[Thrombin substrates containing aminobenzoic acids].
In order to study the interactions of synthetic substrates with the active site of thrombin the compounds of R-CO-Abz-Arg-OMe were obtained which contained, o-, m- and p-amino benzoic acids (Abz) at P2-subsite. R-CO-moiety was butyric, perfluorobutyric, benzoyl, 2-fluorobenzoyl and perfluorobenzoyl groups. Kinetic parameters of their hydrolysis by thrombin were measured and antithrombin activity was studied. Introduction of fluorine atoms into N-acyl groups caused insignificant alterations of the substrate or inhibitor properties of the compounds containing N-butyric group, but significantly influenced the substrate properties, when peptides contained N-benzoyl group. The interaction mechanism of the obtained substrates with thrombin was proposed.
Gershkovich
A A
AA
Podlipskiĭ
V Ia
VIa
Kostiuchenko
N V
NV
Karabut
L I
LI
Kibirev
V K
VK
D000595:Amino Acid Sequence; D062365:Aminobenzoates / Q000737:chemistry*; D000991:Antithrombins / Q000378:metabolism; D001665:Binding Sites; D006868:Hydrolysis; D007700:Kinetics; D008969:Molecular Sequence Data; D015394:Molecular Structure; D013237:Stereoisomerism; D013379:Substrate Specificity; D013917:Thrombin / Q000737:chemistry*
D062365:Aminobenzoates; D000991:Antithrombins; D013917:Thrombin