Bromodomain inhibitors and cancer therapy: From structures to applications
Aberrations in the epigenetic landscape are a hallmark of cancer. Alterations in enzymes that are “writers,” “erasers,” or “readers” of histone modification marks are common. Bromodomains are “readers” that bind acetylated lysines in histone tails. Their most important function is the regulation of...
| Main Authors: | , |
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| Format: | Article |
| Language: | English |
| Published: |
Taylor & Francis Group
2017-05-01
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| Series: | Epigenetics |
| Subjects: | |
| Online Access: | http://dx.doi.org/10.1080/15592294.2016.1265710 |
| _version_ | 1827811620309434368 |
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| author | Montserrat Pérez-Salvia Manel Esteller |
| author_facet | Montserrat Pérez-Salvia Manel Esteller |
| author_sort | Montserrat Pérez-Salvia |
| collection | DOAJ |
| description | Aberrations in the epigenetic landscape are a hallmark of cancer. Alterations in enzymes that are “writers,” “erasers,” or “readers” of histone modification marks are common. Bromodomains are “readers” that bind acetylated lysines in histone tails. Their most important function is the regulation of gene transcription by the recruitment of different molecular partners. Moreover, proteins containing bromodomains are also epigenetic regulators, although little is known about the specific function of these domains. In recent years, there has been increasing interest in developing small molecules that can target specific bromodomains. First, this has helped clarify biological functions of bromodomain-containing proteins. Secondly, it opens a new front for combatting cancer. In this review we will describe the structures and mechanisms associated with Bromodomain and Extra-Terminal motif (BET) inhibitors and non-BET inhibitors, their current status of development, and their promising role as anti-cancer agents. |
| first_indexed | 2024-03-11T23:07:14Z |
| format | Article |
| id | doaj.art-30ae7d3446f946fa8459c9c5774ceb2f |
| institution | Directory Open Access Journal |
| issn | 1559-2294 1559-2308 |
| language | English |
| last_indexed | 2024-03-11T23:07:14Z |
| publishDate | 2017-05-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Epigenetics |
| spelling | doaj.art-30ae7d3446f946fa8459c9c5774ceb2f2023-09-21T12:43:12ZengTaylor & Francis GroupEpigenetics1559-22941559-23082017-05-0112532333910.1080/15592294.2016.12657101265710Bromodomain inhibitors and cancer therapy: From structures to applicationsMontserrat Pérez-Salvia0Manel Esteller1Bellvitge Biomedical Research Institute (IDIBELL)Bellvitge Biomedical Research Institute (IDIBELL)Aberrations in the epigenetic landscape are a hallmark of cancer. Alterations in enzymes that are “writers,” “erasers,” or “readers” of histone modification marks are common. Bromodomains are “readers” that bind acetylated lysines in histone tails. Their most important function is the regulation of gene transcription by the recruitment of different molecular partners. Moreover, proteins containing bromodomains are also epigenetic regulators, although little is known about the specific function of these domains. In recent years, there has been increasing interest in developing small molecules that can target specific bromodomains. First, this has helped clarify biological functions of bromodomain-containing proteins. Secondly, it opens a new front for combatting cancer. In this review we will describe the structures and mechanisms associated with Bromodomain and Extra-Terminal motif (BET) inhibitors and non-BET inhibitors, their current status of development, and their promising role as anti-cancer agents.http://dx.doi.org/10.1080/15592294.2016.1265710acetylationbromodomain and extra-terminal motif inhibitorscancerepigeneticshistone marks |
| spellingShingle | Montserrat Pérez-Salvia Manel Esteller Bromodomain inhibitors and cancer therapy: From structures to applications Epigenetics acetylation bromodomain and extra-terminal motif inhibitors cancer epigenetics histone marks |
| title | Bromodomain inhibitors and cancer therapy: From structures to applications |
| title_full | Bromodomain inhibitors and cancer therapy: From structures to applications |
| title_fullStr | Bromodomain inhibitors and cancer therapy: From structures to applications |
| title_full_unstemmed | Bromodomain inhibitors and cancer therapy: From structures to applications |
| title_short | Bromodomain inhibitors and cancer therapy: From structures to applications |
| title_sort | bromodomain inhibitors and cancer therapy from structures to applications |
| topic | acetylation bromodomain and extra-terminal motif inhibitors cancer epigenetics histone marks |
| url | http://dx.doi.org/10.1080/15592294.2016.1265710 |
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