The transcriptional repressor REV-ERB as a novel target for disease
| Autor: | Matthew J. Fuchter, Heather Ang, Simak Ali, Amaia Uriz-Huarte, Hugh J.M. Brady, Amrita Date |
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| Přispěvatelé: | Cancer Research UK, Engineering & Physical Science Research Council (EPSRC) |
| Rok vydání: | 2020 |
| Předmět: |
Endogenous Factors
viruses Medicinal & Biomolecular Chemistry Clinical Biochemistry Pharmaceutical Science Receptors Cytoplasmic and Nuclear Computational biology Disease Heme Ligands 01 natural sciences Biochemistry 0305 Organic Chemistry Structure-Activity Relationship Immune system Drug Discovery Animals Humans skin and connective tissue diseases Molecular Biology Transcription factor 0304 Medicinal and Biomolecular Chemistry 010405 organic chemistry Chemistry Organic Chemistry 0104 chemical sciences Circadian Rhythm body regions Repressor Proteins 010404 medicinal & biomolecular chemistry Drug development Nuclear receptor Immune System Diseases Nuclear Receptor Subfamily 1 Group D Member 1 Transcriptional Repressor Molecular Medicine 1115 Pharmacology and Pharmaceutical Sciences Function (biology) |
| Zdroj: | Bioorganicmedicinal chemistry letters. 30(17) |
| ISSN: | 1464-3405 |
| Popis: | REV-ERB is a member of the nuclear receptor superfamily of transcription factors involved in the regulation of many physiological processes, from circadian rhythm, to immune function and metabolism. Accordingly, REV-ERB has been considered as a promising, but difficult drug target for the treatment of numerous diseases. Here, we concisely review current understanding of the function of REV-ERB, modulation by endogenous factors and synthetic ligands, and the involvement of REV-ERB in select human diseases. Particular focus is placed on the medicinal chemistry of synthetic REV-ERB ligands, which demonstrates the need for higher quality ligands to aid in robust validation of this exciting target. |
| Databáze: | OpenAIRE |
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