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Page 1
Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Allosteric and Mutant Specific Inhibitors of IDH1.
Levell JR, Caferro T, Chenail G, Dix I, Dooley J, Firestone B, Fortin PD, Giraldes J, Gould T, Growney JD, Jones MD, Kulathila R, Lin F, Liu G, Mueller A, van der Plas S, Slocum K, Smith T, Terranova R, Touré BB, Tyagi V, Wagner T, Xie X, Xu M, Yang FS, Zhou LX, Pagliarini R, Cho YS. Levell JR, et al. Among authors: pagliarini r. ACS Med Chem Lett. 2016 Dec 16;8(2):151-156. doi: 10.1021/acsmedchemlett.6b00334. eCollection 2017 Feb 9. ACS Med Chem Lett. 2016. PMID: 28197303 Free PMC article.
Allosteric Mutant IDH1 Inhibitors Reveal Mechanisms for IDH1 Mutant and Isoform Selectivity.
Xie X, Baird D, Bowen K, Capka V, Chen J, Chenail G, Cho Y, Dooley J, Farsidjani A, Fortin P, Kohls D, Kulathila R, Lin F, McKay D, Rodrigues L, Sage D, Touré BB, van der Plas S, Wright K, Xu M, Yin H, Levell J, Pagliarini RA. Xie X, et al. Among authors: pagliarini ra. Structure. 2017 Mar 7;25(3):506-513. doi: 10.1016/j.str.2016.12.017. Epub 2017 Jan 26. Structure. 2017. PMID: 28132785 Free article.
Discovery and Evaluation of Clinical Candidate IDH305, a Brain Penetrant Mutant IDH1 Inhibitor.
Cho YS, Levell JR, Liu G, Caferro T, Sutton J, Shafer CM, Costales A, Manning JR, Zhao Q, Sendzik M, Shultz M, Chenail G, Dooley J, Villalba B, Farsidjani A, Chen J, Kulathila R, Xie X, Dodd S, Gould T, Liang G, Heimbach T, Slocum K, Firestone B, Pu M, Pagliarini R, Growney JD. Cho YS, et al. Among authors: pagliarini r. ACS Med Chem Lett. 2017 Sep 18;8(10):1116-1121. doi: 10.1021/acsmedchemlett.7b00342. eCollection 2017 Oct 12. ACS Med Chem Lett. 2017. PMID: 29057061 Free PMC article.
Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Orally Bioavailable and Brain Penetrant Mutant IDH1 Inhibitors.
Zhao Q, Manning JR, Sutton J, Costales A, Sendzik M, Shafer CM, Levell JR, Liu G, Caferro T, Cho YS, Palermo M, Chenail G, Dooley J, Villalba B, Farsidjani A, Chen J, Dodd S, Gould T, Liang G, Slocum K, Pu M, Firestone B, Growney J, Heimbach T, Pagliarini R. Zhao Q, et al. Among authors: pagliarini r. ACS Med Chem Lett. 2018 Jun 11;9(7):746-751. doi: 10.1021/acsmedchemlett.8b00182. eCollection 2018 Jul 12. ACS Med Chem Lett. 2018. PMID: 30034612 Free PMC article.
Isocitrate dehydrogenase (IDH) mutations promote a reversible ZEB1/microRNA (miR)-200-dependent epithelial-mesenchymal transition (EMT).
Grassian AR, Lin F, Barrett R, Liu Y, Jiang W, Korpal M, Astley H, Gitterman D, Henley T, Howes R, Levell J, Korn JM, Pagliarini R. Grassian AR, et al. Among authors: pagliarini r. J Biol Chem. 2012 Dec 7;287(50):42180-94. doi: 10.1074/jbc.M112.417832. Epub 2012 Oct 4. J Biol Chem. 2012. PMID: 23038259 Free PMC article.
IDH1 mutations alter citric acid cycle metabolism and increase dependence on oxidative mitochondrial metabolism.
Grassian AR, Parker SJ, Davidson SM, Divakaruni AS, Green CR, Zhang X, Slocum KL, Pu M, Lin F, Vickers C, Joud-Caldwell C, Chung F, Yin H, Handly ED, Straub C, Growney JD, Vander Heiden MG, Murphy AN, Pagliarini R, Metallo CM. Grassian AR, et al. Among authors: pagliarini r. Cancer Res. 2014 Jun 15;74(12):3317-31. doi: 10.1158/0008-5472.CAN-14-0772-T. Epub 2014 Apr 22. Cancer Res. 2014. PMID: 24755473 Free PMC article.
The novolactone natural product disrupts the allosteric regulation of Hsp70.
Hassan AQ, Kirby CA, Zhou W, Schuhmann T, Kityk R, Kipp DR, Baird J, Chen J, Chen Y, Chung F, Hoepfner D, Movva NR, Pagliarini R, Petersen F, Quinn C, Quinn D, Riedl R, Schmitt EK, Schitter A, Stams T, Studer C, Fortin PD, Mayer MP, Sadlish H. Hassan AQ, et al. Among authors: pagliarini r. Chem Biol. 2015 Jan 22;22(1):87-97. doi: 10.1016/j.chembiol.2014.11.007. Epub 2014 Dec 24. Chem Biol. 2015. PMID: 25544045
Tumor-derived IFN triggers chronic pathway agonism and sensitivity to ADAR loss.
Liu H, Golji J, Brodeur LK, Chung FS, Chen JT, deBeaumont RS, Bullock CP, Jones MD, Kerr G, Li L, Rakiec DP, Schlabach MR, Sovath S, Growney JD, Pagliarini RA, Ruddy DA, MacIsaac KD, Korn JM, McDonald ER 3rd. Liu H, et al. Among authors: pagliarini ra. Nat Med. 2019 Jan;25(1):95-102. doi: 10.1038/s41591-018-0302-5. Epub 2018 Dec 17. Nat Med. 2019. PMID: 30559422
Patient-derived glioblastoma cultures as a tool for small-molecule drug discovery.
Ye LF, Reznik E, Korn JM, Lin F, Yang G, Malesky K, Gao H, Loo A, Pagliarini R, Mikkelsen T, Lo DC, deCarvalho AC, Stockwell BR. Ye LF, et al. Among authors: pagliarini r. Oncotarget. 2020 Jan 28;11(4):443-451. doi: 10.18632/oncotarget.27457. eCollection 2020 Jan 28. Oncotarget. 2020. PMID: 32064048 Free PMC article.
Disordered methionine metabolism in MTAP/CDKN2A-deleted cancers leads to dependence on PRMT5.
Mavrakis KJ, McDonald ER 3rd, Schlabach MR, Billy E, Hoffman GR, deWeck A, Ruddy DA, Venkatesan K, Yu J, McAllister G, Stump M, deBeaumont R, Ho S, Yue Y, Liu Y, Yan-Neale Y, Yang G, Lin F, Yin H, Gao H, Kipp DR, Zhao S, McNamara JT, Sprague ER, Zheng B, Lin Y, Cho YS, Gu J, Crawford K, Ciccone D, Vitari AC, Lai A, Capka V, Hurov K, Porter JA, Tallarico J, Mickanin C, Lees E, Pagliarini R, Keen N, Schmelzle T, Hofmann F, Stegmeier F, Sellers WR. Mavrakis KJ, et al. Among authors: pagliarini r. Science. 2016 Mar 11;351(6278):1208-13. doi: 10.1126/science.aad5944. Epub 2016 Feb 11. Science. 2016. PMID: 26912361
40 results