PMID: 1003107Dec 1, 1976

Activation of stimulus-specific serine esterases (proteases) in the initiation of platelet secretion. I. Demonstration with organophosphorus inhibitors

The Journal of Experimental Medicine
P M HensonE L BECKER

Abstract

The effect of organophosphorus inhibitors of serine esterases (proteases) on secretion from washed rabbit platelets was examined. Five noncytotoxic stimuli were employed: collagen, thrombin, heterologous anti-platelet antibody (in the absence of complement), rabbit C3 bound to zymosan, and platelet activating factor derived from antigen-stimulated, IgE-sensitized rabbit basophils. Diisoprophyl phosphofluoridate, three series of p-nitrophenyl ethyl phosphonates, and a series of cyclohexyl phenylalkylphosphonofluridates were all found to be inhibitory to the platelet secretion. These are irreversible inhibitors of serine proteases but in this system were only inhibitory if added to the platelets concurrently with the stimuli. Pretreatment of either the platelets or the stimuli with the inhibitors followed by washing, was without effect on the subsequent reaction. This suggested the involvement of stimulus-activatable serine proteases in the secretory process. The concept was supported by finding that nonphosphorylating phosphonates or hydrolyzed phosphonates or phosphonofluoridates were without inhibitory action. The effect of a series of phosphonates or phosphonoflouridates in inhibiting each stimulus exhibited a unique activity...Continue Reading

References

Jan 1, 1989·Clinical and Experimental Hypertension. Part A, Theory and Practice·J H Campbell, G R Campbell
Mar 1, 1983·Bioscience Reports·G T Gustafson, U Lerner
Nov 1, 1991·Prostaglandins, Leukotrienes, and Essential Fatty Acids·J SugataniK Saito
Aug 29, 1978·Biochemical and Biophysical Research Communications·L W HeckH G Remold

Citations

Jan 1, 1972·International Archives of Allergy and Applied Immunology·N S Ranadive, J D Muir
Jun 1, 1967·The Journal of Experimental Medicine·P A Ward, E L BECKER
Nov 1, 1972·Proceedings of the National Academy of Sciences of the United States of America·P H MorganH Neurath
Jul 1, 1970·British Journal of Haematology·N G ArdlieJ F Mustard
Oct 1, 1969·The Journal of Experimental Medicine·D S PearlmanE L BECKER
Apr 1, 1968·The Journal of Experimental Medicine·P A Ward, E L BECKER
Sep 1, 1965·Journal of Medicinal Chemistry·L S HafnerB H Alexander

Related Concepts

Complement C3 precursor
Floropryl
Secretory Rate
Zyderm
Esterases
Gamma-Thrombin
Zymosan
Blood Platelets
Hydroxytryptamine
Organophosphonates

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