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Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer.
Liu Q, Chang JW, Wang J, Kang SA, Thoreen CC, Markhard A, Hur W, Zhang J, Sim T, Sabatini DM, Gray NS. Liu Q, et al. Among authors: sabatini dm. J Med Chem. 2010 Oct 14;53(19):7146-55. doi: 10.1021/jm101144f. J Med Chem. 2010. PMID: 20860370 Free PMC article.
Discovery of 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a potent, selective, and orally available mammalian target of rapamycin (mTOR) inhibitor for treatment of cancer.
Liu Q, Wang J, Kang SA, Thoreen CC, Hur W, Ahmed T, Sabatini DM, Gray NS. Liu Q, et al. Among authors: sabatini dm. J Med Chem. 2011 Mar 10;54(5):1473-80. doi: 10.1021/jm101520v. Epub 2011 Feb 15. J Med Chem. 2011. PMID: 21322566 Free PMC article.
Functional genomics reveal that the serine synthesis pathway is essential in breast cancer.
Possemato R, Marks KM, Shaul YD, Pacold ME, Kim D, Birsoy K, Sethumadhavan S, Woo HK, Jang HG, Jha AK, Chen WW, Barrett FG, Stransky N, Tsun ZY, Cowley GS, Barretina J, Kalaany NY, Hsu PP, Ottina K, Chan AM, Yuan B, Garraway LA, Root DE, Mino-Kenudson M, Brachtel EF, Driggers EM, Sabatini DM. Possemato R, et al. Among authors: sabatini dm. Nature. 2011 Aug 18;476(7360):346-50. doi: 10.1038/nature10350. Nature. 2011. PMID: 21760589 Free PMC article.
The bromodomain protein Brd4 insulates chromatin from DNA damage signalling.
Floyd SR, Pacold ME, Huang Q, Clarke SM, Lam FC, Cannell IG, Bryson BD, Rameseder J, Lee MJ, Blake EJ, Fydrych A, Ho R, Greenberger BA, Chen GC, Maffa A, Del Rosario AM, Root DE, Carpenter AE, Hahn WC, Sabatini DM, Chen CC, White FM, Bradner JE, Yaffe MB. Floyd SR, et al. Among authors: sabatini dm. Nature. 2013 Jun 13;498(7453):246-50. doi: 10.1038/nature12147. Epub 2013 Jun 2. Nature. 2013. PMID: 23728299 Free PMC article.
Dihydropyrimidine accumulation is required for the epithelial-mesenchymal transition.
Shaul YD, Freinkman E, Comb WC, Cantor JR, Tam WL, Thiru P, Kim D, Kanarek N, Pacold ME, Chen WW, Bierie B, Possemato R, Reinhardt F, Weinberg RA, Yaffe MB, Sabatini DM. Shaul YD, et al. Among authors: sabatini dm. Cell. 2014 Aug 28;158(5):1094-1109. doi: 10.1016/j.cell.2014.07.032. Cell. 2014. PMID: 25171410 Free PMC article.
SHMT2 drives glioma cell survival in ischaemia but imposes a dependence on glycine clearance.
Kim D, Fiske BP, Birsoy K, Freinkman E, Kami K, Possemato RL, Chudnovsky Y, Pacold ME, Chen WW, Cantor JR, Shelton LM, Gui DY, Kwon M, Ramkissoon SH, Ligon KL, Kang SW, Snuderl M, Vander Heiden MG, Sabatini DM. Kim D, et al. Among authors: sabatini dm. Nature. 2015 Apr 16;520(7547):363-7. doi: 10.1038/nature14363. Epub 2015 Apr 8. Nature. 2015. PMID: 25855294 Free PMC article.
Structural basis for leucine sensing by the Sestrin2-mTORC1 pathway.
Saxton RA, Knockenhauer KE, Wolfson RL, Chantranupong L, Pacold ME, Wang T, Schwartz TU, Sabatini DM. Saxton RA, et al. Among authors: sabatini dm. Science. 2016 Jan 1;351(6268):53-8. doi: 10.1126/science.aad2087. Epub 2015 Nov 19. Science. 2016. PMID: 26586190 Free PMC article.
289 results