Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:4.6.1.1 (adenylate cyclase)
 19,190 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Treatment of membranes from the dog caudate nucleus with sulfhydryl alkylating agents, N-ethylmaleimide and p-chloromercuribenzoate, results in selective inhibition of dopamine-sensitive adenylate cyclase activity that can be distinguished from effects on basal enzyme activity. Fifty per cent inhibition of dopamine-sensitive adenylate cyclase activity was observed in the presence of 10(-5) M N-ethylmaleimide and 3 X 10(-6) M p-chloromercuribenzoate. N-Ethylmaleimide (10(-5) M or less) also inhibited GTP- and NaF-stimulated adenylate cyclase activity, but had no effect on basal adenylate cyclase activity (assayed in the presence of magnesium) and on enzyme activity assayed in the presence of manganese. The reducing agents dithiothreitol, 2-mercaptoethanol, glutathione, and cysteine had no inhibitory effect on dopamine-sensitive adenylate cyclase activity. Pretreatment of membranes with guanyl-5'-yl imidodiphosphate or guanosine 5'-O-(3-thio)triphosphate prior to incubation with N-ethylmaleimide prevented the inhibitory effect of N-ethylmaleimide on adenylate cyclase activity. The results suggest that a reactive sulfhydryl group in the domain of the GTP-binding protein is important for the coupling of the components of the dopamine-sensitive adenylate cyclase complex in brain.
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PMID:Selective effects of an essential sulfhydryl group on the activation of dopamine- and guanine nucleotide-sensitive adenylate cyclase. 715 25

[3H]Acetylcholine release elicited with 360 pulses/3 Hz from slices of rabbit hippocampus is facilitated in the presence of the muscarine (M) receptor antagonist atropine (indicating the existence of autoinhibition) and diminished by the M receptor agonists carbachol and oxotremorine. N-Ethylmaleimide (30 microM) and pertussis toxin (8 micrograms/ml) counteracted antagonist-induced facilitation and agonist-induced inhibition of release, suggesting that a pertussis toxin-sensitive GTP-binding protein is involved in the chain of events mediating activation of M receptors to inhibition of release. Neither 8-bromo-cyclic AMP (300 microM), a membrane analogue of cyclic AMP, nor rolipram (10 microM), a phosphodiesterase inhibitor, affected electrically evoked release of [3H]acetylcholine. They also did not influence the oxotremorine-induced inhibition of transmitter release. In conclusion, no evidence was found for the assumption that activation of M autoreceptors is linked to inhibition of adenylate cyclase.
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PMID:Muscarine receptors regulating electrically evoked release of acetylcholine in hippocampus are linked to pertussis toxin-sensitive G proteins but not to adenylate cyclase. 836 Jun 71


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