Michael E. Friedman , Paul Melius , Charles A. McAuliffe
{"title":"顺铂胺配合物的抗肿瘤行为与其抑制模型酶的机制","authors":"Michael E. Friedman , Paul Melius , Charles A. McAuliffe","doi":"10.1016/S0006-3061(00)80168-4","DOIUrl":null,"url":null,"abstract":"<div><p>The twenty-four hour inhibition of m-malate dehydrogenase (E.C. 1.1.1.37)<span><sup>1</sup></span> by various complexes of cis-platinum(II) and <em>cis</em>-platinum(IV) was measured as a function of the platinum concentration. It was observed that increased alkylation of the amine groups of Pt(II) and to a lesser degree of Pt(IV) decreased the activity consistently. It was also observed that the Pt(IV) analogues inhibit the enzyme to about an order of magnitude greater than the Pt(II) complexes. These phenomena will be interpreted.</p></div>","PeriodicalId":9177,"journal":{"name":"Bioinorganic chemistry","volume":"8 4","pages":"Pages 355-361"},"PeriodicalIF":0.0000,"publicationDate":"1978-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/S0006-3061(00)80168-4","citationCount":"4","resultStr":"{\"title\":\"A proposed mechanism relating the antitumor behavior of cis-platinum amine complexes to their inhibition of a model enzyme\",\"authors\":\"Michael E. Friedman , Paul Melius , Charles A. McAuliffe\",\"doi\":\"10.1016/S0006-3061(00)80168-4\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>The twenty-four hour inhibition of m-malate dehydrogenase (E.C. 1.1.1.37)<span><sup>1</sup></span> by various complexes of cis-platinum(II) and <em>cis</em>-platinum(IV) was measured as a function of the platinum concentration. It was observed that increased alkylation of the amine groups of Pt(II) and to a lesser degree of Pt(IV) decreased the activity consistently. It was also observed that the Pt(IV) analogues inhibit the enzyme to about an order of magnitude greater than the Pt(II) complexes. These phenomena will be interpreted.</p></div>\",\"PeriodicalId\":9177,\"journal\":{\"name\":\"Bioinorganic chemistry\",\"volume\":\"8 4\",\"pages\":\"Pages 355-361\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1978-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1016/S0006-3061(00)80168-4\",\"citationCount\":\"4\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Bioinorganic chemistry\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0006306100801684\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Bioinorganic chemistry","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0006306100801684","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
A proposed mechanism relating the antitumor behavior of cis-platinum amine complexes to their inhibition of a model enzyme
The twenty-four hour inhibition of m-malate dehydrogenase (E.C. 1.1.1.37)1 by various complexes of cis-platinum(II) and cis-platinum(IV) was measured as a function of the platinum concentration. It was observed that increased alkylation of the amine groups of Pt(II) and to a lesser degree of Pt(IV) decreased the activity consistently. It was also observed that the Pt(IV) analogues inhibit the enzyme to about an order of magnitude greater than the Pt(II) complexes. These phenomena will be interpreted.