LaFrance LV, Milkiewicz KL, Calvo RR, Maguire D, Lattanze J, Franks CF, Zhao S, Ramachandren K, Bylebyl GR, Zhang M, Manthey CL, Petrella EC, Pantoliano MW, Deckman IC, Spurlino JC, Maroney AC, Tomczuk BE, Molloy CJ, Bone RF. Grasberger BL, et al. Among authors: lu t. J Med Chem. 2005 Feb 24;48(4):909-12. doi: 10.1021/jm049137g. J Med Chem. 2005. PMID: 15715460
Benzodiazepinedione inhibitors of the Hdm2:p53 complex suppress human tumor cell proliferation in vitro and sensitize tumors to doxorubicin in vivo.
Koblish HK, Zhao S, Franks CF, Donatelli RR, Tominovich RM, LaFrance LV, Leonard KA, Gushue JM, Parks DJ, Calvo RR, Milkiewicz KL, Marugán JJ, Raboisson P, Cummings MD, Grasberger BL, Johnson DL, Lu T, Molloy CJ, Maroney AC. Koblish HK, et al. Among authors: lu t. Mol Cancer Ther. 2006 Jan;5(1):160-9. doi: 10.1158/1535-7163.MCT-05-0199. Mol Cancer Ther. 2006. PMID: 16432175
Enhanced pharmacokinetic properties of 1,4-benzodiazepine-2,5-dione antagonists of the HDM2-p53 protein-protein interaction through structure-based drug design.
Parks DJ, LaFrance LV, Calvo RR, Milkiewicz KL, Marugán JJ, Raboisson P, Schubert C, Koblish HK, Zhao S, Franks CF, Lattanze J, Carver TE, Cummings MD, Maguire D, Grasberger BL, Maroney AC, Lu T. Parks DJ, et al. Among authors: lu t. Bioorg Med Chem Lett. 2006 Jun 15;16(12):3310-4. doi: 10.1016/j.bmcl.2006.03.055. Epub 2006 Apr 4. Bioorg Med Chem Lett. 2006. PMID: 16600594
7,336 results