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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
general
Structural basis of synthetic agonist activation of the nuclear receptor REV-ERB
Nature Communications, Volume 13, No. 1, Article 7131, Year 2022
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Description
The nuclear receptor REV-ERB plays an important role in a range of physiological processes. REV-ERB behaves as a ligand-dependent transcriptional repressor and heme has been identified as a physiological agonist. Our current understanding of how ligands bind to and regulate transcriptional repression by REV-ERB is based on the structure of heme bound to REV-ERB. However, porphyrin (heme) analogues have been avoided as a source of synthetic agonists due to the wide range of heme binding proteins and potential pleotropic effects. How non-porphyrin synthetic agonists bind to and regulate REV-ERB has not yet been defined. Here, we characterize a high affinity synthetic REV-ERB agonist, STL1267, and describe its mechanism of binding to REV-ERB as well as the method by which it recruits transcriptional corepressor both of which are unique and distinct from that of heme-bound REV-ERB. © 2022, The Author(s).
Authors & Co-Authors
Chatterjee, Arindam
United States, St. Louis
St. Louis University School of Medicine
Veerakanellore, Giri Babu
United States, St. Louis
Washington University School of Medicine in St. Louis
United States, St. Louis
University of Health Sciences and Pharmacy
Elgendy, Bahaa
United States, St. Louis
Washington University School of Medicine in St. Louis
United States, St. Louis
University of Health Sciences and Pharmacy
Walker, John K.
United States, St. Louis
St. Louis University School of Medicine
Hegazy, Lamees S.
United States, St. Louis
Washington University School of Medicine in St. Louis
United States, St. Louis
University of Health Sciences and Pharmacy
Burris, Thomas P.
United States, Gainesville
University of Florida
Statistics
Citations: 5
Authors: 6
Affiliations: 4
Identifiers
Doi:
10.1038/s41467-022-34892-4
ISSN:
20411723
Research Areas
Cancer