Steer, M. L. and Braun, S. and Lester, H. A. and Levitzki, A. (1982) Activation of adenylate cyclase from purified platelet membranes by prostaglandin E1 and its inhibition by L-epinephrine: mechanistic effects. Journal of Cyclic Nucleotide Research, 8 (5). pp. 309-322. ISSN 0095-1544. https://resolver.caltech.edu/CaltechAUTHORS:20201009-153010808
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Abstract
Activation and inhibition of adenylate cyclase in purified human platelet membranes by hormones and guanyl nucleotides was studied. The rate constant of enzyme activation (kon) was measured using the GTP analog guanylimidodiphosphate (Gpp(NH)p), and the rate constant of enzyme deactivation (koff) was determined using the guanosine diphosphate analog guanosine 5'-0-(2-thio)-diphosphate (GDP beta S). PGE1 which was found previously (15) to accelerate kon has been found to accelerate also koff, from 0.1 sec-1 (6 min-1) to 0.2 sec-1 (12 min-1). The alpha 2-adrenergic inhibitory hormone 1-epinephrine did not alter kon, whether measured in the absence or presence of GTP, and also did not alter koff, whether measured under basal or PGE1-dependent GTP-ase activity at any concentration of GTP tested. These results suggest that the alpha 2-adrenergic receptor exerts its inhibitory effect on adenylate cyclase by a mechanism which does not involve its direct interaction with the GTP regulatory protein that is associated with the stimulatory hormone. These results support the view that the inhibitor involves the interaction of the inhibitory receptor with a GTP binding unit separate from the one mediating hormonal stimulation. This regulatory unit attenuates the adenylate cyclase activity either by interacting directly with the catalytic moiety or by modulating the interaction of the stimulatory GTP regulatory protein with the catalytic moiety.
Item Type: | Article | ||||
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ORCID: |
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Additional Information: | © 1982 Raven Press. | ||||
Issue or Number: | 5 | ||||
Record Number: | CaltechAUTHORS:20201009-153010808 | ||||
Persistent URL: | https://resolver.caltech.edu/CaltechAUTHORS:20201009-153010808 | ||||
Usage Policy: | No commercial reproduction, distribution, display or performance rights in this work are provided. | ||||
ID Code: | 105974 | ||||
Collection: | CaltechAUTHORS | ||||
Deposited By: | George Porter | ||||
Deposited On: | 09 Oct 2020 22:36 | ||||
Last Modified: | 09 Oct 2020 22:36 |
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