Covalent sequestration of melphalan by metallothionein and selective alkylation of cysteines.

Yu X; Wu Z; Fenselau C

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Covalent sequestration of melphalan by metallothionein and selective alkylation of cysteines.

机译：金属硫蛋白共价螯合美法仑和半胱氨酸的选择性烷基化。

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Rabbit liver metallothionein-2 is shown to form covalent bonds with the anticancer agent melphalan, in support of the hypothesis that covalent sequestration by metallothionein constitutes one mechanism for the cross-resistance acquired by cancer patients to therapeutic alkylating agents. Among 20 cysteines in the 2-domain protein, 89% of the first alkylation reaction occurs with 2 that cochelate a zinc cation in the carboxy domain. Computer-supported docking studies indicate a favorable binding site for melphalan near these cysteine sulfhydryl groups. Although folded metallothionein-2 is resistant to trypsin cleavage, alkylation by 1 mol of melphalan allows cleavage by trypsin between the two globular domains.

机译：显示兔肝金属硫蛋白-2与抗癌药美法仑形成共价键，支持以下假设：金属硫蛋白的共价螯合构成癌症患者获得的对治疗性烷化剂的交叉耐药性的一种机制。在2结构域蛋白中的20个半胱氨酸中，发生89％的第一次烷基化反应与2螯合羧基结构域中的锌阳离子。计算机支持的对接研究表明，在这些半胱氨酸巯基附近，美法仑具有良好的结合位点。尽管折叠的金属硫蛋白-2对胰蛋白酶的切割有抵抗力，但是1摩尔马法兰的烷基化允许胰蛋白酶在两个球状结构域之间切割。

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《Biochemistry》 |1995年第10期|共9页
作者
Yu X; Wu Z; Fenselau C;
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正文语种 eng
中图分类生物化学;
关键词
Melphalan; Metallothionein; Peptide Fragments; Cysteine; 美法仑; 金属硫蛋白;

机译：Melphalan;Metallothionein;Peptide Fragments;Cysteine;美法仑;金属硫蛋白;

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专利

1. Covalent sequestration of melphalan by metallothionein and selective alkylation of cysteines. [J] . Yu X, Wu Z, Fenselau C Biochemistry . 1995,第10期

机译：金属硫蛋白共价螯合美法仑和半胱氨酸的选择性烷基化。
2. Covalent sequestration of phosphoramide mustard by metallothionein--an in vitro study. [J] . Wei D, Fabris D, Fenselau C Drug Metabolism and Disposition: The Biological Fate of Chemicals . 1999,第7期

机译：金属硫蛋白共价螯合磷酰胺芥末的体外研究。
3. Covalent sequestration of the nitrogen mustard mechlorethamine by metallothionein. [J] . Antoine M, Fabris D, Fenselau C Drug Metabolism and Disposition: The Biological Fate of Chemicals . 1998,第9期

机译：金属硫蛋白共渗氮芥子甲氧乙胺。
4. Analysing covalent protein-drug adducts: protein-melphalan adducts [C] . Debbie Dewaele, Geert Baggerman, Frank Sobott, International Mass Spectrometry Conference . 2014

机译：分析共价蛋白 - 药物加合物：蛋白质 - Melphalan加合物
5. Part I. The use of covalently attached synthetic metalloporphyrins in the remote site-selective hydroxylation of steroids. Part II. The use of ionically coordinated metalloporphyrins in the remote site-selective hydroxylation of steroids. [D] . Stuk, Timothy Lee. 1991

机译：第一部分共价连接的合成金属卟啉在类固醇的远程部位选择性羟基化中的用途。第二部分离子配位的金属卟啉在类固醇的远程位点选择性羟基化中的使用。
6. Biomphalaria glabrata Metallothionein: Lacking Metal Specificity of the Protein and Missing Gene Upregulation Suggest Metal Sequestration by Exchange Instead of through Selective Binding [O] . Michael Niederwanger, Sara Calatayud, Oliver Zerbe, 1999

机译：Biomphalaria glabrata Metallothionein：缺乏蛋白质的金属特异性和缺少基因上调表明通过交换而不是通过选择性结合的金属螯合。
7. Biomphalaria glabrata Metallothionein: Lacking Metal Specificity of the Protein and Missing Gene Upregulation Suggest Metal Sequestration by Exchange Instead of through Selective Binding [O] . Niederwanger, Michael, Calatayud, Sara, Zerbe, Oliver, 2017

机译：Biomphalaria glabrata Metallothionein：缺乏蛋白质的金属特异性和缺少基因上调表明通过交换而不是通过选择性结合的金属螯合。

Covalent sequestration of melphalan by metallothionein and selective alkylation of cysteines.

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