GSK 4716 - CAS 101574-65-6
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
Estrogen Receptor/ERR
GSK 4716 is a selective agonist of estrogen-related receptors ERRβ and ERRγ displaying selectivity over ERRα and the classical estrogen receptors. Activation of GSK 4716 regulates mitochondrial activity in skeletal muscle during exercise.
Brife Description:
ERRβ/γ agonist
≥99% by HPLC
Canonical SMILES:
1.ATP Maintenance via Two Types of ATP Regulators Mitigates Pathological Phenotypes in Mouse Models of Parkinson's Disease.
Nakano M;Imamura H;Sasaoka N;Yamamoto M;Uemura N;Shudo T;Fuchigami T;Takahashi R;Kakizuka A EBioMedicine. 2017 Aug;22:225-241. doi: 10.1016/j.ebiom.2017.07.024. Epub 2017 Jul 25.
Parkinson's disease is assumed to be caused by mitochondrial dysfunction in the affected dopaminergic neurons in the brain. We have recently created small chemicals, KUSs (Kyoto University Substances), which can reduce cellular ATP consumption. By contrast, agonistic ligands of ERRs (estrogen receptor-related receptors) are expected to raise cellular ATP levels via enhancing ATP production. Here, we show that esculetin functions as an ERR agonist, and its addition to culture media enhances glycolysis and mitochondrial respiration, leading to elevated cellular ATP levels. Subsequently, we show the neuroprotective efficacies of KUSs, esculetin, and GSK4716 (an ERRγ agonist) against cell death in Parkinson's disease models. In the surviving neurons, ATP levels and expression levels of α-synuclein and CHOP (an ER stress-mediated cell death executor) were all rectified. We propose that maintenance of ATP levels, by inhibiting ATP consumption or enhancing ATP production, or both, would be a promising therapeutic strategy for Parkinson's disease.
2.Estrogen-related receptors as emerging targets in cancer and metabolic disorders.
Ariazi EA;Jordan VC Curr Top Med Chem. 2006;6(3):203-15.
While estrogen receptor (ER)-targeted therapeutics have clearly been a success in the treatment of breast cancer, the orphan estrogen-related receptors (ERRs) represent novel targets for future development. The ERRs, comprising ERRalpha, ERRbeta and ERRgamma, bind and regulate transcription via estrogen response elements (EREs) and extended ERE half-sites termed ERR response elements (ERREs), but do not bind endogenous estrogens. The emerging role of ERRalpha and ERRgamma in modulating estrogen responsiveness, substituting for ER activities, and serving as prognosticators in breast and other cancers is providing an impetus for the identification of compounds which target these proteins. Moreover, ERRalpha plays a role in energy homeostasis and will likely be targeted for the treatment of metabolic disorders. Multiple classes of synthetic ligands have already been identified. The phytoestrogens genistein, daidzein, biochanin A and 6,3'4'-tryhydroxyflavone have been reported as ERRalpha agonists. The phenolic acyl hydrazones GSK4716 and GSK9089 act as selective agonists of ERRbeta and ERRgamma. The organochlorine pesticides toxaphene and chlordane, and the synthetic compound XCT790 antagonize ERRalpha.
3.Transcriptional mechanism for the paired miR-433 and miR-127 genes by nuclear receptors SHP and ERRgamma.
Song G;Wang L Nucleic Acids Res. 2008 Oct;36(18):5727-35. doi: 10.1093/nar/gkn567. Epub 2008 Sep 6.
MicroRNAs (miRNAs, miRs) are genomically encoded small approximately 22 nt RNA molecules that have been shown to mediate translational repression of target mRNAs involved in cellular proliferation, differentiation and death. Despite intensive studies on their physiological and pathological functions, the molecular mechanism of how miRNA gene transcription is regulated remains largely unknown. Microarray profiling revealed 21 miRNAs clustered on chromosome 12, including miR-433 and miR-127, that were co-upregulated in small heterodimer partner (SHP, NR0B2) SHP knockouts (SHP(-/-)) liver. Gene cloning revealed that the 3'-coding region of pri-miR-433 served as the promoter region of pri-miR-127. Estrogen related receptor (ERRgamma, NR3B3) robustly activated miR-433 and miR-127 promoter reporters through ERRE, which was transrepressed by SHP. The strong elevation of miR-433 and miR-127 in Hepa-1 cells correlated with the down-regulation of SHP and up-regulation of ERRgamma. Ectopic expression of ERRgamma induced miR-433 and miR-127 expression, which was repressed by SHP coexpression. In contrast, knockdown ERRgamma decreased miR-433 and miR-127 expression. In addition, the ERRgamma agonist GSK4716 induced miR-433 and miR-127 expression both in vitro and in vivo, respectively.
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CAS 101574-65-6 GSK 4716

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