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

Malmquist, Nicholas A; Moss, Thomas A; Mecheri, Salah; Scherf, Artur; Fuchter, Matthew J

Malmquist, Nicholas A; Moss, Thomas A; Mecheri, Salah; Scherf, Artur; Fuchter, Matthew J.

Affiliation

Malmquist NA; Unité de Biologie des Interactions Hôte-Parasite, Institut Pasteur, Paris, France.

Proc Natl Acad Sci U S A ; 109(41): 16708-13, 2012 Oct 09.

Article in En | MEDLINE | ID: mdl-23011794

Subject(s)

Antimalarials/pharmacology; Azepines/pharmacology; Histone-Lysine N-Methyltransferase/antagonists & inhibitors; Plasmodium falciparum/drug effects; Quinazolines/pharmacology; Amino Acid Sequence; Animals; Antimalarials/chemistry; Azepines/chemistry; Blotting, Western; Cells, Cultured; Dose-Response Relationship, Drug; Erythrocytes/parasitology; Histone Methyltransferases; Histone-Lysine N-Methyltransferase/genetics; Histone-Lysine N-Methyltransferase/metabolism; Histones/metabolism; Humans; Life Cycle Stages; Lysine/metabolism; Malaria/drug therapy; Malaria/parasitology; Methylation/drug effects; Mice; Mice, Inbred C57BL; Molecular Sequence Data; Parasitemia/parasitology; Parasitemia/prevention & control; Plasmodium berghei/drug effects; Plasmodium berghei/growth & development; Plasmodium falciparum/growth & development; Quinazolines/chemistry; Sequence Homology, Amino Acid

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Plasmodium falciparum / Quinazolines / Azepines / Histone-Lysine N-Methyltransferase / Antimalarials Limits: Animals / Humans Language: En Journal: Proc Natl Acad Sci U S A Year: 2012 Type: Article Affiliation country: France

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