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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Main Authors:	Huihui Zhu, Tao Wei, Yong Cai, Jingji Jin
Format:	Article
Language:	English
Published:	MDPI AG 2020-01-01
Series:	Molecules
Subjects:	histone marks histone acetylation histone methylation cancer therapy
Online Access:	https://www.mdpi.com/1420-3049/25/3/578

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spelling	doaj-cccefad914ef4473921f7727abe8d34e2020-11-25T02:20:45ZengMDPI AGMolecules1420-30492020-01-0125357810.3390/molecules25030578molecules25030578Small Molecules Targeting the Specific Domains of Histone-Mark Readers in Cancer TherapyHuihui Zhu0Tao Wei1Yong Cai2Jingji Jin3School of Life Sciences, Jilin University, Changchun 130012, ChinaSchool of Life Sciences, Jilin University, Changchun 130012, ChinaSchool of Life Sciences, Jilin University, Changchun 130012, ChinaSchool of Life Sciences, Jilin University, Changchun 130012, ChinaEpigenetic 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.https://www.mdpi.com/1420-3049/25/3/578histone markshistone acetylationhistone methylationcancer therapy
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	Huihui Zhu Tao Wei Yong Cai Jingji Jin
spellingShingle	Huihui Zhu Tao Wei Yong Cai Jingji Jin Small Molecules Targeting the Specific Domains of Histone-Mark Readers in Cancer Therapy Molecules histone marks histone acetylation histone methylation cancer therapy
author_facet	Huihui Zhu Tao Wei Yong Cai Jingji Jin
author_sort	Huihui Zhu
title	Small Molecules Targeting the Specific Domains of Histone-Mark Readers in Cancer Therapy
title_short	Small Molecules Targeting the Specific Domains of Histone-Mark Readers in Cancer Therapy
title_full	Small Molecules Targeting the Specific Domains of Histone-Mark Readers in Cancer Therapy
title_fullStr	Small Molecules Targeting the Specific Domains of Histone-Mark Readers in Cancer Therapy
title_full_unstemmed	Small Molecules Targeting the Specific Domains of Histone-Mark Readers in Cancer Therapy
title_sort	small molecules targeting the specific domains of histone-mark readers in cancer therapy
publisher	MDPI AG
series	Molecules
issn	1420-3049
publishDate	2020-01-01
description	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.
topic	histone marks histone acetylation histone methylation cancer therapy
url	https://www.mdpi.com/1420-3049/25/3/578
work_keys_str_mv	AT huihuizhu smallmoleculestargetingthespecificdomainsofhistonemarkreadersincancertherapy AT taowei smallmoleculestargetingthespecificdomainsofhistonemarkreadersincancertherapy AT yongcai smallmoleculestargetingthespecificdomainsofhistonemarkreadersincancertherapy AT jingjijin smallmoleculestargetingthespecificdomainsofhistonemarkreadersincancertherapy
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Small Molecules Targeting the Specific Domains of Histone-Mark Readers in Cancer Therapy

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