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Page 1
In vivo activation of the p53 pathway by small-molecule antagonists of MDM2.
Vassilev LT, Vu BT, Graves B, Carvajal D, Podlaski F, Filipovic Z, Kong N, Kammlott U, Lukacs C, Klein C, Fotouhi N, Liu EA. Vassilev LT, et al. Among authors: lukacs c. Science. 2004 Feb 6;303(5659):844-8. doi: 10.1126/science.1092472. Epub 2004 Jan 2. Science. 2004. PMID: 14704432
Activation of the p53 pathway by small-molecule-induced MDM2 and MDMX dimerization.
Graves B, Thompson T, Xia M, Janson C, Lukacs C, Deo D, Di Lello P, Fry D, Garvie C, Huang KS, Gao L, Tovar C, Lovey A, Wanner J, Vassilev LT. Graves B, et al. Among authors: lukacs c. Proc Natl Acad Sci U S A. 2012 Jul 17;109(29):11788-93. doi: 10.1073/pnas.1203789109. Epub 2012 Jun 28. Proc Natl Acad Sci U S A. 2012. PMID: 22745160 Free PMC article.
Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2,3-difluoro-6- methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity.
Chu XJ, DePinto W, Bartkovitz D, So SS, Vu BT, Packman K, Lukacs C, Ding Q, Jiang N, Wang K, Goelzer P, Yin X, Smith MA, Higgins BX, Chen Y, Xiang Q, Moliterni J, Kaplan G, Graves B, Lovey A, Fotouhi N. Chu XJ, et al. Among authors: lukacs c. J Med Chem. 2006 Nov 2;49(22):6549-60. doi: 10.1021/jm0606138. J Med Chem. 2006. PMID: 17064073
3,5,6-Trisubstituted naphthostyrils as CDK2 inhibitors.
Liu JJ, Dermatakis A, Lukacs C, Konzelmann F, Chen Y, Kammlott U, Depinto W, Yang H, Yin X, Chen Y, Schutt A, Simcox ME, Luk KC. Liu JJ, et al. Among authors: lukacs c. Bioorg Med Chem Lett. 2003 Aug 4;13(15):2465-8. doi: 10.1016/s0960-894x(03)00488-8. Bioorg Med Chem Lett. 2003. PMID: 12852944
Benzazepinones and benzoxazepinones as antagonists of inhibitor of apoptosis proteins (IAPs) selective for the second baculovirus IAP repeat (BIR2) domain.
Donnell AF, Michoud C, Rupert KC, Han X, Aguilar D, Frank KB, Fretland AJ, Gao L, Goggin B, Hogg JH, Hong K, Janson CA, Kester RF, Kong N, Le K, Li S, Liang W, Lombardo LJ, Lou Y, Lukacs CM, Mischke S, Moliterni JA, Polonskaia A, Schutt AD, Solis DS, Specian A, Taylor RT, Weisel M, Remiszewski SW. Donnell AF, et al. Among authors: lukacs cm. J Med Chem. 2013 Oct 24;56(20):7772-87. doi: 10.1021/jm400731m. Epub 2013 Oct 1. J Med Chem. 2013. PMID: 24083782
Fragment-Based Drug Design of Novel Pyranopyridones as Cell Active and Orally Bioavailable Tankyrase Inhibitors.
de Vicente J, Tivitmahaisoon P, Berry P, Bolin DR, Carvajal D, He W, Huang KS, Janson C, Liang L, Lukacs C, Petersen A, Qian H, Yi L, Zhuang Y, Hermann JC. de Vicente J, et al. Among authors: lukacs c. ACS Med Chem Lett. 2015 Aug 4;6(9):1019-24. doi: 10.1021/acsmedchemlett.5b00251. eCollection 2015 Sep 10. ACS Med Chem Lett. 2015. PMID: 26396691 Free PMC article.
Pyrazolobenzodiazepines: part I. Synthesis and SAR of a potent class of kinase inhibitors.
Liu JJ, Daniewski I, Ding Q, Higgins B, Ju G, Kolinsky K, Konzelmann F, Lukacs C, Pizzolato G, Rossman P, Swain A, Thakkar K, Wei CC, Miklowski D, Yang H, Yin X, Wovkulich PM. Liu JJ, et al. Among authors: lukacs c. Bioorg Med Chem Lett. 2010 Oct 15;20(20):5984-7. doi: 10.1016/j.bmcl.2010.08.079. Epub 2010 Aug 21. Bioorg Med Chem Lett. 2010. PMID: 20832307
Optimization of benzodiazepinones as selective inhibitors of the X-linked inhibitor of apoptosis protein (XIAP) second baculovirus IAP repeat (BIR2) domain.
Kester RF, Donnell AF, Lou Y, Remiszewski SW, Lombardo LJ, Chen S, Le NT, Lo J, Moliterni JA, Han X, Hogg JH, Liang W, Michoud C, Rupert KC, Mischke S, Le K, Weisel M, Janson CA, Lukacs CM, Fretland AJ, Hong K, Polonskaia A, Gao L, Li S, Solis DS, Aguilar D, Tardell C, Dvorozniak M, Tannu S, Lee EC, Schutt AD, Goggin B. Kester RF, et al. Among authors: lukacs cm. J Med Chem. 2013 Oct 24;56(20):7788-803. doi: 10.1021/jm400732v. Epub 2013 Oct 7. J Med Chem. 2013. PMID: 24093940
The structure of XIAP BIR2: understanding the selectivity of the BIR domains.
Lukacs C, Belunis C, Crowther R, Danho W, Gao L, Goggin B, Janson CA, Li S, Remiszewski S, Schutt A, Thakur MK, Singh SK, Swaminathan S, Pandey R, Tyagi R, Gosu R, Kamath AV, Kuglstatter A. Lukacs C, et al. Acta Crystallogr D Biol Crystallogr. 2013 Sep;69(Pt 9):1717-25. doi: 10.1107/S0907444913016284. Epub 2013 Aug 15. Acta Crystallogr D Biol Crystallogr. 2013. PMID: 23999295 Free PMC article.
44 results