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A phase 1 dose escalation study of the pyruvate kinase activator mitapivat (AG-348) in sickle cell disease.
Xu JZ, Conrey A, Frey I, Gwaabe E, Menapace LA, Tumburu L, Lundt M, Lequang T, Li Q, Glass K, Dunkelberger EB, Iyer V, Mangus H, Kung C, Dang L, Kosinski PA, Hawkins P, Jeffries N, Eaton WA, Lay Thein S. Xu JZ, et al. Among authors: dang l. Blood. 2022 Nov 10;140(19):2053-2062. doi: 10.1182/blood.2022015403. Blood. 2022. PMID: 35576529 Free PMC article. Clinical Trial.
Mitapivat increases ATP and decreases oxidative stress and erythrocyte mitochondria retention in a SCD mouse model.
Quezado ZMN, Kamimura S, Smith M, Wang X, Heaven MR, Jana S, Vogel S, Zerfas P, Combs CA, Almeida LEF, Li Q, Quezado M, Horkayne-Szakaly I, Kosinski PA, Yu S, Kapadnis U, Kung C, Dang L, Wakim P, Eaton WA, Alayash AI, Thein SL. Quezado ZMN, et al. Among authors: dang l. Blood Cells Mol Dis. 2022 Jul;95:102660. doi: 10.1016/j.bcmd.2022.102660. Epub 2022 Mar 12. Blood Cells Mol Dis. 2022. PMID: 35366607 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: dang 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.
AG-348 (Mitapivat), an allosteric activator of red blood cell pyruvate kinase, increases enzymatic activity, protein stability, and ATP levels over a broad range of PKLR genotypes.
Rab MAE, Van Oirschot BA, Kosinski PA, Hixon J, Johnson K, Chubukov V, Dang L, Pasterkamp G, Van Straaten S, Van Solinge WW, Van Beers EJ, Kung C, Van Wijk R. Rab MAE, et al. Among authors: dang l. Haematologica. 2021 Jan 1;106(1):238-249. doi: 10.3324/haematol.2019.238865. Haematologica. 2021. PMID: 31974203 Free PMC article.
The pyruvate kinase activator mitapivat reduces hemolysis and improves anemia in a β-thalassemia mouse model.
Matte A, Federti E, Kung C, Kosinski PA, Narayanaswamy R, Russo R, Federico G, Carlomagno F, Desbats MA, Salviati L, Leboeuf C, Valenti MT, Turrini F, Janin A, Yu S, Beneduce E, Ronseaux S, Iatcenko I, Dang L, Ganz T, Jung CL, Iolascon A, Brugnara C, De Franceschi L. Matte A, et al. Among authors: dang l. J Clin Invest. 2021 May 17;131(10):e144206. doi: 10.1172/JCI144206. J Clin Invest. 2021. PMID: 33822774 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. Among authors: dang l. Blood Adv. 2020 May 12;4(9):1894-1905. doi: 10.1182/bloodadvances.2020001503. Blood Adv. 2020. PMID: 32380538 Free PMC article.
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. Among authors: dang l. 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.
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: dang l. 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.
1,079 results