Chelerythrine inhibits the secretory response of human blood platelets without specifically inhibiting protein kinase c - 4 0 16; Trevor Land and Philipp Novales-Li; 5 (Taguig, Metro Manila : STII-DOST, 1997)
ABSTRACT : Chelerythrine (chloride) has previously been documented to be a potent and selective inhibitor of the serine/threonine-specific protein kinase C (PKC). In this study, it was shown that 10 pM chelerythrine completely inhibited serotonin secretion and partially inhibited phosphatidic acid formation. In human blood platelets activated by thrombin, (1U/ml). However, there was no effect on PKC activity, as assessed by the level of phosphorylation of the 47 Kd protein. Therefore, chelerythrine has been shown not to be a specific inhibitor of PKC and without specifically affecting PKC activity, is nevertheless capable of completely inhibiting platelet secretion, indicating that it may affect the signal transductionpathway responsible for platelet secretion at a point dwostream or independent of PKC.
Keywords: 2 -- 0; 6; Protein Kinase C -- Medicine -- Chelerythrine -- Human Blodd Platelets; 20; 2