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Page 1
Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis.
Anastasiou D, Yu Y, Israelsen WJ, Jiang JK, Boxer MB, Hong BS, Tempel W, Dimov S, Shen M, Jha A, Yang H, Mattaini KR, Metallo CM, Fiske BP, Courtney KD, Malstrom S, Khan TM, Kung C, Skoumbourdis AP, Veith H, Southall N, Walsh MJ, Brimacombe KR, Leister W, Lunt SY, Johnson ZR, Yen KE, Kunii K, Davidson SM, Christofk HR, Austin CP, Inglese J, Harris MH, Asara JM, Stephanopoulos G, Salituro FG, Jin S, Dang L, Auld DS, Park HW, Cantley LC, Thomas CJ, Vander Heiden MG. Anastasiou D, et al. Among authors: yen ke. Nat Chem Biol. 2012 Oct;8(10):839-47. doi: 10.1038/nchembio.1060. Nat Chem Biol. 2012. PMID: 22922757 Free PMC article.
Small molecule activation of PKM2 in cancer cells induces serine auxotrophy.
Kung C, Hixon J, Choe S, Marks K, Gross S, Murphy E, DeLaBarre B, Cianchetta G, Sethumadhavan S, Wang X, Yan S, Gao Y, Fang C, Wei W, Jiang F, Wang S, Qian K, Saunders J, Driggers E, Woo HK, Kunii K, Murray S, Yang H, Yen K, Liu W, Cantley LC, Vander Heiden MG, Su SM, Jin S, Salituro FG, Dang L. Kung C, et al. Chem Biol. 2012 Sep 21;19(9):1187-98. doi: 10.1016/j.chembiol.2012.07.021. Chem Biol. 2012. PMID: 22999886 Free PMC article.
Cancer-associated IDH1 mutations produce 2-hydroxyglutarate.
Dang L, White DW, Gross S, Bennett BD, Bittinger MA, Driggers EM, Fantin VR, Jang HG, Jin S, Keenan MC, Marks KM, Prins RM, Ward PS, Yen KE, Liau LM, Rabinowitz JD, Cantley LC, Thompson CB, Vander Heiden MG, Su SM. Dang L, et al. Among authors: yen ke. Nature. 2009 Dec 10;462(7274):739-44. doi: 10.1038/nature08617. Nature. 2009. PMID: 19935646 Free PMC article.
Cancer-associated IDH1 mutations produce 2-hydroxyglutarate.
Dang L, White DW, Gross S, Bennett BD, Bittinger MA, Driggers EM, Fantin VR, Jang HG, Jin S, Keenan MC, Marks KM, Prins RM, Ward PS, Yen KE, Liau LM, Rabinowitz JD, Cantley LC, Thompson CB, Vander Heiden MG, Su SM. Dang L, et al. Among authors: yen ke. Nature. 2010 Jun 17;465(7300):966. doi: 10.1038/nature09132. Nature. 2010. PMID: 20559394 Free PMC article. No abstract available.
Targeted inhibition of mutant IDH2 in leukemia cells induces cellular differentiation.
Wang F, Travins J, DeLaBarre B, Penard-Lacronique V, Schalm S, Hansen E, Straley K, Kernytsky A, Liu W, Gliser C, Yang H, Gross S, Artin E, Saada V, Mylonas E, Quivoron C, Popovici-Muller J, Saunders JO, Salituro FG, Yan S, Murray S, Wei W, Gao Y, Dang L, Dorsch M, Agresta S, Schenkein DP, Biller SA, Su SM, de Botton S, Yen KE. Wang F, et al. Among authors: yen ke. Science. 2013 May 3;340(6132):622-6. doi: 10.1126/science.1234769. Epub 2013 Apr 4. Science. 2013. PMID: 23558173
Discovery of the First Potent Inhibitors of Mutant IDH1 That Lower Tumor 2-HG in Vivo.
Popovici-Muller J, Saunders JO, Salituro FG, Travins JM, Yan S, Zhao F, Gross S, Dang L, Yen KE, Yang H, Straley KS, Jin S, Kunii K, Fantin VR, Zhang S, Pan Q, Shi D, Biller SA, Su SM. Popovici-Muller J, et al. Among authors: yen ke. ACS Med Chem Lett. 2012 Sep 17;3(10):850-5. doi: 10.1021/ml300225h. eCollection 2012 Oct 11. ACS Med Chem Lett. 2012. PMID: 24900389 Free PMC article.
Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers.
Popovici-Muller J, Lemieux RM, Artin E, Saunders JO, Salituro FG, Travins J, Cianchetta G, Cai Z, Zhou D, Cui D, Chen P, Straley K, Tobin E, Wang F, David MD, Penard-Lacronique V, Quivoron C, Saada V, de Botton S, Gross S, Dang L, Yang H, Utley L, Chen Y, Kim H, Jin S, Gu Z, Yao G, Luo Z, Lv X, Fang C, Yan L, Olaharski A, Silverman L, Biller S, Su SM, Yen K. Popovici-Muller J, et al. ACS Med Chem Lett. 2018 Jan 19;9(4):300-305. doi: 10.1021/acsmedchemlett.7b00421. eCollection 2018 Apr 12. ACS Med Chem Lett. 2018. PMID: 29670690 Free PMC article.
AG-221, a First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations.
Yen K, Travins J, Wang F, David MD, Artin E, Straley K, Padyana A, Gross S, DeLaBarre B, Tobin E, Chen Y, Nagaraja R, Choe S, Jin L, Konteatis Z, Cianchetta G, Saunders JO, Salituro FG, Quivoron C, Opolon P, Bawa O, Saada V, Paci A, Broutin S, Bernard OA, de Botton S, Marteyn BS, Pilichowska M, Xu Y, Fang C, Jiang F, Wei W, Jin S, Silverman L, Liu W, Yang H, Dang L, Dorsch M, Penard-Lacronique V, Biller SA, Su SM. Yen K, et al. Cancer Discov. 2017 May;7(5):478-493. doi: 10.1158/2159-8290.CD-16-1034. Epub 2017 Feb 13. Cancer Discov. 2017. PMID: 28193778
An inhibitor of mutant IDH1 delays growth and promotes differentiation of glioma cells.
Rohle D, Popovici-Muller J, Palaskas N, Turcan S, Grommes C, Campos C, Tsoi J, Clark O, Oldrini B, Komisopoulou E, Kunii K, Pedraza A, Schalm S, Silverman L, Miller A, Wang F, Yang H, Chen Y, Kernytsky A, Rosenblum MK, Liu W, Biller SA, Su SM, Brennan CW, Chan TA, Graeber TG, Yen KE, Mellinghoff IK. Rohle D, et al. Among authors: yen ke. Science. 2013 May 3;340(6132):626-30. doi: 10.1126/science.1236062. Epub 2013 Apr 4. Science. 2013. PMID: 23558169 Free PMC article.
45 results