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Epigenomes
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Epidrugs: Toward Understanding and Treating Diverse Diseases
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Epidrugs: Toward Understanding and Treating Diverse Diseases

A special issue of Epigenomes (ISSN 2075-4655).

Deadline for manuscript submissions: closed (31 May 2023) | Viewed by 13828

Special Issue Editor

Dr. Takashi Umehara

E-Mail Website
Guest Editor
Drug Discovery Structural Biology Platform Unit, RIKEN Center for Biosystems Dynamics Research, 1-7-22 Suehiro, Tsurumi, Yokohama 230-0045, Japan
Interests: chromatin biochemistry; drug discovery; histone acetylation; histone methylation; synthetic biology

Special Issue Information

Dear Colleagues,

Epigenomic modifications are unique in that the type and amount of chemical modification at each chromosomal location can vary from cell to cell. In recent years, not only have these epigenomic modifications been revealed genome-wide, but rapid progress has also been made in the identification of the proteins responsible for epigenomic modifications and the development of their regulatory compounds. This Special Issue on "Epidrugs" aims to provide insights into broad aspects of biology and drug development through epigenome-regulating compounds.

Dr. Takashi Umehara
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Epigenomes is an international peer-reviewed open access quarterly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 1500 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

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Published Papers (3 papers)

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Editorial

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3 pages, 181 KiB  
Editorial
Epidrugs: Toward Understanding and Treating Diverse Diseases
by Takashi Umehara
Epigenomes 2022, 6(3), 18; https://doi.org/10.3390/epigenomes6030018 - 12 Jul 2022
Cited by 5 | Viewed by 2683
Abstract
Epigenomic modifications are unique in the type and amount of chemical modification at each chromosomal location, can vary from cell to cell, and can be externally modulated by small molecules. In recent years, genome-wide epigenomic modifications have been revealed, and rapid progress has [...] Read more.
Epigenomic modifications are unique in the type and amount of chemical modification at each chromosomal location, can vary from cell to cell, and can be externally modulated by small molecules. In recent years, genome-wide epigenomic modifications have been revealed, and rapid progress has been made in the identification of proteins responsible for epigenomic modifications and in the development of compounds that regulate them. This Special Issue on “Epidrugs: Toward Understanding and Treating Diverse Diseases” aims to provide insights into various aspects of the biology and development of epigenome-regulating compounds. Full article
(This article belongs to the Special Issue Epidrugs: Toward Understanding and Treating Diverse Diseases)

Review

Jump to: Editorial

17 pages, 1071 KiB  
Review
Chemical Inhibitors Targeting the Histone Lysine Demethylase Families with Potential for Drug Discovery
by Nando Dulal Das, Hideaki Niwa and Takashi Umehara
Epigenomes 2023, 7(1), 7; https://doi.org/10.3390/epigenomes7010007 - 11 Mar 2023
Cited by 8 | Viewed by 3907
Abstract
The dynamic regulation of histone methylation and demethylation plays an important role in the regulation of gene expression. Aberrant expression of histone lysine demethylases has been implicated in various diseases including intractable cancers, and thus lysine demethylases serve as promising therapeutic targets. Recent [...] Read more.
The dynamic regulation of histone methylation and demethylation plays an important role in the regulation of gene expression. Aberrant expression of histone lysine demethylases has been implicated in various diseases including intractable cancers, and thus lysine demethylases serve as promising therapeutic targets. Recent studies in epigenomics and chemical biology have led to the development of a series of small-molecule demethylase inhibitors that are potent, specific, and have in vivo efficacy. In this review, we highlight emerging small-molecule inhibitors targeting the histone lysine demethylases and their progress toward drug discovery. Full article
(This article belongs to the Special Issue Epidrugs: Toward Understanding and Treating Diverse Diseases)
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16 pages, 995 KiB  
Review
Epigenetic Regulation in Breast Cancer: Insights on Epidrugs
by Ayoung Kim, Kyumin Mo, Hyeonseok Kwon, Soohyun Choe, Misung Park, Woori Kwak and Hyunho Yoon
Epigenomes 2023, 7(1), 6; https://doi.org/10.3390/epigenomes7010006 - 18 Feb 2023
Cited by 22 | Viewed by 6131
Abstract
Breast cancer remains a common cause of cancer-related death in women. Therefore, further studies are necessary for the comprehension of breast cancer and the revolution of breast cancer treatment. Cancer is a heterogeneous disease that results from epigenetic alterations in normal cells. Aberrant [...] Read more.
Breast cancer remains a common cause of cancer-related death in women. Therefore, further studies are necessary for the comprehension of breast cancer and the revolution of breast cancer treatment. Cancer is a heterogeneous disease that results from epigenetic alterations in normal cells. Aberrant epigenetic regulation is strongly associated with the development of breast cancer. Current therapeutic approaches target epigenetic alterations rather than genetic mutations due to their reversibility. The formation and maintenance of epigenetic changes depend on specific enzymes, including DNA methyltransferases and histone deacetylases, which are promising targets for epigenetic-based therapy. Epidrugs target different epigenetic alterations, including DNA methylation, histone acetylation, and histone methylation, which can restore normal cellular memory in cancerous diseases. Epigenetic-targeted therapy using epidrugs has anti-tumor effects on malignancies, including breast cancer. This review focuses on the importance of epigenetic regulation and the clinical implications of epidrugs in breast cancer. Full article
(This article belongs to the Special Issue Epidrugs: Toward Understanding and Treating Diverse Diseases)
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