cercosporamide

Cercosporamide is a **natural product initially isolated as a broad-spectrum antifungal agent** from the fungus *Cercosporidium henningsii* with a unique structure based on a dibenzofuran scaffold. It functions as a **potent and selective inhibitor of mitogen-activated protein kinase (MAPK)-interacting kinases (Mnks)**, primarily targeting **Mnk2**, **JAK3**, and to a lesser extent, **Mnk1**. At the molecular level, cercosporamide **blocks phosphorylation of the eukaryotic initiation factor 4E (eIF4E)**, producing antitumor effects through the induction of apoptosis and suppression of cell proliferation. It is also a **potent ATP-competitive inhibitor of protein kinase C (Pkc1)**, a signaling protein with a critical role in fungal cell wall integrity; inhibition of Pkc1 underlies its antifungal effects. In preclinical studies, cercosporamide demonstrated **antileukemic activity** in acute myeloid leukemia (AML) models and enhanced the effect of chemotherapeutics such as cytarabine or mTOR inhibitors. It has also shown **activity in models of cancer metastasis and resistance**, and analogs of cercosporamide have been explored for antidiabetic potential[1][2][3][5][7][9].

Brand names

cercosporamide

Other names

(9aS)-8-acetyl-1,3,7-trihydroxy-9a-methyl-9-oxodibenzofuran-4-carboxamideCHEBI:78696CAS 131436-22-1CAS131436-22-1CAS-131436-22-14-dibenzofurancarboxamide, 8-acetyl-9,9a-dihydro-1,3,7-trihydroxy-9a-methyl-9-oxo-, (S)-(9aS)-8-acetyl-1,3,7-trihydroxy-9a-methyl-9-oxo-9,9a-dihydrodibenzo[b,d]furan-4-carboxamide