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AuthorDhulkifle, Hevna
AuthorDiab, Mohammad Issam
AuthorAlgonaiah, Majed
AuthorKorashy, Hesham M.
AuthorMaayah, Zaid H.
Available date2024-04-29T11:04:12Z
Publication Date2024-02-06
Publication NameACS Pharmacology and Translational Science
Identifierhttp://dx.doi.org/10.1021/acsptsci.3c00219
CitationDhulkifle, H., Diab, M. I., Algonaiah, M., Korashy, H. M., & Maayah, Z. H. (2024). Apabetalone (RVX-208): A Potential Epigenetic Therapy for the Treatment of Cardiovascular, Renal, Neurological, Viral, and Cancer Disorders. ACS Pharmacology & Translational Science, 7(3), 546-559.
URIhttps://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85185264335&origin=inward
URIhttp://hdl.handle.net/10576/54453
AbstractBromodomain and extra-terminal domain proteins (BET proteins) are epigenetic reader proteins that have been implicated in regulating gene expression through binding to chromatin and interaction with transcription factors. These proteins are located in the nucleus and are responsible for recognizing acetylated lysine residues on histones, reading epigenetic messages, recruiting key transcription factors, and thereby regulating gene expression. BET proteins control the transcription of genes responsible for maladaptive effects in inflammation, cancer, and renal and cardiovascular diseases. Given the multifaceted role of BET proteins in the pathogenesis of various diseases, several small molecule inhibitors of BET proteins have been developed as potential therapeutic targets for treating different diseases in recent years. However, while many nonselective BET inhibitors are indicated for the treatment of cancer, a selective BET inhibitor, apabetalone, is the only oral BET inhibitor in phase III clinical trials for the treatment of cardiovascular diseases and others. Thus, this review aims to present and discuss the preclinical and clinical evidence for the beneficial effects and mechanism of action of apabetalone for treating various diseases.
SponsorThis publication was supported by Qatar University Internal Grant No. QUCG-CPH-23/24-209.
Languageen
PublisherAmerican Chemical Society (ACS)
SubjectApabetalone
cardiovascular
epigenetics
inflammation
TitleApabetalone (RVX-208): A Potential Epigenetic Therapy for the Treatment of Cardiovascular, Renal, Neurological, Viral, and Cancer Disorders
TypeArticle
Pagination546-559
Issue Number3
Volume Number7
ESSN2575-9108
dc.accessType Full Text


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