Small-molecule histone methyltransferase inhibitors display rapid antimalarial activity against all blood stage forms in Plasmodium falciparum

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

Volumn 109, Issue 41, 2012, Pages 16708-16713

  Malmquist, Nicholas A ^a,b   Moss, Thomas A ^c   Mecheri, Salah ^a,b   Scherf, Artur ^a,b   Fuchter, Matthew J ^c  

^a INSTITUT PASTEUR   (France)

^b CNRS   (France)

^c IMPERIAL COLLEGE LONDON   (United Kingdom)

Author keywords

Chemical genetics; Chromatin; Global health

Indexed keywords

CHLOROQUINE; HISTONE; HISTONE LYSINE METHYLTRANSFERASE; HISTONE LYSINE METHYLTRANSFERASE INHIBITOR; N (1 BENZYL 4 PIPERIDINYL) 2 (HEXAHYDRO 4 METHYL 1H 1,4 DIAZEPIN 1 YL) 6,7 DIMETHOXY 4 QUINAZOLINAMINE; TM2 115; TM2 119; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIMALARIAL ACTIVITY; ARTICLE; CONCENTRATION RESPONSE; CONTROLLED STUDY; DEVELOPMENTAL STAGE; DOSE TIME EFFECT RELATION; DRUG EFFICACY; DRUG POTENCY; DRUG SYNTHESIS; ENZYME INHIBITION; EPIGENETICS; HUMAN; HUMAN CELL; IC 50; METHYLATION; MOUSE; NONHUMAN; PARASITE DEVELOPMENT; PARASITEMIA; PLASMODIUM BERGHEI; PLASMODIUM FALCIPARUM; PRIORITY JOURNAL; SINGLE DRUG DOSE; TIME;

AMINO ACID SEQUENCE; ANIMALS; ANTIMALARIALS; AZEPINES; BLOTTING, WESTERN; CELLS, CULTURED; DOSE-RESPONSE RELATIONSHIP, DRUG; ERYTHROCYTES; HISTONE-LYSINE N-METHYLTRANSFERASE; HISTONES; HUMANS; LIFE CYCLE STAGES; LYSINE; MALARIA; METHYLATION; MICE; MICE, INBRED C57BL; MOLECULAR SEQUENCE DATA; PARASITEMIA; PLASMODIUM BERGHEI; PLASMODIUM FALCIPARUM; QUINAZOLINES; SEQUENCE HOMOLOGY, AMINO ACID;

EID: 84867393622     PISSN: 00278424     EISSN: 10916490     Source Type: Journal    
DOI: 10.1073/pnas.1205414109     Document Type: Article

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