Small Molecules Targeting the Specific Domains of Histone-Mark Readers in Cancer Therapy

Epigenetic modifications (or epigenetic tags) on DNA and histones not only alter the chromatin structure, but also provide a recognition platform for subsequent protein recruitment and enable them to acquire executive instructions to carry out specific intracellular biological processes. In cells, d...

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Published inMolecules (Basel, Switzerland) Vol. 25; no. 3; p. 578
Main Authors Zhu, Huihui, Wei, Tao, Cai, Yong, Jin, Jingji
Format Journal Article
LanguageEnglish
Published Switzerland MDPI AG 29.01.2020
MDPI
Subjects
Biological activity
Brain tumors
Cancer therapies
cancer therapy
Cell cycle
Chromatin
Deoxyribonucleic acid
DNA
DNA methylation
Drug development
Enzymes
Genes
histone acetylation
histone marks
histone methylation
Histones
Homeobox
Intracellular
Proteins
Recognition
Recruitment
Review
Stem cells
Tags
Tumors
cancer therapy
histone methylation
histone marks
histone acetylation
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Summary:Epigenetic modifications (or epigenetic tags) on DNA and histones not only alter the chromatin structure, but also provide a recognition platform for subsequent protein recruitment and enable them to acquire executive instructions to carry out specific intracellular biological processes. In cells, different epigenetic-tags on DNA and histones are often recognized by the specific domains in proteins (readers), such as bromodomain (BRD), chromodomain (CHD), plant homeodomain (PHD), Tudor domain, Pro-Trp-Trp-Pro (PWWP) domain and malignant brain tumor (MBT) domain. Recent accumulating data reveal that abnormal intracellular histone modifications (histone marks) caused by tumors can be modulated by small molecule-mediated changes in the activity of the above domains, suggesting that small molecules targeting histone-mark reader domains may be the trend of new anticancer drug development. Here, we summarize the protein domains involved in histone-mark recognition, and introduce recent research findings about small molecules targeting histone-mark readers in cancer therapy.
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ISSN:1420-3049
1420-3049
DOI:10.3390/molecules25030578