ArticleNature communications2022
Structural basis of synthetic agonist activation of the nuclear receptor REV-ERB.
Article in Nature communications, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
What it found
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
19 citing papers in PubMed, 28 citations in OpenAlex.
- Time matters: circadian genetics and the molecular logic of human health and disease.Nature reviews. Genetics · 2026Review
- REV-ERB-Mediated Regulation of Neural Functional Mechanisms by Phytochemicals in the Circadian System.Nutrients · 2026Review
- Bidirectional Mechanisms Linking Circadian Rhythm Disruption and Parkinson's Disease: Chronobiomarkers and Therapeutic Implications.International journal of molecular sciences · 2026Review
- More than a ring: the emerging role of heme in angiogenesis.Cell communication and signaling : CCS · 2026Review
- STL1267 inhibits myofibroblast differentiation in a TGFβ1-driven human lung fibroblast model.American journal of physiology. Cell physiology · 2026Article
- REV-ERBs as regulators of circadian rhythm, neuroinflammation, and glial lipid homeostasis in Alzheimer's disease. A narrative review.British journal of biomedical science · 2026Review
- The Circadian Modulators as Molecular Targets in Cancer-A Review.International journal of molecular sciences · 2025Review
- From Deficiency to Therapy: Systemic Consequences of ALAS1 Disruption and the Protective Role of 5-ALA.Life (Basel, Switzerland) · 2025Review
- Uncovering a novel binding trench in ERRα: insights from molecular simulations.Frontiers in molecular biosciences · 2025Article
- BMAL1 deficiency in macrophages exacerbates sepsis-induced inflammatory response and organ damage by regulating PGC-1α.American journal of clinical and experimental immunology · 2025Article
- Circadian rhythms in cardiovascular (dys)function: approaches for future therapeutics.NPJ cardiovascular health · 2024Review
- Chemogenomics for NR1 nuclear hormone receptors.Nature communications · 2024Article
- Mechanism of antagonist ligand binding to REV-ERBα.Scientific reports · 2024Article
- ED-71 Ameliorates Bone Loss in Type 2 Diabetes Mellitus by Enhancing Osteogenesis Through Upregulation of the Circadian Rhythm Coregulator BMAL1.Drug design, development and therapy · 2024Article
- International Union of Basic and Clinical Pharmacology CXIII: Nuclear Receptor Superfamily-Update 2023.Pharmacological reviews · 2023Review
- Metabolic and chemical architecture of the mammalian circadian clock.Cell chemical biology · 2023Review
- The Role of REV-ERB Receptors in Cancer Pathogenesis.International journal of molecular sciences · 2023Review
- Regulating the Clock: REV-ERB Agonists as Promising Therapeutic Agents.GEN biotechnology · 2023Article
- REV-ERB activation as a novel pharmacological approach for treating inflammatory pain.Frontiers in pharmacology · 2023Article
Corrections and comments
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Authors and funding
11 authors at 3 institutions in 1 country.
Funding
Abstract
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.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.