Table 3 Histone Deacetylase (HDAC) inhibitors in P. falciparum
From: Epigenetic regulation as a therapeutic target in the malaria parasite Plasmodium falciparum
Targeting Class I and II HDACs | |||||
|---|---|---|---|---|---|
Inhibitors | Structure | P. falciparum IC50 in µM | Specificity | Development stage | CC50 on mammalian cells in µM (Cell type) |
Cyclic tetrapeptides | |||||
Apicidin |
| Targets class I and II HDACs [76] | – | 10 (Jurkat) [148] | |
CTP-NPDG 19 |
| 0.3 [122] | Targets class I HDACs | – | > 25 (HepG2) [122] |
Romidepsin |
| 0.09 [149] | Targets class I and II HDACs | FDA-approved in cancer therapy | 0.001 (NFF) [149] |
HC-toxin |
| < 0.01 [49] | Targets class I and II HDACs | – | 0.9 (TFK-1) [150] |
FR235222 |
| 0.01 [151] | Targets class I HDACs | – | 0.13 (HFF) [152] |
Hydroxamates | |||||
Trichostatin A |
| Targets class I and II HDACs | – | 0.2 (HeLa) [153] | |
SAHA (Vorinostat) |
| Targets class I and II HDACs | FDA-approved in cancer therapy | 5.5 (NFF) [149] | |
JAHA |
| 0.5 [147] | Targets class I and II HDACs[154] | – | 2.4 (MCF7) [154] |
SBHA |
| 1 [120] | Targets class I and II HDACs | – | 12 (HEK) [155] |
WR301801 |
| 0.001 [156] | Targets class I and II HDACs | Tested in vivo | 0.6 (RAW) [156] |
Belinostat |
| 0.06 [149] | Targets class I and II HDACs | FDA-approved in cancer therapy | 2.37 (NFF) [149] |
Panobinostat |
| 0.01 [149] | Targets class I and II HDACs | FDA-approved in cancer therapy | 0.07 (NFF) [149] |
FNDR-20123 |
| 0.04 [124] | Targets class I HDACs | – | > 100 (HepG2 & THP-1) [124] |
JX21108 |
| 0.004 [125] | Targets class I HDACs | – | > 4 (HepG2) [125] |
Compound 29 |
| 0.45 [139] | Targets class I HDACs | – | 17 (Hela) [139] |
Peptoid-based hydroxamic acids 2h |
| 0.005 [138] | HDACs | – | 4.6 (HepG2) [138] |
2-aminosuberic acid derivatives | |||||
2-aminosuberic acid derivatives |
| 0.01; 0.3 [120] | Targets class I HDACs | – | 0.2–5.8 (NFF) [120] |
L-cysteine derivatives | |||||
L-cysteine derivatives |
| 0.05; 0.34 [120] | Targets class I HDACs | – | 0.35–2.2 (NFF) [120] |
Targeting Sir2 HDAC (Class III) | |||||
Surfactin |
| 9.3 [79] | Unknown off-targets since it induces apoptosis | – | 9.6 (MCF-7) [157] |
Sirtinol |
| 10 [120] | No off-targets known Inhibits both PfSir2A and B | – | > 25 (NFF) [120] |
