1-氨基-2-苯乙基膦酸：一种体外L-苯丙氨酸解氨酶抑制剂。

1-Amino-2-phenylethylphosphonic acid: an inhibitor of L-phenylalanine ammonia-lyase in vitro.

作者信息

Janas K M, Filipiak A, Kowalik J, Mastalerz P, Knypl J S

出版信息

Acta Biochim Pol. 1985;32(2):131-43.

Abstract

L(-)-, and D(+)-enantiomers of 1-amino-2-phenylethylphosphonic acid (PheP), a phosphonic analogue of phenylalanine, inhibit the activity of L-phenylalanine ammonia-lyase (EC 4.3.1.5) of potato tuber tissue in vitro. The apparent type of inhibition depends on concentration of PheP; as the concentration of D-PheP is raised from 10(-5) M to 2.5 X 10(-3) M, the type of inhibition shifts from competitive through mixed and non-competitive to uncompetitive. L-PheP exerts either a competitive or mixed-type inhibition at low (10(-6)-10(-5) M) or moderate (5 X 10(-5)-2 X 10(-4) M) concentration. Ki for the concentration range of competitive inhibition were 6.5 X 10(-6) M, 5.3 X 10(-5)M and 1.6 X 10(-5) M for L-, D-, and D,L-PheP, respectively. These Ki values are valid for a relatively narrow range of L-Phe concentration (0.2-4 mM) as L-phenylalanine ammonia-lyase does not follow the Michaelis-Menten kinetics of the reaction.

摘要

苯丙氨酸的膦酸类似物1-氨基-2-苯乙基膦酸（PheP）的L（-）-和D（+）-对映体在体外抑制马铃薯块茎组织的L-苯丙氨酸解氨酶（EC 4.3.1.5）的活性。表观抑制类型取决于PheP的浓度；随着D-PheP的浓度从10^（-5）M提高到2.5×10^（-3）M，抑制类型从竞争性依次转变为混合型、非竞争性和反竞争性。L-PheP在低浓度（10^（-6）-10^（-5）M）或中等浓度（5×10^（-5）-2×10^（-4）M）时表现为竞争性或混合型抑制。L-、D-和D,L-PheP在竞争性抑制浓度范围内的Ki值分别为6.5×10^（-6）M、5.3×10^（-5）M和1.6×10^（-5）M。由于L-苯丙氨酸解氨酶不遵循该反应的米氏动力学，这些Ki值仅在相对较窄的L-苯丙氨酸浓度范围（0.2-4 mM）内有效。