Crystal structures of reversible ketone-Based inhibitors of the cysteine protease cruzain.

Huang L; Brinen LS; Ellman JA

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Crystal structures of reversible ketone-Based inhibitors of the cysteine protease cruzain.

机译：Crystal structures of reversible ketone-Based inhibitors of the cysteine protease cruzain.

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摘要

The crystal structures of two hydroxymethyl ketone inhibitors complexed to the cysteine protease cruzain have been determined at 1.1 and 1.2 A resolution, respectively. These high resolution crystal structures provide the first structures of non-covalent inhibitors bound to cruzain. A series of compounds were prepared and tested based upon the structures providing further insight into the key binding interactions.

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来源
《Bioorganic and medicinal chemistry》 |2003年第1期|21-29|共9页
作者
Huang L; Brinen LS; Ellman JA;
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作者单位

Center for New Directions in Organic Synthesis, Department of Chemistry, University of California, CA, 94720, Berkeley, USA;

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正文语种英语
中图分类药学;生物化学;
关键词
inhibitors; cruzain; Endopeptidases; Ketones; Cysteine; 酮类; 半胱氨酸;

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Crystal structures of reversible ketone-Based inhibitors of the cysteine protease cruzain.

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