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

by 1, 1, 1,2 and 1,2,*
1
School of Life Sciences, Jilin University, Changchun 130012, China
2
School of Pharmacy, Changchun University of Chinese Medicine, Changchun 130117, China
*
Author to whom correspondence should be addressed.
Academic Editors: Franco M. Buonaguro and Anna Lucia Tornesello
Molecules 2020, 25(3), 578; https://doi.org/10.3390/molecules25030578
Received: 17 December 2019 / Revised: 20 January 2020 / Accepted: 22 January 2020 / Published: 29 January 2020
(This article belongs to the Special Issue Peptides and Small Molecules as Anti-Cancer Agents)
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. View Full-Text
Keywords: histone marks; histone acetylation; histone methylation; cancer therapy histone marks; histone acetylation; histone methylation; cancer therapy
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MDPI and ACS Style

Zhu, H.; Wei, T.; Cai, Y.; Jin, J. Small Molecules Targeting the Specific Domains of Histone-Mark Readers in Cancer Therapy. Molecules 2020, 25, 578. https://doi.org/10.3390/molecules25030578

AMA Style

Zhu H, Wei T, Cai Y, Jin J. Small Molecules Targeting the Specific Domains of Histone-Mark Readers in Cancer Therapy. Molecules. 2020; 25(3):578. https://doi.org/10.3390/molecules25030578

Chicago/Turabian Style

Zhu, Huihui, Tao Wei, Yong Cai, and Jingji Jin. 2020. "Small Molecules Targeting the Specific Domains of Histone-Mark Readers in Cancer Therapy" Molecules 25, no. 3: 578. https://doi.org/10.3390/molecules25030578

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