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Page 1
Selective Vulnerability to Pyrimidine Starvation in Hematologic Malignancies Revealed by AG-636, a Novel Clinical-Stage Inhibitor of Dihydroorotate Dehydrogenase.
McDonald G, Chubukov V, Coco J, Truskowski K, Narayanaswamy R, Choe S, Steadman M, Artin E, Padyana AK, Jin L, Ronseaux S, Locuson C, Fan ZP, Erdmann T, Mann A, Hayes S, Fletcher M, Nellore K, Rao SS, Subramanya H, Reddy KS, Panigrahi SK, Antony T, Gopinath S, Sui Z, Nagaraja N, Dang L, Lenz G, Hurov J, Biller SA, Murtie J, Marks KM, Ulanet DB. McDonald G, et al. Among authors: biller sa. Mol Cancer Ther. 2020 Dec;19(12):2502-2515. doi: 10.1158/1535-7163.MCT-20-0550. Epub 2020 Oct 20. Mol Cancer Ther. 2020. PMID: 33082276
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: biller sa. Nat Commun. 2019 Jan 9;10(1):96. doi: 10.1038/s41467-018-07959-4. Nat Commun. 2019. PMID: 30626880 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: biller sa. 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
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: biller sa. 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.
Structure and inhibition mechanism of the catalytic domain of human squalene epoxidase.
Padyana AK, Gross S, Jin L, Cianchetta G, Narayanaswamy R, Wang F, Wang R, Fang C, Lv X, Biller SA, Dang L, Mahoney CE, Nagaraja N, Pirman D, Sui Z, Popovici-Muller J, Smolen GA. Padyana AK, et al. Among authors: biller sa. Nat Commun. 2019 Jan 9;10(1):97. doi: 10.1038/s41467-018-07928-x. Nat Commun. 2019. PMID: 30626872 Free PMC article.
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: biller sa. 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.
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: biller sa. 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.
Leveraging Structure-Based Drug Design to Identify Next-Generation MAT2A Inhibitors, Including Brain-Penetrant and Peripherally Efficacious Leads.
Li M, Konteatis Z, Nagaraja N, Chen Y, Zhou S, Ma G, Gross S, Marjon K, Hyer ML, Mandley E, Lein M, Padyana AK, Jin L, Tong S, Peters R, Murtie J, Travins J, Medeiros M, Liu P, Frank V, Judd ET, Biller SA, Marks KM, Sui Z, Reznik SK. Li M, et al. Among authors: biller sa. J Med Chem. 2022 Mar 24;65(6):4600-4615. doi: 10.1021/acs.jmedchem.1c01595. Epub 2022 Mar 16. J Med Chem. 2022. PMID: 35293760
Preclinical Drug Metabolism, Pharmacokinetic, and Pharmacodynamic Profiles of Ivosidenib, an Inhibitor of Mutant Isocitrate Dehydrogenase 1 for Treatment of Isocitrate Dehydrogenase 1-Mutant Malignancies.
Chen Y, Nagaraja NV, Fan B, Utley L, Lemieux RM, Popovici-Muller J, Dang L, Kim H, Yan L, Su SM, Biller SA, Yang H. Chen Y, et al. Among authors: biller sa. Drug Metab Dispos. 2021 Oct;49(10):870-881. doi: 10.1124/dmd.120.000234. Epub 2021 Jul 28. Drug Metab Dispos. 2021. PMID: 34321251
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.
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