Calphostins (UCN-1028), novel and specific inhibitors of protein kinase C. I. Fermentation, isolation, physico-chemical properties and biological activities.
نویسندگان
چکیده
A novel complex of calphostin (UCN-1028), which specifically inhibits protein kinase C (PKC) has been isolated from the culture broth of a fungi Cladosporium cladosporioides. Purification of individual components was carried out by silica gel, non-porus resin Diaion HP-20SS and Sephadex LH-20 chromatography, leading to isolation of five closely related components. A, B, C, D and I. Calphostins showed cytotoxic activities against various tumor cells, and these cytotoxicities were proportional to their inhibitory activities against PKC.
منابع مشابه
Calphostins, novel and specific inhibitors of protein kinase C. II. Chemical structures.
The structures of new antitumor antibiotics, calphostins (UCN-1028) A, B, C, D and I, which are specific and potent inhibitors of protein kinase C, were determined by spectral and chemical studies. All of the antibiotics have a 3,10-perylenequinone skeleton and calphostin D was revealed to be an antipode of isophleichrome.
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ورودعنوان ژورنال:
- The Journal of antibiotics
دوره 42 10 شماره
صفحات -
تاریخ انتشار 1989