AdoHcy hydrolase of Trichomonas vaginalis: Studies of the effects of 5′-modified adenosine analogues and related 6-N-cyclopropyl derivatives

被引：3

作者：

Dornbush, Padraick J. ^{[1
]}

Vazquez-Anaya, Guillermo ^{[1
]}

Shokar, Ajit ^{[1
]}

Benson, Saoly ^{[1
]}

Rapp, Magdalena ^{[2
]}

Wnuk, Stanislaw F. ^{[2
]}

Wrischnik, Lisa A. ^{[1
]}

Land, Kirkwood M. ^{[1
]}

机构：

[1] Univ Pacific, Dept Biol Sci, Stockton, CA 95211 USA

[2] Florida Int Univ, Dept Chem & Biochem, Miami, FL 33199 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 24期

关键词：

Trichomonas vaginalis; AdoHcy Hydrolase; 5 '-Modified adenosine analogue; 6-N-Cylcopropyl derivative; L-HOMOCYSTEINE HYDROLASE; S-ADENOSYLHOMOCYSTEINE HYDROLASE; INACTIVATION; ANTICANCER; INHIBITORS; ACID;

D O I：

10.1016/j.bmcl.2010.10.014

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Trypanosoma brucei and Trichomonas vaginalis are both parasitic protozoans that are known to share many similar biochemical pathways. Aristeromycin, as well as 5 '-iodovinyl and 5 '-oxime analogues of adenosine, are potent inhibitors of AdoHcy hydrolase in T. brucei, an enzyme that catalyses the hydrolysis of AdoHcy to adenosine and L-homocysteine. To help determine the role of this enzyme in T. vaginalis, we have tested a library of 5 '-modified adenosine derivatives, including 5 '-deoxy-5 '-( iodomethylene)-adenosine and related 6-N-cyclopropyl analogues. Our results indicate that these inhibitors are effective at inhibiting the growth of T. vaginalis, by as much as 95%. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：7466 / 7468

页数：3