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Overview
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Cytosporone B (Dothiorelone G; Csn-B) is a naturally occurring octaketide isolated from an endophytic fungus Cytospora sp, acting as an agonist for the nuclear orphan receptor Nur77 (EC50 = 0.278 nM) with antitumor activity. Nuclear orphan receptor Nur77 has important roles in many biological processes. Csn-B binds specifically to the ligand-binding domain of Nur77 with high affinity (IC50=0.278 nM) and stimulates Nur77-dependent transactivational activity towards target genes including Nr4a1 (Nur77) itself, which contains multiple consensus response elements allowing positive autoregulation in a Csn-B-dependent manner. Csn-B also elevates blood glucose levels in fasting C57 mice, an effect that is accompanied by induction of multiple genes involved in gluconeogenesis.
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Overview