苯丙氨酸解氨酶抑制剂：苯环上被取代的1-氨基苄基膦酸

Inhibitors of phenylalanine ammonia-lyase: 1-aminobenzylphosphonic acids substituted in the benzene ring.

作者信息

Zon Jerzy, Amrhein Nikolaus, Gancarz Roman

机构信息

Institute of Organic Chemistry, Biochemistry and Biotechnology, Wroclaw University of Technology, Wybrzeze Wyspianskiego 27, 50-370, Wroclaw, Poland.

出版信息

Phytochemistry. 2002 Jan;59(1):9-21. doi: 10.1016/s0031-9422(01)00425-3.

DOI:10.1016/s0031-9422(01)00425-3

PMID:11754939

Abstract

Dextrorotatory 1-amino-3',4'-dichlorobenzylphosphonic acid was found to be a potent inhibitor of the plant enzyme phenylalanine ammonia-lyase both in vitro and in vivo from among the ring-substituted 1-aminobenzylphosphonic acids and other analogues of phenylglycine. A structure activity relationship analysis of the results obtained permits predictions on the geometry of the pocket of the enzyme and is a basis in the strategy of better inhibitor synthesis.

摘要

在环取代的1-氨基苄基膦酸和苯甘氨酸的其他类似物中，发现右旋1-氨基-3'，4'-二氯苄基膦酸在体外和体内都是植物酶苯丙氨酸解氨酶的有效抑制剂。对所得结果进行的构效关系分析有助于预测酶口袋的几何形状，并且是更好地合成抑制剂策略的基础。