Farnesyltransferase inhibitors inhibit the growth of malaria parasites in vitro and in vivo

被引：73

作者：

Wiesner, J

Kettler, K

Sakowski, J

Ortmann, R

Katzin, AM

Kimura, EA

Silber, K

Klebe, G

Jomaa, H

Schlitzer, M

机构：

[1] Univ Munich, Dept Pharm, Zentrum Pharmaforsch, D-81377 Munich, Germany

[2] Univ Giessen, Inst Biochem, D-35392 Giessen, Germany

[3] Univ Sao Paulo, Inst Ciencias Biomed, BR-05508900 Sao Paulo, Brazil

[4] Univ Marburg, Inst Pharmazeut Chem, D-35032 Marburg, Germany

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2004年 / 43卷 / 02期

关键词：

drug design; enzyme inhibitors; farnesyltransferase; malaria; medicinal chemistry;

D O I：

10.1002/anie.200351169

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

The inhibition of farnesyltransferase was recently suggested as a new strategy for malaria therapy. A class of farnesyltransferase inhibitors such as 1 has been prepared which have in vivo activity in a murine malaria model. These inhibitors significantly reduce the farnesylation of parasite proteins.

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收藏

页码：251 / 254

页数：4

相关论文

共 31 条

[1] Inhibitors of protein prenylation 2000 [J].

Bell, IM .

EXPERT OPINION ON THERAPEUTIC PATENTS, 2000, 10 (12) :1813-1831

[2] Cloning, heterologous expression, and distinct substrate specificity of protein farnesyltransferase from Trypanosoma brucei [J].

Buckner, FS ;

Yokoyama, K ;

Nguyen, L ;

Grewal, A ;

Erdjument-Bromage, H ;

Tempst, P ;

Strickland, CL ;

Xiao, L ;

Van Voorhis, WC ;

Gelb, MH .

JOURNAL OF BIOLOGICAL CHEMISTRY, 2000, 275 (29) :21870-21876

[3] Cloning, heterologous expression, and substrate specificities of protein farnesyltransferases from Trypanosoma cruzi and Leishmania major [J].

Buckner, FS ;

Eastman, RT ;

Nepomuceno-Silva, JL ;

Speelmon, EC ;

Myler, PJ ;

Van Voorhis, WC ;

Yokoyama, K .

MOLECULAR AND BIOCHEMICAL PARASITOLOGY, 2002, 122 (02) :181-188

[4]

CAPRINO LA, 1988, ORGANIC SYNTHESIS CO, V6, P403

[5]

Case D.A., 2002, AMBER 7

[6] Protein prenyl transferase activities of Plasmodium falciparum [J].

Chakrabarti, D ;

Azam, T ;

DelVecchio, C ;

Qiu, LB ;

Park, Y ;

Allen, CM .

MOLECULAR AND BIOCHEMICAL PARASITOLOGY, 1998, 94 (02) :175-184

[7] Protein farnesyltransferase and protein prenylation in Plasmodium falciparum [J].

Chakrabarti, D ;

Da Silva, T ;

Barger, J ;

Paquette, S ;

Patel, H ;

Patterson, S ;

Allen, CM .

JOURNAL OF BIOLOGICAL CHEMISTRY, 2002, 277 (44) :42066-42073

[8] Farnesyltransferase inhibitors: promises and realities [J].

Cox, AD ;

Der, CJ .

CURRENT OPINION IN PHARMACOLOGY, 2002, 2 (04) :388-393

[9]

Fu HW, 1999, RECENT PROG HORM RES, V54, P315

[10] ITERATIVE PARTIAL EQUALIZATION OF ORBITAL ELECTRONEGATIVITY - A RAPID ACCESS TO ATOMIC CHARGES [J].

GASTEIGER, J ;

MARSILI, M .

TETRAHEDRON, 1980, 36 (22) :3219-3228

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