Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:4.6.1.2 (guanylate cyclase)
 8,497 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Guanidine thiol derivatives--a new class of soluble guanylate cyclase activators--have been studied. Guanidine thiols contain in their molecule both the guanidine and thiol groups which act as donors acceptors of nitric oxide (NO), respectively. The role of the guanidine thiol SH-groups in the mechanism of soluble guanylate cyclase activation has been evaluated. The effect of three guanidine thiol derivatives: mercaptoethylguanidine (MEG), mercaptoethylguanidine disulfide (MEG disulfide) and S-methyl mercaptoethylguanidine (S-methyl MEG) on human platelet guanylate cyclase activity, has been examined. It was found that all the compounds tested in this study were substrates for NO-synthase and guanylate cyclase activators. The stimulatory effects of MEG and MEG disulfide surpassed the L-arginine-induced activation of guanylate cyclase-2- and 4-fold, respectively. The enzyme stimulation by S-methyl MEG was of the same order as that of L-arginine. The important role of S-acceptor groups of guanidine thiols in the mechanism of directed increase of guanylate cyclase activation was established. This mechanism explains the nature of differences in the intensity of guanylate cyclase activation by the guanidine thiols under study. The NO-acceptor properties of disulfide bond of guanidine thiols in the case of the NO-synthase mechanism of NO formation have been established.
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PMID:[The role of SH-groups in guanidine thiols--new substrates for NO-synthase--in stimulating the activity of guanylate cyclase]. 867 71

The study is concerned with the mechanism of activation of soluble guanylate cycla-se by guanidine thiol derivatives-a new class of enzyme activators. Guanidine thiols contain both the guanidine and SH group which act, respectively, as donor and acceptor of nitric oxide (NO). The role of guanidine thiol SH group in the mechanism of soluble guanylate cyclase activation was studied. Three guanidine thiol derivatives were tested: mercaptoethylguanidine, its disulfide and S-methyl mercaptoethylguani-dine. All three compounds proved to be NO-synthase substrates and, simultaneously, guanylate cyclase activators. The degrees of guanylate cyclase activation by mercaptoethylguanidine and its disulfide were, respectively, two and four times higher than that by L-arginine. The stimulatory effects of S-methyl mercaptoethylguanidine and L-arginine were evaluated and found to be of the same order. The important role of S-acceptor group of guanidine thiols in the mechanism of guanylate cyclase activation increase provides an explanation for different intensities of guanylate cyclase activation by the compounds tested. NO-acceptor properties of guanidine thiols disulfide bonds in the synthase mechanism of NO generation were first reported.
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PMID:Mechanism of activation of soluble guanylate cyclase by guanidine thiols--a new class of enzyme activators. 882 10