Epigenetic regulation as a therapeutic target in the malaria parasite Plasmodium falciparum

Malaria Journal

Table 4 Histone methyltransferase (HKMT) inhibitors in P. falciparum targeting lysine methylation

Inhibitors	P. falciparum IC₅₀ in µM	Specificity	Development stage	CC₅₀ on mammalian cells in µM (Cell type)
UNC0638	0.028 [130]	Targets G9a methyltransferases in mammalian cells	–	23 (HL-60) [158]
BIX-01294	0.056; 0.075 [127, 147]	No target properly identified but inhibits H3K4me3	Tested on a humanized mouse model	6.1 (HFF) [127]
TM2-115	0.130; 0.137 [127, 147]	Identical to BIX-01294	Tested on a humanized mouse model	5.7 (HFF) [127]
Chaetocin	0.64; 0.95 [147, 159]; 14 [90]	No target properly identified but inhibits H3K9me2/me3	–	0.13 (HL-60) [158]

ISSN: 1475-2875