期刊
INTERNATIONAL JOURNAL OF HEMATOLOGY
卷 104, 期 3, 页码 300-309出版社
SPRINGER JAPAN KK
DOI: 10.1007/s12185-016-2008-0
关键词
Multiple myeloma; Histone deacetylase (HDAC); HDAC inhibitor; Proteasome inhibitor; Immunomodulatory drugs
类别
Histone deacetylases (HDACs) deacetylate the lysine residues of both histones and non-histone proteins. Histone acetylation results in a loose local chromatin structure that regulates gene-specific transcription. Non-histone proteins can also be acetylated, leading to dynamic changes in their activity and stability. For these reasons, HDAC inhibition has emerged as a potential approach for the treatment of MM. Specifically, combination treatment with HDAC inhibitors and proteasome inhibitors or immunomodulatory drugs shows remarkable anti-MM activity in both preclinical and clinical settings. However, the clinical studies using non-selective HDAC inhibitors also cause unfavorable side effects in patients, leading us to develop more isoform- and/or class-selective HDAC inhibitors to enhance tolerability without diminishing anti-MM activity, thereby improving patient outcome in MM.
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