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[Antithrombic Activity of N(alpha)-lauroyl-L-arginine Ethyl Ester (LAE) and 9-fluorenylmethoxycarbonyl-L-arginine Methyl Ester (Fmoc-L-Arg-OMe)]

[Antithrombic Activity of N(alpha)-lauroyl-L-arginine Ethyl Ester (LAE) and 9-fluorenylmethoxycarbonyl-L-arginine Methyl Ester (Fmoc-L-Arg-OMe)]

A A Poiarkov, S A Poiarkova, V P Kukhar'

Ukr Biokhim Zh (1999). Jan-Feb 2007;79(1):124-31.

PMID: 18030741

Abstract:

Simple synthetic compounds of lauroyl-arginine ethyl ester (LAE) and 9-fluorenylmethoxycarbonyl-L-agrinine methyl ester (Fmoc-Arg-OMe) were studied for their inhibitory effect on the hydrolysis of chromogenic substrate Tos-Gly-Pro-Arg-pNA (Chromozym TH) by thrombin with K(i) for LAE 1.92 microM and 77 microM for Fmoc Arg-OMe. It was shown that LAE inhibits thrombin activity almost 20 times more strongly than trypsin (K(i) = 18.9 microM). At the same time LAE preserves the ability to be hydrolyzed by thrombin at pH 8.5 (k(cat) = 3.6 c(-1)) and trypsin (k(cat) = 56 c(-1)). It is suggested, that LAE ability to suppress growth of some microorganisms is conditioned to some extent by its ability to inhibit the activity of trypsin-like serine proteases, participating in the infection process.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP181434855	Lauroyl arginine		181434-85-5	Price

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