Abstract
THE presence on the cholinergic receptor of a critical disulphide bond has been demonstrated and localised to within 10 Å of the cholinergic receptor anionic binding subsite1–4. Reduction of this bond by dithiothreitol results in a reduced response of the nicotinic cholinergic receptor to acetylcholine (ACh) in many systems1,5–8. I report here that heterolytic cleavage of this disulphide bond is produced using sodium bisulphite, a reagent which shows a high degree of specificity, reactivity and reversibility of interaction with the disulphide bond9. The active agent is the bisulphite ion, the reaction being RSSR + HSO2−3⇄RSSO−3 + HSR and resulting in the addition of the strongly nucleophilic sulphonate group to the receptor. The addition of this group seems to modify the ACh receptor–ionophore complex in a unique manner which results in an increase in its response to ACh.
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STEINACKER, A. Sulphonation of cholinergic receptor disulphide bond increases response to ACh. Nature 278, 358–360 (1979). https://doi.org/10.1038/278358a0
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DOI: https://doi.org/10.1038/278358a0
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