Table 5 Histone Demethylases (HKDM) inhibitors in P. falciparum targeting lysine demethylation
From: Epigenetic regulation as a therapeutic target in the malaria parasite Plasmodium falciparum
Inhibitors | Structure | P. falciparum IC50 in µM | Specificity | Development stage | CC50 on mammalian cells in µM (Cell type) |
|---|---|---|---|---|---|
Tranylcypromine |
| > 10 [160] | Inhibits human LSD1 [161] | FDA-approved monoamine oxidase inhibitor | > 200 (HEK293) [162] |
GSK-J1 |
| > 10 [130] | Inhibits human Jumonji demethylases | – | 9 (Human primary macrophages) [163] |
IOX 1 |
| 1; 10 [160] | Inhibits human Jumonji demethylases [164] | – | 86.5 (HeLa) [164] |
JIB-04 |
| – | > 10 (Human mesenchymal stem) [166] |
