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Page 1
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. Among authors: grasberger b. 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
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: grasberger bl. 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
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. 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: grasberger bl. Mol Cancer Ther. 2006 Jan;5(1):160-9. doi: 10.1158/1535-7163.MCT-05-0199. Mol Cancer Ther. 2006. PMID: 16432175
Structure-based design, synthesis and SAR of a novel series of thiopheneamidine urokinase plasminogen activator inhibitors.
Subasinghe NL, Illig C, Hoffman J, Rudolph MJ, Wilson KJ, Soll R, Randle T, Green D, Lewandowski F, Zhang M, Bone R, Spurlino J, DesJarlais R, Deckman I, Molloy CJ, Manthey C, Zhou Z, Sharp C, Maguire D, Crysler C, Grasberger B. Subasinghe NL, et al. Among authors: grasberger b. Bioorg Med Chem Lett. 2001 Jun 4;11(11):1379-82. doi: 10.1016/s0960-894x(01)00247-5. Bioorg Med Chem Lett. 2001. PMID: 11378359
Crystal structure of a soluble form of human monoglyceride lipase in complex with an inhibitor at 1.35 Å resolution.
Schalk-Hihi C, Schubert C, Alexander R, Bayoumy S, Clemente JC, Deckman I, DesJarlais RL, Dzordzorme KC, Flores CM, Grasberger B, Kranz JK, Lewandowski F, Liu L, Ma H, Maguire D, Macielag MJ, McDonnell ME, Mezzasalma Haarlander T, Miller R, Milligan C, Reynolds C, Kuo LC. Schalk-Hihi C, et al. Among authors: grasberger b. Protein Sci. 2011 Apr;20(4):670-83. doi: 10.1002/pro.596. Epub 2011 Mar 1. Protein Sci. 2011. PMID: 21308848 Free PMC article.
Synthesis of thiophene-2-carboxamidines containing 2-aminothiazoles and their biological evaluation as urokinase inhibitors.
Wilson KJ, Illig CR, Subasinghe N, Hoffman JB, Rudolph MJ, Soll R, Molloy CJ, Bone R, Green D, Randall T, Zhang M, Lewandowski FA, Zhou Z, Sharp C, Maguire D, Grasberger B, DesJarlais RL, Spurlino J. Wilson KJ, et al. Among authors: grasberger b. Bioorg Med Chem Lett. 2001 Apr 9;11(7):915-8. doi: 10.1016/s0960-894x(01)00102-0. Bioorg Med Chem Lett. 2001. PMID: 11294390
Design and synthesis of 4,5-disubstituted-thiophene-2-amidines as potent urokinase inhibitors.
Rudolph MJ, Illig CR, Subasinghe NL, Wilson KJ, Hoffman JB, Randle T, Green D, Molloy CJ, Soll RM, Lewandowski F, Zhang M, Bone R, Spurlino JC, Deckman IC, Manthey C, Sharp C, Maguire D, Grasberger BL, DesJarlais RL, Zhou Z. Rudolph MJ, et al. Among authors: grasberger bl. Bioorg Med Chem Lett. 2002 Feb 11;12(3):491-5. doi: 10.1016/s0960-894x(01)00787-9. Bioorg Med Chem Lett. 2002. PMID: 11814826
19 results