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MAT2A Inhibition Blocks the Growth of MTAP-Deleted Cancer Cells by Reducing PRMT5-Dependent mRNA Splicing and Inducing DNA Damage.
Kalev P, Hyer ML, Gross S, Konteatis Z, Chen CC, Fletcher M, Lein M, Aguado-Fraile E, Frank V, Barnett A, Mandley E, Goldford J, Chen Y, Sellers K, Hayes S, Lizotte K, Quang P, Tuncay Y, Clasquin M, Peters R, Weier J, Simone E, Murtie J, Liu W, Nagaraja R, Dang L, Sui Z, Biller SA, Travins J, Marks KM, Marjon K. Kalev P, et al. Among authors: nagaraja r. Cancer Cell. 2021 Feb 8;39(2):209-224.e11. doi: 10.1016/j.ccell.2020.12.010. Epub 2021 Jan 14. Cancer Cell. 2021. PMID: 33450196 Free article.
Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous MTAP Deletion.
Konteatis Z, Travins J, Gross S, Marjon K, Barnett A, Mandley E, Nicolay B, Nagaraja R, Chen Y, Sun Y, Liu Z, Yu J, Ye Z, Jiang F, Wei W, Fang C, Gao Y, Kalev P, Hyer ML, DeLaBarre B, Jin L, Padyana AK, Dang L, Murtie J, Biller SA, Sui Z, Marks KM. Konteatis Z, et al. Among authors: nagaraja r. J Med Chem. 2021 Apr 22;64(8):4430-4449. doi: 10.1021/acs.jmedchem.0c01895. Epub 2021 Apr 8. J Med Chem. 2021. PMID: 33829783 Free 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: nagaraja r. 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
Vorasidenib (AG-881): A First-in-Class, Brain-Penetrant Dual Inhibitor of Mutant IDH1 and 2 for Treatment of Glioma.
Konteatis Z, Artin E, Nicolay B, Straley K, Padyana AK, Jin L, Chen Y, Narayaraswamy R, Tong S, Wang F, Zhou D, Cui D, Cai Z, Luo Z, Fang C, Tang H, Lv X, Nagaraja R, Yang H, Su SM, Sui Z, Dang L, Yen K, Popovici-Muller J, Codega P, Campos C, Mellinghoff IK, Biller SA. Konteatis Z, et al. Among authors: nagaraja r. ACS Med Chem Lett. 2020 Jan 22;11(2):101-107. doi: 10.1021/acsmedchemlett.9b00509. eCollection 2020 Feb 13. ACS Med Chem Lett. 2020. PMID: 32071674 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. 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
JAK2/IDH-mutant-driven myeloproliferative neoplasm is sensitive to combined targeted inhibition.
McKenney AS, Lau AN, Somasundara AVH, Spitzer B, Intlekofer AM, Ahn J, Shank K, Rapaport FT, Patel MA, Papalexi E, Shih AH, Chiu A, Freinkman E, Akbay EA, Steadman M, Nagaraja R, Yen K, Teruya-Feldstein J, Wong KK, Rampal R, Vander Heiden MG, Thompson CB, Levine RL. McKenney AS, et al. Among authors: nagaraja r. J Clin Invest. 2018 Feb 1;128(2):789-804. doi: 10.1172/JCI94516. Epub 2018 Jan 22. J Clin Invest. 2018. PMID: 29355841 Free PMC article.
A new class of 5-HT2B antagonists possesses favorable potency, selectivity, and rat pharmacokinetic properties.
Moss N, Choi Y, Cogan D, Flegg A, Kahrs A, Loke P, Meyn O, Nagaraja R, Napier S, Parker A, Thomas Peterson J, Ramsden P, Sarko C, Skow D, Tomlinson J, Tye H, Whitaker M. Moss N, et al. Among authors: nagaraja r. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2206-10. doi: 10.1016/j.bmcl.2009.02.126. Epub 2009 Mar 9. Bioorg Med Chem Lett. 2009. PMID: 19307114
JAK2/IDH-mutant-driven myeloproliferative neoplasm is sensitive to combined targeted inhibition.
McKenney AS, Lau AN, Somasundara AVH, Spitzer B, Intlekofer AM, Ahn J, Shank K, Rapaport FT, Patel MA, Papalexi E, Shih AH, Chiu A, Freinkman E, Akbay EA, Steadman M, Nagaraja R, Yen K, Teruya-Feldstein J, Wong KK, Rampal R, Vander Heiden MG, Thompson CB, Levine RL. McKenney AS, et al. Among authors: nagaraja r. J Clin Invest. 2018 Oct 1;128(10):4743. doi: 10.1172/JCI124920. Epub 2018 Sep 17. J Clin Invest. 2018. PMID: 30222137 Free PMC article. No abstract available.
124 results