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Page 1
Discovery of lactoquinomycin and related pyranonaphthoquinones as potent and allosteric inhibitors of AKT/PKB: mechanistic involvement of AKT catalytic activation loop cysteines.
Toral-Barza L, Zhang WG, Huang X, McDonald LA, Salaski EJ, Barbieri LR, Ding WD, Krishnamurthy G, Hu YB, Lucas J, Bernan VS, Cai P, Levin JI, Mansour TS, Gibbons JJ, Abraham RT, Yu K. Toral-Barza L, et al. Among authors: mansour ts. Mol Cancer Ther. 2007 Nov;6(11):3028-38. doi: 10.1158/1535-7163.MCT-07-0211. Epub 2007 Nov 7. Mol Cancer Ther. 2007. PMID: 17989320
Pyranonaphthoquinone lactones: a new class of AKT selective kinase inhibitors alkylate a regulatory loop cysteine.
Salaski EJ, Krishnamurthy G, Ding WD, Yu K, Insaf SS, Eid C, Shim J, Levin JI, Tabei K, Toral-Barza L, Zhang WG, McDonald LA, Honores E, Hanna C, Yamashita A, Johnson B, Li Z, Laakso L, Powell D, Mansour TS. Salaski EJ, et al. Among authors: mansour ts. J Med Chem. 2009 Apr 23;52(8):2181-4. doi: 10.1021/jm900075g. J Med Chem. 2009. PMID: 19309081
Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin.
Yu K, Toral-Barza L, Shi C, Zhang WG, Lucas J, Shor B, Kim J, Verheijen J, Curran K, Malwitz DJ, Cole DC, Ellingboe J, Ayral-Kaloustian S, Mansour TS, Gibbons JJ, Abraham RT, Nowak P, Zask A. Yu K, et al. Among authors: mansour ts. Cancer Res. 2009 Aug 1;69(15):6232-40. doi: 10.1158/0008-5472.CAN-09-0299. Epub 2009 Jul 7. Cancer Res. 2009. PMID: 19584280
ATP-competitive inhibitors of the mammalian target of rapamycin: design and synthesis of highly potent and selective pyrazolopyrimidines.
Zask A, Verheijen JC, Curran K, Kaplan J, Richard DJ, Nowak P, Malwitz DJ, Brooijmans N, Bard J, Svenson K, Lucas J, Toral-Barza L, Zhang WG, Hollander I, Gibbons JJ, Abraham RT, Ayral-Kaloustian S, Mansour TS, Yu K. Zask A, et al. Among authors: mansour ts. J Med Chem. 2009 Aug 27;52(16):5013-6. doi: 10.1021/jm900851f. J Med Chem. 2009. PMID: 19645448
Beyond rapalog therapy: preclinical pharmacology and antitumor activity of WYE-125132, an ATP-competitive and specific inhibitor of mTORC1 and mTORC2.
Yu K, Shi C, Toral-Barza L, Lucas J, Shor B, Kim JE, Zhang WG, Mahoney R, Gaydos C, Tardio L, Kim SK, Conant R, Curran K, Kaplan J, Verheijen J, Ayral-Kaloustian S, Mansour TS, Abraham RT, Zask A, Gibbons JJ. Yu K, et al. Among authors: mansour ts. Cancer Res. 2010 Jan 15;70(2):621-31. doi: 10.1158/0008-5472.CAN-09-2340. Epub 2010 Jan 12. Cancer Res. 2010. PMID: 20068177
PWT-458, a novel pegylated-17-hydroxywortmannin, inhibits phosphatidylinositol 3-kinase signaling and suppresses growth of solid tumors.
Yu K, Lucas J, Zhu T, Zask A, Gaydos C, Toral-Barza L, Gu J, Li F, Chaudhary I, Cai P, Lotvin J, Petersen R, Ruppen M, Fawzi M, Ayral-Kaloustian S, Skotnicki J, Mansour T, Frost P, Gibbons J. Yu K, et al. Cancer Biol Ther. 2005 May;4(5):538-45. doi: 10.4161/cbt.4.5.1660. Epub 2005 May 28. Cancer Biol Ther. 2005. PMID: 15846106 Free article.
Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent.
Verheijen JC, Richard DJ, Curran K, Kaplan J, Lefever M, Nowak P, Malwitz DJ, Brooijmans N, Toral-Barza L, Zhang WG, Lucas J, Hollander I, Ayral-Kaloustian S, Mansour TS, Yu K, Zask A. Verheijen JC, et al. Among authors: mansour ts. J Med Chem. 2009 Dec 24;52(24):8010-24. doi: 10.1021/jm9013828. J Med Chem. 2009. PMID: 19894727
Hybrid inhibitors of phosphatidylinositol 3-kinase (PI3K) and the mammalian target of rapamycin (mTOR): design, synthesis, and superior antitumor activity of novel wortmannin-rapamycin conjugates.
Ayral-Kaloustian S, Gu J, Lucas J, Cinque M, Gaydos C, Zask A, Chaudhary I, Wang J, Di L, Young M, Ruppen M, Mansour TS, Gibbons JJ, Yu K. Ayral-Kaloustian S, et al. Among authors: mansour ts. J Med Chem. 2010 Jan 14;53(1):452-9. doi: 10.1021/jm901427g. J Med Chem. 2010. PMID: 19928864
Novel imidazolopyrimidines as dual PI3-Kinase/mTOR inhibitors.
Venkatesan AM, Dehnhardt CM, Chen Z, Santos ED, Dos Santos O, Bursavich M, Gilbert AM, Ellingboe JW, Ayral-Kaloustian S, Khafizova G, Brooijmans N, Mallon R, Hollander I, Feldberg L, Lucas J, Yu K, Gibbons J, Abraham R, Mansour TS. Venkatesan AM, et al. Among authors: mansour ts. Bioorg Med Chem Lett. 2010 Jan 15;20(2):653-6. doi: 10.1016/j.bmcl.2009.11.057. Epub 2009 Dec 1. Bioorg Med Chem Lett. 2010. PMID: 19954970
Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: discovery of PKI-402.
Dehnhardt CM, Venkatesan AM, Delos Santos E, Chen Z, Santos O, Ayral-Kaloustian S, Brooijmans N, Mallon R, Hollander I, Feldberg L, Lucas J, Chaudhary I, Yu K, Gibbons J, Abraham R, Mansour TS. Dehnhardt CM, et al. Among authors: mansour ts. J Med Chem. 2010 Jan 28;53(2):798-810. doi: 10.1021/jm9014982. J Med Chem. 2010. PMID: 19968288
86 results