Special Issue "Bromodomains: A New Target Class for Drug Development"

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: 31 May 2022.

Special Issue Editors

Dr. Jun Qi
E-Mail Website
Guest Editor
Dana-Farber Cancer Insitute, 450 Brookline Ave. Boston, MA 02215, Harvard Medical School, 25 Shattuck St, Boston, MA 02115, USA
Interests: bromodomain; epigenetics; drug discovery
Dr. Adam David Durbin
E-Mail Website
Guest Editor
St. Jude Children’s Research Hospital, 262 Danny Thomas Pl., Memphis, TN 38105, USA
Interests: epigenetics; transcription; drug discovery

Special Issue Information

Dear Colleagues,

Epigenetic proteins, including histone writers, readers and erasers, modulate the epigenetic landscape of cells which impacts upon gene expression and cell state. Increasing evidence suggests that epigenetic protein function can be dysregulated in neoplastic cell states. Intensive studies by many groups have focused on the bromodomain, an epigenetic reader domain that recognizes acetylated protein and is broadly dysregulated in distinct cancer and disease states. Thus, bromodomains have enormous potential as targets for novel therapeutic development in cancer. An explosion of interest in these proteins was facilitated by the establishment of small molecule inhibitors with great selectivity and potency both in vitro and in vivo. Widespread use of these molecules, especially JQ1 and I-BET762 (Filippakopoulos et al., 2010; Nicodeme et al., 2010), to probe cell responses has led to widely applicable insights into the mechanisms of how inhibition of epigenetic readers impacts transcriptional programs in cancer cells, resulting in differentiation and apoptosis. On the basis of these promising early results, BET inhibitors have entered human clinical investigations for the treatment of different cancers and other diseases (Alqahtani et al., 2019). Next-generation compounds targeting BET bromodomains have been generated using proteolysis-targeted chimera (PROTAC) chemistry, in order to induce targeted degradation of BET proteins (Winter et al., 2015). In parallel, further non-BET bromodomains have been identified as targets for novel therapy in cancers and other diseases. This Special Issue will focus on recent advancements in understanding bromodomain function, ranging from structure to function, and identifying opportunities for drug development for this intriguing class of proteins.

Dr. Jun Qi
Dr. Adam David Durbin
Guest Editors

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 papers will be 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. Pharmaceuticals is an international peer-reviewed open access monthly 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 2000 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.

Keywords

  • epigenetic targets
  • inhibitor
  • degrader
  • transcription factor
  • drug development

Published Papers

This special issue is now open for submission.
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