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GS4071是一种对甲型和乙型流感病毒株的神经氨酸酶均具有慢结合抑制作用的抑制剂。

GS4071 is a slow-binding inhibitor of influenza neuraminidase from both A and B strains.

作者信息

Kati W M, Saldivar A S, Mohamadi F, Sham H L, Laver W G, Kohlbrenner W E

机构信息

Infectious Diseases Research, Abbott Laboratories, Illinois 60064, USA.

出版信息

Biochem Biophys Res Commun. 1998 Mar 17;244(2):408-13. doi: 10.1006/bbrc.1998.8282.

Abstract

The kinetics of inhibition of purified influenza neuraminidases from A/Tokyo/3/67 and B/Memphis/3/89 influenza viruses by (3R,4R,5S)-4-acetamido-5-amino-3-(1-ethylpropoxy)-1-cyclohexene- 1-carboxylic acid (GS4071) were investigated. Progress curve experiments established that GS4071 is a time dependent inhibitor of both A and B strains of influenza neuraminidase. The apparent association and dissociation rate constants, as well as the overall Ki values, were only modestly different for the two neuraminidase strains. The time dependent inhibition phenomenon, often referred to as slow-binding inhibition, appears to be a consequence of the very slow rate of dissociation of the compound from influenza neuraminidase.

摘要

研究了(3R,4R,5S)-4-乙酰氨基-5-氨基-3-(1-乙基丙氧基)-1-环己烯-1-羧酸(GS4071)对A/东京/3/67和B/孟菲斯/3/89流感病毒纯化的神经氨酸酶的抑制动力学。进程曲线实验表明,GS4071是甲型和乙型流感神经氨酸酶的时间依赖性抑制剂。两种神经氨酸酶菌株的表观缔合和解离速率常数以及总体Ki值仅有适度差异。时间依赖性抑制现象,通常称为慢结合抑制,似乎是该化合物从流感神经氨酸酶解离速率非常缓慢的结果。

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