Antimalarial drug discovery: Efficacy models for compound screening

被引：597

作者：

Fidock, DA

Rosenthal, PJ

Croft, SL

Brun, R

Nwaka, S

机构：

[1] Albert Einstein Coll Med, Dept Microbiol & Immunol, Bronx, NY 10461 USA

[2] Univ Calif San Francisco, Dept Med, San Francisco, CA 94143 USA

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

[4] Swiss Trop Inst, Dept Med Parasitol & Infect Biol, CH-4002 Basel, Switzerland

[5] Med Malaria Venture, CH-1215 Geneva 15, Switzerland

来源：

NATURE REVIEWS DRUG DISCOVERY | 2004年 / 3卷 / 06期

关键词：

D O I：

10.1038/nrd1416

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

Increased efforts in antimalarial drug discovery are urgently needed. The goal must be to develop safe and affordable new drugs to counter the spread of malaria parasites that are resistant to existing agents. Drug efficacy, pharmacology and toxicity are important parameters in the selection of compounds for development, yet little attempt has been made to review and standardize antimalarial drug-efficacy screens. Here, we suggest different in vitro and in vivo screens for antimalarial drug discovery and recommend a streamlined process for evaluating new compounds on the path from drug discovery to development.

引用

收藏

页码：509 / 520

页数：12

相关论文

共 108 条

[81] Critical role of amino acid 23 in mediating activity and specificity of vinckepain-2, a papain-family cysteine protease of rodent malaria parasites [J].

Singh, A ;

Shenai, BR ;

Choe, Y ;

Gut, J ;

Sijwali, PS ;

Craik, CS ;

Rosenthal, PJ .

BIOCHEMICAL JOURNAL, 2002, 368 :273-281

[82] Amodiaquine, sulfadoxine/pyrimethamine, and combination therapy for treatment of uncomplicated falciparum malaria in Kampala, Uganda: a randomised trial [J].

Staedke, SG ;

Kamya, MR ;

Dorsey, G ;

Gasasira, A ;

Ndeezi, G ;

Charlebois, ED ;

Rosenthal, PJ .

LANCET, 2001, 358 (9279) :368-374

[83] Novel short chain chloroquine analogues retain activity against chloroquine resistant K1 Plasmodium falciparum [J].

Stocks, PA ;

Raynes, KJ ;

Bray, PG ;

Park, BK ;

O'Neill, PM ;

Ward, SA .

JOURNAL OF MEDICINAL CHEMISTRY, 2002, 45 (23) :4975-4983

[84] Triclosan offers protection against blood stages of malaria by inhibiting enoyl-ACP reductase of Plasmodium falciparum [J].

Surolia, N ;

Surolia, A .

NATURE MEDICINE, 2001, 7 (02) :167-173

[85] Developmental arrest of the human malaria parasite Plasmodium falciparum within the mosquito midgut via CTRP gene disruption [J].

Templeton, TJ ;

Kaslow, DC ;

Fidock, DA .

MOLECULAR MICROBIOLOGY, 2000, 36 (01) :1-9

[86] PLASMODIUM-FALCIPARUM - INVITRO STUDIES OF THE PHARMACODYNAMIC PROPERTIES OF DRUGS USED FOR THE TREATMENT OF SEVERE MALARIA [J].

TERKUILE, F ;

WHITE, NJ ;

HOLLOWAY, P ;

PASVOL, G ;

KRISHNA, S .

EXPERIMENTAL PARASITOLOGY, 1993, 76 (01) :85-95

[87] The public health impact of chloroquine resistance in Africa [J].

Trape, JF .

AMERICAN JOURNAL OF TROPICAL MEDICINE AND HYGIENE, 2001, 64 (1-2) :12-17

[88] Chloroquine resistance in the malarial parasite, Plasmodium falciparum [J].

Ursos, LMB ;

Roepe, PD .

MEDICINAL RESEARCH REVIEWS, 2002, 22 (05) :465-491

[89]

Vaidya AB, 2001, INFEC DIS S, P203

[90] Artemether-lumefantrine for the treatment of multidrug-resistant falciparum malaria [J].

van Vugt, M ;

Looareesuwan, S ;

Wilairatana, P ;

McGready, R ;

Villegas, L ;

Gathmann, I ;

Mull, R ;

Brockman, A ;

White, NJ ;

Nosten, F .

TRANSACTIONS OF THE ROYAL SOCIETY OF TROPICAL MEDICINE AND HYGIENE, 2000, 94 (05) :545-548

← 2 3 4 5 6 7 8 9 10 11 →