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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: nagaraja n. Nat Commun. 2019 Jan 9;10(1):96. doi: 10.1038/s41467-018-07959-4. Nat Commun. 2019. PMID: 30626880 Free PMC 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: nagaraja n. Nat Commun. 2019 Jan 9;10(1):97. doi: 10.1038/s41467-018-07928-x. Nat Commun. 2019. PMID: 30626872 Free PMC article.
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: nagaraja n. 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
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: nagaraja n. 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. 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
Selective CB2 receptor agonists. Part 3: the optimization of a piperidine-based series that demonstrated efficacy in an in vivo neuropathic pain model.
Bartolozzi A, Cirillo PF, Berry AK, Hickey ER, Thomson DS, Wu L, Zindell R, Albrecht C, Ceci A, Gemkow MJ, Nagaraja NV, Romig H, Sauer A, Riether D. Bartolozzi A, et al. Bioorg Med Chem Lett. 2015 Feb 1;25(3):587-92. doi: 10.1016/j.bmcl.2014.12.031. Epub 2014 Dec 17. Bioorg Med Chem Lett. 2015. PMID: 25575658
SAR studies of non-zinc-chelating MMP-13 inhibitors: improving selectivity and metabolic stability.
Gao DA, Xiong Z, Heim-Riether A, Amodeo L, August EM, Cao X, Ciccarelli L, Collins BK, Harrington K, Haverty K, Hill-Drzewi M, Li X, Liang S, Margarit SM, Moss N, Nagaraja N, Proudfoot J, Roman R, Schlyer S, Keenan LS, Taylor S, Wellenzohn B, Wiedenmayer D, Li J, Farrow NA. Gao DA, et al. Among authors: nagaraja n. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5039-43. doi: 10.1016/j.bmcl.2010.07.036. Epub 2010 Jul 15. Bioorg Med Chem Lett. 2010. PMID: 20675133
92 results