期刊
MOLECULAR BIOLOGY REPORTS
卷 48, 期 11, 页码 7499-7508出版社
SPRINGER
DOI: 10.1007/s11033-021-06701-6
关键词
SMYD2; SMYD3; Inhibitors; Epigenetics; Cancer
This review focuses on the advances in pharmacology regarding drugs targeting SMYD2 and SMYD3 in the past five years, discussing their potential cellular and molecular mechanisms of action and applications in anti-tumor therapy and other diseases.
The revelance of the epigenetic regulation of cancer led to the design and testing of many drugs targeting epigenetic modifiers. The Su(Var)3-9, Enhancer-of-zeste and Trithorax (SET) and myeloid, Nervy, and DEAF-1 (MYND) domain-containing protein 2 (SMYD2) and 3 (SMYD3) are methyltransferases which act on histone and non-histone proteins to promote tumorigenesis in many cancer types. In addition to their oncogenic roles, SMYD2 and SMYD3 are involved in many other physiopathological conditions. In this review we will focus on the advances made in the last five years in the field of pharmacology regarding drugs targeting SMYD2 (such as LLY-507 or AZ505) and SMYD3 (such as BCI-121 or EPZ031686) and their potential cellular and molecular mechanisms of action and application in anti-tumoural therapy and/or against other diseases.
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