Calphostins (UCN-1028), novel and specific inhibitors of protein kinase C. I. Fermentation, isolation, physico-chemical properties and biological activities.
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.
Kobayashi
E
E
Tokyo Research Laboratory, Kyowa Hakko Kogyo Co., Ltd., Tokyo, Japan.
Ando
K
K
Nakano
H
H
Iida
T
T
Ohno
H
H
Morimoto
M
M
Tamaoki
T
T
D000903:Antibiotics, Antineoplastic / Q000032:analysis / Q000302:isolation & purification* / Q000494:pharmacology; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002851:Chromatography, High Pressure Liquid; D002963:Cladosporium / Q000378:metabolism; D005285:Fermentation; D006367:HeLa Cells / Q000187:drug effects; D009281:Naphthalenes; D011083:Polycyclic Compounds / Q000032:analysis* / Q000302:isolation & purification* / Q000494:pharmacology; D011493:Protein Kinase C / Q000037:antagonists & inhibitors*
D000903:Antibiotics, Antineoplastic; D009281:Naphthalenes; D011083:Polycyclic Compounds; C061465:calphostin complex; C058747:calphostin A; C061462:calphostin B; C061464:calphostin I; D011493:Protein Kinase C; C061463:calphostin D; C058819:calphostin C