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Structure-activity studies on N-Substituted tranylcypromine derivatives lead to selective inhibitors of lysine specific demethylase 1 (LSD1) and potent inducers of leukemic cell differentiation.
Schulz-Fincke J, Hau M, Barth J, Robaa D, Willmann D, Kürner A, Haas J, Greve G, Haydn T, Fulda S, Lübbert M, Lüdeke S, Berg T, Sippl W, Schüle R, Jung M. Schulz-Fincke J, et al. Among authors: greve g. Eur J Med Chem. 2018 Jan 20;144:52-67. doi: 10.1016/j.ejmech.2017.12.001. Epub 2017 Dec 6. Eur J Med Chem. 2018. PMID: 29247860
LSD1 inhibition by tranylcypromine derivatives interferes with GFI1-mediated repression of PU.1 target genes and induces differentiation in AML.
Barth J, Abou-El-Ardat K, Dalic D, Kurrle N, Maier AM, Mohr S, Schütte J, Vassen L, Greve G, Schulz-Fincke J, Schmitt M, Tosic M, Metzger E, Bug G, Khandanpour C, Wagner SA, Lübbert M, Jung M, Serve H, Schüle R, Berg T. Barth J, et al. Among authors: greve g. Leukemia. 2019 Jun;33(6):1411-1426. doi: 10.1038/s41375-018-0375-7. Epub 2019 Jan 24. Leukemia. 2019. PMID: 30679800
Correction: LSD1 inhibition by tranylcypromine derivatives interferes with GFI1-mediated repression of PU.1 target genes and induces differentiation in AML.
Barth J, Abou-El-Ardat K, Dalic D, Kurrle N, Maier AM, Mohr S, Schütte J, Vassen L, Greve G, Schulz-Fincke J, Schmitt M, Tosic M, Metzger E, Bug G, Khandanpour C, Wagner SA, Lübbert M, Jung M, Serve H, Schüle R, Berg T. Barth J, et al. Among authors: greve g. Leukemia. 2019 Jun;33(6):1541. doi: 10.1038/s41375-019-0415-y. Leukemia. 2019. PMID: 30837671
127 results