Catalytic inactivation of human carbonic anhydrase I by a metallopeptide-sulfonamide conjugate is mediated by oxidation of active site residues

被引:32
作者
Gokhale, Nikhil H. [1 ]
Bradford, Seth [1 ]
Cowan, J. A. [1 ]
机构
[1] Ohio State Univ, Evans Lab Chem, Columbus, OH 43210 USA
关键词
D O I
10.1021/ja0778038
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Oxidation of active site residues (His and Trp), following catalytic inactivation of human carbonic anhydrase I by a copper-ATCUN conjugate of sulfanilimide, is evidenced by mass spectrometric analysis of tryptic and chymotryptic digest of the modified CA-I. Accordingly, residue oxidation rather than protein cleavage is the demonstrated mods of inactivation. An apparent second-order rate constant, k(2) similar to 7600 M(-1)min(-1), has been determined for catalytic inactivation of CA-I.
引用
收藏
页码:2388 / 2389
页数:2
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