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Inhibitors of bromodomain and extra‐terminal proteins for treating multiple human diseases
- Source :
- Medicinal Research Reviews
- Publication Year :
- 2020
- Publisher :
- Wiley, 2020.
-
Abstract
- Clinical development of bromodomain and extra‐terminal (BET) protein inhibitors differs from the traditional course of drug development. These drugs are simultaneously being evaluated for treating a wide spectrum of human diseases due to their novel mechanism of action. BET proteins are epigenetic “readers,” which play a primary role in transcription. Here, we briefly describe the BET family of proteins, of which BRD4 has been studied most extensively. We discuss BRD4 activity at latent enhancers as an example of BET protein function. We examine BRD4 redistribution and enhancer reprogramming in embryonic development, cancer, cardiovascular, autoimmune, and metabolic diseases, presenting hallmark studies that highlight BET proteins as attractive targets for therapeutic intervention. We review the currently available approaches to targeting BET proteins, methods of selectively targeting individual bromodomains, and review studies that compare the effects of selective BET inhibition to those of pan‐BET inhibition. Lastly, we examine the current clinical landscape of BET inhibitor development.
- Subjects :
- BRD4
BD‐selective
Cell Cycle Proteins
chemical and pharmacologic phenomena
Review Article
Computational biology
Biology
BETi
BET inhibitor
03 medical and health sciences
0302 clinical medicine
Protein Domains
Neoplasms
Drug Discovery
medicine
Humans
Epigenetics
Enhancer
Review Articles
030304 developmental biology
Pharmacology
0303 health sciences
Nuclear Proteins
hemic and immune systems
BET
Bromodomain
Mechanism of action
Drug development
030220 oncology & carcinogenesis
Molecular Medicine
bromodomain (BD)
enhancer
medicine.symptom
Reprogramming
Transcription Factors
Subjects
Details
- ISSN :
- 10981128 and 01986325
- Volume :
- 41
- Database :
- OpenAIRE
- Journal :
- Medicinal Research Reviews
- Accession number :
- edsair.doi.dedup.....66a547b2e3488ffee02634305b6765c1