Malarial dihydrofolate reductase as a paradigm for drug development against a resistance-compromised target

Proceedings of the National Academy of Sciences of the United States of America

Volumn 109, Issue 42, 2012, Pages 16823-16828

  Yuthavong, Yongyuth ^a   Tarnchompoo, Bongkoch ^a   Vilaivan, Tirayut ^b   Chitnumsub, Penchit ^a   Kamchonwongpaisan, Sumalee ^a   Charman, Susan A ^c   McLennan, Danielle N ^c   White, Karen L ^c   Vivas, Livia ^d   Bongard, Emily ^d   Thongphanchang, Chawanee ^a   Taweechai, Supannee ^a   Vanichtanankul, Jarunee ^a   Rattanajak, Roonglawan ^a   Arwon, Uthai ^a   Fantauzzi, Pascal ^e   Yuvaniyama, Jirundon ^f   Charman, William N ^c   Matthews, David ^e  

^a NATIONAL SCIENCE AND TECHNOLOGY DEVELOPMENT AGENCY   (Thailand)

^b CHULALONGKORN UNIVERSITY   (Thailand)

^c MONASH UNIVERSITY   (Australia)

^d LONDON SCHOOL OF HYGIENE AND TROPICAL MEDICINE   (United Kingdom)

^e Medicines for Malaria Venture   (Switzerland)

^f MAHIDOL UNIVERSITY   (Thailand)

Author keywords

2,4 Diaminopyrimidines; Drug resistance; Drug target; Slow binding inhibitors; Structure informed drug discovery

Indexed keywords

4,6 DIAMINO 1,2 DIHYDRO 2,2 DIMETHYL 1 [3 (2,4,5 TRICHLOROPHENOXY)PROPOXY] 1,3,5 TRIAZINE; ANTIMALARIAL AGENT; CARBOXYLIC ACID; CYCLOGUANIL; DIHYDROFOLATE REDUCTASE; DIHYDROFOLATE REDUCTASE INHIBITOR; DIHYDROFOLIC ACID; HEXAMETHYLENE 1,6 BIS(4 TERT BUTYLPYRIDINIUM); METHOTREXATE; P 218; PYRIMETHAMINE; PYRIMIDINE; UNCLASSIFIED DRUG;

AMINO ACID SUBSTITUTION; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG BIOAVAILABILITY; DRUG EFFICACY; ENZYME ACTIVE SITE; ENZYME INHIBITION; ENZYME SUBSTRATE; HYDROGEN BOND; IN VIVO STUDY; MALARIA FALCIPARUM; MALE; MOUSE; NONHUMAN; PLASMODIUM FALCIPARUM; PRIORITY JOURNAL; RAT; SCID MOUSE;

ANIMALS; ANTIMALARIALS; CATALYTIC DOMAIN; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; FOLIC ACID ANTAGONISTS; MICE; MICE, SCID; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PLASMODIUM FALCIPARUM; PROTEIN CONFORMATION; TETRAHYDROFOLATE DEHYDROGENASE;

EID: 84867653932     PISSN: 00278424     EISSN: 10916490     Source Type: Journal    
DOI: 10.1073/pnas.1204556109     Document Type: Article

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