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Page 1
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: silverman l. Science. 2013 May 3;340(6132):626-30. doi: 10.1126/science.1236062. Epub 2013 Apr 4. Science. 2013. PMID: 23558169 Free PMC article.
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: silverman l. 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.
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: silverman l. 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
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. Among authors: silverman l. 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-348 enhances pyruvate kinase activity in red blood cells from patients with pyruvate kinase deficiency.
Kung C, Hixon J, Kosinski PA, Cianchetta G, Histen G, Chen Y, Hill C, Gross S, Si Y, Johnson K, DeLaBarre B, Luo Z, Gu Z, Yao G, Tang H, Fang C, Xu Y, Lv X, Biller S, Su SM, Yang H, Popovici-Muller J, Salituro F, Silverman L, Dang L. Kung C, et al. Among authors: silverman l. Blood. 2017 Sep 14;130(11):1347-1356. doi: 10.1182/blood-2016-11-753525. Epub 2017 Jul 31. Blood. 2017. PMID: 28760888 Free PMC article.
A mouse model of a human congenital disorder of glycosylation caused by loss of PMM2.
Chan B, Clasquin M, Smolen GA, Histen G, Powe J, Chen Y, Lin Z, Lu C, Liu Y, Cang Y, Yan Z, Xia Y, Thompson R, Singleton C, Dorsch M, Silverman L, Su SM, Freeze HH, Jin S. Chan B, et al. Among authors: silverman l. Hum Mol Genet. 2016 Jun 1;25(11):2182-2193. doi: 10.1093/hmg/ddw085. Epub 2016 Apr 5. Hum Mol Genet. 2016. PMID: 27053713 Free PMC article.
Preclinical toxicology profile of squalene epoxidase inhibitors.
Nagaraja R, Olaharski A, Narayanaswamy R, Mahoney C, Pirman D, Gross S, Roddy TP, Popovici-Muller J, Smolen GA, Silverman L. Nagaraja R, et al. Among authors: silverman l. Toxicol Appl Pharmacol. 2020 Aug 15;401:115103. doi: 10.1016/j.taap.2020.115103. Epub 2020 Jun 6. Toxicol Appl Pharmacol. 2020. PMID: 32522582
Phase 1 Single- and Multiple-Ascending-Dose Randomized Studies of the Safety, Pharmacokinetics, and Pharmacodynamics of AG-348, a First-in-Class Allosteric Activator of Pyruvate Kinase R, in Healthy Volunteers.
Yang H, Merica E, Chen Y, Cohen M, Goldwater R, Kosinski PA, Kung C, Yuan ZJ, Silverman L, Goldwasser M, Silver BA, Agresta S, Barbier AJ. Yang H, et al. Among authors: silverman l. Clin Pharmacol Drug Dev. 2019 Feb;8(2):246-259. doi: 10.1002/cpdd.604. Epub 2018 Aug 9. Clin Pharmacol Drug Dev. 2019. PMID: 30091852 Clinical Trial.
Characterization of Alisertib (MLN8237), an investigational small-molecule inhibitor of aurora A kinase using novel in vivo pharmacodynamic assays.
Manfredi MG, Ecsedy JA, Chakravarty A, Silverman L, Zhang M, Hoar KM, Stroud SG, Chen W, Shinde V, Huck JJ, Wysong DR, Janowick DA, Hyer ML, Leroy PJ, Gershman RE, Silva MD, Germanos MS, Bolen JB, Claiborne CF, Sells TB. Manfredi MG, et al. Among authors: silverman l. Clin Cancer Res. 2011 Dec 15;17(24):7614-24. doi: 10.1158/1078-0432.CCR-11-1536. Epub 2011 Oct 20. Clin Cancer Res. 2011. PMID: 22016509
Phase I assessment of new mechanism-based pharmacodynamic biomarkers for MLN8054, a small-molecule inhibitor of Aurora A kinase.
Chakravarty A, Shinde V, Tabernero J, Cervantes A, Cohen RB, Dees EC, Burris H, Infante JR, Macarulla T, Elez E, Andreu J, Rodriguez-Braun E, Rosello S, von Mehren M, Meropol NJ, Langer CJ, ONeil B, Bowman D, Zhang M, Danaee H, Faron-Yowe L, Gray G, Liu H, Pappas J, Silverman L, Simpson C, Stringer B, Tirrell S, Veiby OP, Venkatakrishnan K, Galvin K, Manfredi M, Ecsedy JA. Chakravarty A, et al. Among authors: silverman l. Cancer Res. 2011 Feb 1;71(3):675-85. doi: 10.1158/0008-5472.CAN-10-1030. Epub 2010 Dec 10. Cancer Res. 2011. PMID: 21148750 Clinical Trial.
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