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Page 1
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: marks km. Nat Commun. 2019 Jan 9;10(1):96. doi: 10.1038/s41467-018-07959-4. Nat Commun. 2019. PMID: 30626880 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: marks km. 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
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. 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.
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: marks km. Nature. 2009 Dec 10;462(7274):739-44. doi: 10.1038/nature08617. Nature. 2009. PMID: 19935646 Free PMC article.
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: marks km. 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: marks km. 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: marks km. 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
MTAP Deletions in Cancer Create Vulnerability to Targeting of the MAT2A/PRMT5/RIOK1 Axis.
Marjon K, Cameron MJ, Quang P, Clasquin MF, Mandley E, Kunii K, McVay M, Choe S, Kernytsky A, Gross S, Konteatis Z, Murtie J, Blake ML, Travins J, Dorsch M, Biller SA, Marks KM. Marjon K, et al. Among authors: marks km. Cell Rep. 2016 Apr 19;15(3):574-587. doi: 10.1016/j.celrep.2016.03.043. Epub 2016 Apr 7. Cell Rep. 2016. PMID: 27068473 Free article.
mTORC1-dependent AMD1 regulation sustains polyamine metabolism in prostate cancer.
Zabala-Letona A, Arruabarrena-Aristorena A, Martín-Martín N, Fernandez-Ruiz S, Sutherland JD, Clasquin M, Tomas-Cortazar J, Jimenez J, Torres I, Quang P, Ximenez-Embun P, Bago R, Ugalde-Olano A, Loizaga-Iriarte A, Lacasa-Viscasillas I, Unda M, Torrano V, Cabrera D, van Liempd SM, Cendon Y, Castro E, Murray S, Revandkar A, Alimonti A, Zhang Y, Barnett A, Lein G, Pirman D, Cortazar AR, Arreal L, Prudkin L, Astobiza I, Valcarcel-Jimenez L, Zuñiga-García P, Fernandez-Dominguez I, Piva M, Caro-Maldonado A, Sánchez-Mosquera P, Castillo-Martín M, Serra V, Beraza N, Gentilella A, Thomas G, Azkargorta M, Elortza F, Farràs R, Olmos D, Efeyan A, Anguita J, Muñoz J, Falcón-Pérez JM, Barrio R, Macarulla T, Mato JM, Martinez-Chantar ML, Cordon-Cardo C, Aransay AM, Marks K, Baselga J, Tabernero J, Nuciforo P, Manning BD, Marjon K, Carracedo A. Zabala-Letona A, et al. Nature. 2017 Jul 6;547(7661):109-113. doi: 10.1038/nature22964. Epub 2017 Jun 28. Nature. 2017. PMID: 28658205 Free PMC article.
Molecular mechanisms mediating relapse following ivosidenib monotherapy in IDH1-mutant relapsed or refractory AML.
Choe S, Wang H, DiNardo CD, Stein EM, de Botton S, Roboz GJ, Altman JK, Mims AS, Watts JM, Pollyea DA, Fathi AT, Tallman MS, Kantarjian HM, Stone RM, Quek L, Konteatis Z, Dang L, Nicolay B, Nejad P, Liu G, Zhang V, Liu H, Goldwasser M, Liu W, Marks K, Bowden C, Biller SA, Attar EC, Wu B. Choe S, et al. Blood Adv. 2020 May 12;4(9):1894-1905. doi: 10.1182/bloodadvances.2020001503. Blood Adv. 2020. PMID: 32380538 Free PMC article.
53 results