{"title":"新斯的明与青霉素的作用机制","authors":"T. Alston","doi":"10.2174/1874321800802010046","DOIUrl":null,"url":null,"abstract":"The molecular mechanism of penicillin action is closely analogous to that of neostigmine. Both drugs react co- valently with the active-site serine of their target enzymes. In both cases, the susceptible enzymes self-catalyze their inac- tivation by their respective drugs. Kinetic analysis of cholinesterase by Richard J. Kitz and Irwin B. Wilson helped to es- tablish that concept. Neostigmine and penicillin are kindred examples of mechanism-based enzyme inhibition, a generally important phenomenon in pharmacology and physiology.","PeriodicalId":272376,"journal":{"name":"The Open Anesthesiology Journal","volume":"28 1","pages":"0"},"PeriodicalIF":0.0000,"publicationDate":"2008-06-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"2","resultStr":"{\"title\":\"Kitz-Wilson Mechanisms of Action of Neostigmine and Penicillin\",\"authors\":\"T. Alston\",\"doi\":\"10.2174/1874321800802010046\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"The molecular mechanism of penicillin action is closely analogous to that of neostigmine. Both drugs react co- valently with the active-site serine of their target enzymes. In both cases, the susceptible enzymes self-catalyze their inac- tivation by their respective drugs. Kinetic analysis of cholinesterase by Richard J. Kitz and Irwin B. Wilson helped to es- tablish that concept. Neostigmine and penicillin are kindred examples of mechanism-based enzyme inhibition, a generally important phenomenon in pharmacology and physiology.\",\"PeriodicalId\":272376,\"journal\":{\"name\":\"The Open Anesthesiology Journal\",\"volume\":\"28 1\",\"pages\":\"0\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2008-06-05\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"2\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"The Open Anesthesiology Journal\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.2174/1874321800802010046\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"The Open Anesthesiology Journal","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.2174/1874321800802010046","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 2
摘要
青霉素作用的分子机制与新斯的明非常相似。两种药物都与其靶酶的活性位点丝氨酸共价反应。在这两种情况下，易感酶通过各自的药物自我催化灭活。Richard J. Kitz和Irwin B. Wilson对胆碱酯酶的动力学分析帮助我们确立了这一概念。新斯的明和青霉素是类似的基于机制的酶抑制的例子，这是药理学和生理学中普遍重要的现象。
Kitz-Wilson Mechanisms of Action of Neostigmine and Penicillin
The molecular mechanism of penicillin action is closely analogous to that of neostigmine. Both drugs react co- valently with the active-site serine of their target enzymes. In both cases, the susceptible enzymes self-catalyze their inac- tivation by their respective drugs. Kinetic analysis of cholinesterase by Richard J. Kitz and Irwin B. Wilson helped to es- tablish that concept. Neostigmine and penicillin are kindred examples of mechanism-based enzyme inhibition, a generally important phenomenon in pharmacology and physiology.
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