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Article: Recent advances in the development of peptide-based inhibitors targeting epigenetic readers of histone lysine acetylation and methylation marks

TitleRecent advances in the development of peptide-based inhibitors targeting epigenetic readers of histone lysine acetylation and methylation marks
Authors
KeywordsChemical probe
Epigenetic reader
Lysine acetylation
Lysine methylation
Peptide-based inhibitor
Issue Date30-May-2023
PublisherElsevier
Citation
Current Opinion in Chemical Biology, 2023, v. 75 How to Cite?
Abstract

Inhibitors for epigenetic readers of histone modifications are useful chemical probes to interrogate the functional roles played by their cognate targets in epigenetic regulation and can even serve as drugs for the treatment of diseases associated with the dysregulated targets. However, many epigenetic readers are intractable to small molecules, as the recognition of modified histone peptides commonly involves flat and extended protein surfaces. In contrast, the relatively large sizes and structural complexity of peptides help them achieve tight and specific binding to the target proteins. Increasing efforts have been made to target epigenetic readers using peptide-based inhibitors that can complement small molecules. In this review, we discuss the recent advances in the development of peptide-based inhibitors of lysine acetylation and methylation readers.


Persistent Identifierhttp://hdl.handle.net/10722/331697
ISSN
2023 Impact Factor: 6.9
2023 SCImago Journal Rankings: 2.328
ISI Accession Number ID

 

DC FieldValueLanguage
dc.contributor.authorLiu, Sha-
dc.contributor.authorLi, Xiang-
dc.contributor.authorLi, Xin-
dc.contributor.authorLi, Xiang David-
dc.date.accessioned2023-09-21T06:58:06Z-
dc.date.available2023-09-21T06:58:06Z-
dc.date.issued2023-05-30-
dc.identifier.citationCurrent Opinion in Chemical Biology, 2023, v. 75-
dc.identifier.issn1367-5931-
dc.identifier.urihttp://hdl.handle.net/10722/331697-
dc.description.abstract<p>Inhibitors for <a href="https://www.sciencedirect.com/topics/biochemistry-genetics-and-molecular-biology/epigenetics" title="Learn more about epigenetic from ScienceDirect's AI-generated Topic Pages">epigenetic</a> readers of <a href="https://www.sciencedirect.com/topics/chemistry/histone" title="Learn more about histone from ScienceDirect's AI-generated Topic Pages">histone</a> modifications are useful chemical probes to interrogate the functional roles played by their cognate targets in <a href="https://www.sciencedirect.com/topics/biochemistry-genetics-and-molecular-biology/epigenetics" title="Learn more about epigenetic from ScienceDirect's AI-generated Topic Pages">epigenetic</a> regulation and can even serve as drugs for the treatment of diseases associated with the dysregulated targets. However, many epigenetic readers are intractable to <a href="https://www.sciencedirect.com/topics/biochemistry-genetics-and-molecular-biology/small-molecule" title="Learn more about small molecules from ScienceDirect's AI-generated Topic Pages">small molecules</a>, as the recognition of modified <a href="https://www.sciencedirect.com/topics/chemistry/histone" title="Learn more about histone from ScienceDirect's AI-generated Topic Pages">histone</a> peptides commonly involves flat and extended <a href="https://www.sciencedirect.com/topics/biochemistry-genetics-and-molecular-biology/cell-surface-protein" title="Learn more about protein surfaces from ScienceDirect's AI-generated Topic Pages">protein surfaces</a>. In contrast, the relatively large sizes and structural complexity of peptides help them achieve tight and specific binding to the target proteins. Increasing efforts have been made to target epigenetic readers using peptide-based inhibitors that can complement <a href="https://www.sciencedirect.com/topics/biochemistry-genetics-and-molecular-biology/small-molecule" title="Learn more about small molecules from ScienceDirect's AI-generated Topic Pages">small molecules</a>. In this review, we discuss the recent advances in the development of peptide-based inhibitors of lysine <a href="https://www.sciencedirect.com/topics/biochemistry-genetics-and-molecular-biology/acetylation" title="Learn more about acetylation from ScienceDirect's AI-generated Topic Pages">acetylation</a> and <a href="https://www.sciencedirect.com/topics/biochemistry-genetics-and-molecular-biology/methylation" title="Learn more about methylation from ScienceDirect's AI-generated Topic Pages">methylation</a> readers.</p>-
dc.languageeng-
dc.publisherElsevier-
dc.relation.ispartofCurrent Opinion in Chemical Biology-
dc.subjectChemical probe-
dc.subjectEpigenetic reader-
dc.subjectLysine acetylation-
dc.subjectLysine methylation-
dc.subjectPeptide-based inhibitor-
dc.titleRecent advances in the development of peptide-based inhibitors targeting epigenetic readers of histone lysine acetylation and methylation marks-
dc.typeArticle-
dc.identifier.doi10.1016/j.cbpa.2023.102334-
dc.identifier.scopuseid_2-s2.0-85160529067-
dc.identifier.volume75-
dc.identifier.isiWOS:001013660000001-
dc.identifier.issnl1367-5931-

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