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KARI酶及其抑制剂
  • 期刊名称：化学进展，2008，20（11），1788-1797
  • 时间：0
  • 分类：Q559[生物学—生物化学] O629.12[理学—有机化学;理学—化学]
  • 作者机构：[1]南开大学元素有机化学国家重点实验室农药国家工程研究中心（天津）,天津300071
  • 相关基金：国家重点基础研究计划（973）项目（No.2003CB114406）,国家自然科学重点基金项目（No.20432010）,高等学校博士学科点专项科研基金（No.20070055044）,天津市应用基础及前沿技术研究计划项目（No.08JCYBJC00800,07JCYBJC00200）资助
  • 相关项目：生物合理设计绿色农药的分子基础研究
关键词： KARI, 抑制剂, 构效关系, 药物设计, KARI , inhibitors , SAR , drug design
中文摘要：

酮醇酸还原异构酶（keto-acid reductoisomerase，KARI或称作乙酰羟基酸异构还原酶（aceto hydroxyacid isomeroreductase，AHIR））是植物、微生物中的支链氨基酸生物合成途径中第二步的关键酶。由于哺乳动物和人体内不存在这种酶，因此靶向KARI酶的抑制剂具有安全、高效等特点，成为农用除草剂以及医药抗真菌药物的一个引入注目的研究方向。本文综述了KARI的酶学、KARI抑制剂及其抑制机理和理论研究进展，并对其发展趋势进行了展望。

英文摘要：

Keto-acid reductoisomerase （KARI; EC 1.1.1.86） is an attractive target for argochemical discovery because it catalyzes the second important step in the biosynthesis of the branched chain amino acid which exists in higher plants and certain fungi only but not in animals. Thus it is an ideal target from which to design non-toxic KARI-inhibitors as potential novel herbicides and antibiotics. The X-ray crystallography of the KARl enzyme, inhibitors and their inhibit mechanism, and theoretical research are reviewed.

同期刊论文项目
生物合理设计绿色农药的分子基础研究
期刊论文 141 会议论文 29
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