Disrupted ADP-ribose metabolism with nuclear Poly (ADP-ribose) accumulation leads to different cell death pathways in presence of hydrogen peroxide in procyclic Trypanosoma brucei

Table 1 The most potent inhibitors of TbPARP

Compound	TbPARP	TbPARP	hPARP-1	Reference
Compound	IC₅₀/μM	pIC₅₀ ± SEM	IC₅₀ (K_i)/μM	Reference
3-AB	58	4.24 ± 0.192	22	[50]
Veliparib	0.049	7.31 ± 0.073	0.005 (K_i)	[51]
4-ANI	0.023	7.64 ± 0.198	0.18	[50]
EB-47	0.0065	8.19 ± 0.184	0.045	[52]
1,5-Isoquinolinediol	1.2	5.91 ± 0.072	0.39	[50]
NU1025	0.68	6.17 ± 0.046	0.4	[53]
PJ-34	0.58	6.23 ± 0.109	0.02	[52]
Olaparib	0.0029	8.53 ± 0.104	0.005	[54]
RF03876	1.1	5.94 ± 0.166	-	-
Rucaparib	0.15	6.83 ± 0.032	0.0014 (K_i)	[55]

Potency values are compared with those reported for human PARP-1. Potency values are means of the three dose-response curves fitted separately

ISSN: 1756-3305