Histone Methyltransferase SETDB1: A Common Denominator of Tumorigenesis with Therapeutic Potential

Abstract Epigenetic regulation of gene expression has been ultimately linked to cancer development, with posttranslational histone modifications representing attractive targets for disease monitoring and therapy. Emerging data have demonstrated lysine (K) methylation by methyltransferase SETDB1 as a common denominator in several types. reversibly catalyzes the di- trimethylation 3 (H3) K9 euchromatic regions chromosomes, inhibiting transcription within these promoting switch from heterochromatic states. Recent studies implicated aberrant activity development various types cancers, including brain, head neck, lung, breast, gastrointestinal, ovarian, endometrial prostate cancer, mesothelioma, melanoma, leukemias, osteosarcoma. Although its role not fully elucidated every case, most point toward pro-oncogenic potential via downregulation critical tumor-suppressive genes. Less commonly, however, can also acquire role, depending on type stage. Here we provide an updated overview cellular molecular effects underlying progression along current targeting strategies different types, promising either standalone therapy or conjunction other therapeutic agents.