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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: lucas j. 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
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: lucas j. J Med Chem. 2009 Aug 27;52(16):5013-6. doi: 10.1021/jm900851f. J Med Chem. 2009. PMID: 19645448
Discovery of a stable macrocyclic o-aminobenzamide Hsp90 inhibitor which significantly decreases tumor volume in a mouse xenograft model.
Zapf CW, Bloom JD, Li Z, Dushin RG, Nittoli T, Otteng M, Nikitenko A, Golas JM, Liu H, Lucas J, Boschelli F, Vogan E, Olland A, Johnson M, Levin JI. Zapf CW, et al. Among authors: lucas j. Bioorg Med Chem Lett. 2011 Aug 1;21(15):4602-7. doi: 10.1016/j.bmcl.2011.05.102. Epub 2011 Jun 27. Bioorg Med Chem Lett. 2011. PMID: 21715165
Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor.
Venkatesan AM, Dehnhardt CM, Delos Santos E, Chen Z, Dos Santos O, Ayral-Kaloustian S, Khafizova G, Brooijmans N, Mallon R, Hollander I, Feldberg L, Lucas J, Yu K, Gibbons J, Abraham RT, Chaudhary I, Mansour TS. Venkatesan AM, et al. Among authors: lucas j. J Med Chem. 2010 Mar 25;53(6):2636-45. doi: 10.1021/jm901830p. J Med Chem. 2010. PMID: 20166697
2,363 results