{"title":"Characterization of estrone hydroxylase activities in porcine endometrial cells.","authors":"J Adamski, E Hohls, P W Jungblut","doi":"10.1055/s-0029-1211309","DOIUrl":null,"url":null,"abstract":"<p><p>The oxidation of estradiol to estrone in porcine endometrial cells is succeeded by hydroxylation at either 6 alpha- or 7 alpha-. The products are devoid of receptor affinity. Their formation is inhibited by cytochrome P450 blockers like ketoconazol but not by chloroquine and analogues. The hydroxylation at 6 alpha- proceeds with KM = 1.9 x 10(-7) M, that at 7 alpha- with KM = 3.6 x 10(-7) M. The respective values for the cytochrome P450-reductase cosubstrate NADPH are 1.7 x 10(-5) M and 1.9 x 10(-5) M. The kinetic parameters of the enzymes are compatible with a metabolic sequence: estradiol-->estrone--> 6 alpha/17 alpha-estrone.</p>","PeriodicalId":12104,"journal":{"name":"Experimental and clinical endocrinology","volume":"102 5","pages":"388-93"},"PeriodicalIF":0.0000,"publicationDate":"1994-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1055/s-0029-1211309","citationCount":"3","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Experimental and clinical endocrinology","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1055/s-0029-1211309","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 3
Abstract
The oxidation of estradiol to estrone in porcine endometrial cells is succeeded by hydroxylation at either 6 alpha- or 7 alpha-. The products are devoid of receptor affinity. Their formation is inhibited by cytochrome P450 blockers like ketoconazol but not by chloroquine and analogues. The hydroxylation at 6 alpha- proceeds with KM = 1.9 x 10(-7) M, that at 7 alpha- with KM = 3.6 x 10(-7) M. The respective values for the cytochrome P450-reductase cosubstrate NADPH are 1.7 x 10(-5) M and 1.9 x 10(-5) M. The kinetic parameters of the enzymes are compatible with a metabolic sequence: estradiol-->estrone--> 6 alpha/17 alpha-estrone.
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