Peptidomimetic inhibitors of protein farnesyltransferase show potent antimalarial activity

被引：66

作者：

Ohkanda, J

Lockman, JW

Yokoyama, K

Gelb, MH

Croft, SL

Kendrick, H

Harrell, MI

Feagin, JE

Blaskovich, MA

Sebti, SM

Hamilton, AD

机构：

[1] Yale Univ, Dept Chem, New Haven, CT 06520 USA

[2] Univ Washington, Dept Chem, Seattle, WA 98195 USA

[3] Univ Washington, Dept Biochem, Seattle, WA 98195 USA

[4] Univ London London Sch Hyg & Trop Med, Dept Infect & Trop Dis, London WC1E 7HT, England

[5] Seattle Biomed Res Inst, Seattle, WA 98109 USA

[6] Univ Washington, Sch Publ Hlth & Community Med, Dept Pathobiol, Seattle, WA 98195 USA

[7] Univ S Florida, Dept Biochem & Mol Biol, H Lee Moffit Canc Ctr & Res Inst, Drug Discovery Program, Tampa, FL 33612 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 06期

关键词：

D O I：

10.1016/S0960-894X(01)00055-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Malaria continues to represent a very serious health problem in the tropics. The current methods of clinical treatment are showing deficiencies due to the increased incidence of resistance in the parasite. In the present paper we report the design, synthesis, and evaluation of potential antimalarial agents against a novel target, protein farnesyltransferase. We show that the most potent compounds are active against Plasmodium falciparum in vitro at submicromolar concentrations. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：761 / 764

页数：4

共 50 条

[41] Bisubstrate analog inhibitors of protein farnesyltransferase
Musa, Musa M.
Distefano, Mark D.
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2009, 238
[42] Synthesis, molecular modeling, and structure-activity relationship of benzophenone-based CAAX-peptidomimetic farnesyltransferase inhibitors
Sakowski, J
Böhm, M
Sattler, I
Dahse, HM
Schlitzer, M
JOURNAL OF MEDICINAL CHEMISTRY, 2001, 44 (18) : 2886 - 2899
[43] The discovery of potent and selective peptidomimetic inhibitors of thrombin.
Cody, WL
Berryman, KA
Cai, C
Doherty, AM
Edmunds, JJ
He, JX
Holland, DR
Narasimhan, L
Plummer, JS
Rapundalo, ST
Susser, A
VanHuis, CA
Siddiqui, MA
St-Denis, Y
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1999, 217 : U1178 - U1178
[44] NONFARNESYLATED TETRAPEPTIDE INHIBITORS OF PROTEIN FARNESYLTRANSFERASE
GOLDSTEIN, JL
BROWN, MS
STRADLEY, SJ
REISS, Y
GIERASCH, LM
JOURNAL OF BIOLOGICAL CHEMISTRY, 1991, 266 (24) : 15575 - 15578
[45] 2-(Aminoacylamino)benzophenones: farnesyltransferase inhibition and antimalarial activity
Kettler, K
Wiesner, J
Fucik, K
Sakowski, J
Ortmann, R
Dahse, HM
Jomaa, H
Schlitzer, M
PHARMAZIE, 2005, 60 (09): : 677 - 682
[46] Different amino acid replacements in CAAX-tetrapeptide based peptidomimetic farnesyltransferase inhibitors
Schlitzer, M
Sattler, I
Dahse, HM
ARCHIV DER PHARMAZIE, 1999, 332 (04) : 124 - 132
[47] Peptidomimetic plasmepsin inhibitors with potent anti-malarial activity and selectivity against cathepsin D
Zogota, Rimants
Kinena, Linda
Withers-Martinez, Chrislaine
Blackman, Michael J.
Bobrovs, Raitis
Pantelejevs, Teodors
Kanepe-Lapsa, Iveta
Ozola, Vita
Jaudzems, Kristaps
Suna, Edgars
Jirgensons, Aigars
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2019, 163 : 344 - 352
[48] Discovery of potent and orally active farnesyltransferase (FT) inhibitors.
Tong, YS
Wang, L
Hasvold, L
Leonard, N
Li, TM
Li, Q
Wang, WB
Cohen, J
Gu, WZ
Zhang, HY
Bauch, J
Marsh, K
Rosenberg, SH
Lin, NH
Sham, HL
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2002, 224 : U29 - U29
[49] A mutant form of human protein farnesyltransferase exhibits increased resistance to farnesyltransferase inhibitors
Del Villar, K
Urano, J
Guo, L
Tamanoi, F
JOURNAL OF BIOLOGICAL CHEMISTRY, 1999, 274 (38) : 27010 - 27017
[50] Improved Cell-Potent and Selective Peptidomimetic Inhibitors of Protein N-Terminal Methyltransferase 1
Dong, Guangping
Iyamu, Iredia D.
Vilseck, Jonah Z.
Chen, Dongxing
Huang, Rong
MOLECULES, 2022, 27 (04):

← 1 2 3 4 5 →