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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: gross s. Nature. 2010 Jun 17;465(7300):966. doi: 10.1038/nature09132. Nature. 2010. PMID: 20559394 Free PMC article. No abstract available.
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: gross s. Nature. 2009 Dec 10;462(7274):739-44. doi: 10.1038/nature08617. Nature. 2009. PMID: 19935646 Free PMC article.
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: gross s. 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.
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: gross s. Science. 2013 May 3;340(6132):622-6. doi: 10.1126/science.1234769. Epub 2013 Apr 4. Science. 2013. PMID: 23558173
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. Among authors: gross s. 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
A small molecule inhibitor of mutant IDH2 rescues cardiomyopathy in a D-2-hydroxyglutaric aciduria type II mouse model.
Wang F, Travins J, Lin Z, Si Y, Chen Y, Powe J, Murray S, Zhu D, Artin E, Gross S, Santiago S, Steadman M, Kernytsky A, Straley K, Lu C, Pop A, Struys EA, Jansen EE, Salomons GS, David MD, Quivoron C, Penard-Lacronique V, Regan KS, Liu W, Dang L, Yang H, Silverman L, Agresta S, Dorsch M, Biller S, Yen K, Cang Y, Su SM, Jin S. Wang F, et al. Among authors: gross s. J Inherit Metab Dis. 2016 Nov;39(6):807-820. doi: 10.1007/s10545-016-9960-y. Epub 2016 Jul 28. J Inherit Metab Dis. 2016. PMID: 27469509 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. Among authors: gross s. 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.
A chemical biology screen identifies a vulnerability of neuroendocrine cancer cells to SQLE inhibition.
Mahoney CE, Pirman D, Chubukov V, Sleger T, Hayes S, Fan ZP, Allen EL, Chen Y, Huang L, Liu M, Zhang Y, McDonald G, Narayanaswamy R, Choe S, Chen Y, Gross S, Cianchetta G, Padyana AK, Murray S, Liu W, Marks KM, Murtie J, Dorsch M, Jin S, Nagaraja N, Biller SA, Roddy T, Popovici-Muller J, Smolen GA. Mahoney CE, et al. Among authors: gross s. Nat Commun. 2019 Jan 9;10(1):96. doi: 10.1038/s41467-018-07959-4. Nat Commun. 2019. PMID: 30626880 Free PMC article.
Transformation by the (R)-enantiomer of 2-hydroxyglutarate linked to EGLN activation.
Koivunen P, Lee S, Duncan CG, Lopez G, Lu G, Ramkissoon S, Losman JA, Joensuu P, Bergmann U, Gross S, Travins J, Weiss S, Looper R, Ligon KL, Verhaak RG, Yan H, Kaelin WG Jr. Koivunen P, et al. Among authors: gross s. Nature. 2012 Feb 15;483(7390):484-8. doi: 10.1038/nature10898. Nature. 2012. PMID: 22343896 Free PMC article.
2,193 results