Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: EC:2.7.11.13 (
protein kinase C
)
49,245
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
The inhibitory effects of gold compounds on the NADPH oxidase system of human polymorphonuclear leukocytes (PMNs) has been investigated. Auranofin (0.5-4.0 micrograms Au/ml) suppressed the rate of superoxide anion generation as well as the total yield in cells stimulated with phorbol myristate acetate and f-Met-Leu-Phe. This implies that drug action may be occurring at the level of
protein kinase C
or steps subsequent to this in the signal transduction sequence.
Sodium aurothiomalate
(1-100 micrograms Au/ml) lacked such activity. Neither gold compound altered the ability of the granule-rich fraction of PMNs to produce oxy radicals whether this fraction was obtained from drug-treated cells or was treated after its isolation. Therefore, in order for auranofin to exhibit its inhibitory effects on the NADPH oxidase system, an intact cell membrane is necessary.
...
PMID:Effect of gold compounds on NADPH oxidase system of human neutrophils. 301 58
Slow translocation of
protein kinase C
was observed by both auranofin and gold sodium thiomalate pretreatment of neutrophils. Both gold compounds failed to influence the activity of this enzyme directly when cell-free studies were performed. In intact neutrophils incubated with 5.1-20.3 microM auranofin,
protein kinase C
activity decreased in the cytosol in a time- and dose-dependent manner. Concomitantly, the levels of the membrane-associated
protein kinase C
were significantly elevated, although the amount of activity recovered could not account for that lost from the cytosol.
Gold sodium thiomalate
(5.0 microM-0.505 mM) demonstrated similar effects but with lesser potency than auranofin. In confirmation of previous results, phorbol myristate acetate (PMA), a cellular stimulus, also induced the translocation of
protein kinase C
. Key differences were that the reaction was rapid (occurring within minutes after PMA addition) and that relative recovery of kinase activity from the particulate fraction was fourfold greater. The relationship between gold compound-mediated kinase C redistribution and inhibition of neutrophil responses remains to be elucidated.
...
PMID:Gold compounds alter distribution of protein kinase C activity in human neutrophils. 365 80
