TABLE 17.
Inhibitory potencies of purine nucleotides and nucleotide analogs
| Name or abbreviation | Inhibitory potency (reference) |
|---|---|
| Excess free ATP | 1 Mg2+/8-10 ATPa (R. rubrum F1-ATPase) (291); 1 mMb (R. rubrum F1-ATPase) (291); 5% inhibition at 12 mM (P. blakesleeanus F1-ATPase) (98) |
| ADP | 15-17 μMb (bovine heart MF1-ATPase) (272, 362); 8.6-9 μMb (rat liver SMP-ATPase) (263, 272) |
| GTP | 5-10 μMa for 15 min (spinach CF1-ATPase) (159) |
| FTP | 5-10 μMa for 15 min (spinach CF1-ATPase) (159) |
| TNP-ATP | 100 nMa (bovine heart MF1-ATPase) (277); 5.5 nMb (157), 25 nMb (214) (bovine heart MF1-ATPase); 21 nMb (bovine heart SMP-ATPase) (157); noncatalytic sites 0.2 μMc and catalytic sites < 0.001, 0.023, 1.39 μMc (EF1-ATPase) (429) |
| TNP-ADP | 15-20 nMa (bovine heart MF1-ATPase) (277); 8 nMb (214), 10 nMb (157) (bovine heart MF1-ATPase); 1.3 μMb (bovine heart SMP-ATP synthesis) (157); noncatalytic sites 6.5 μMc and catalytic sites 0.008, 1.3, 1.3 μMc (EF1-ATPase) (429) |
| TNP-Ado | 33 μMb (bovine heart MF1-ATPase) (214) |
| Lin-benzo-ADP | 16 μMb (bovine heart MF1-ATPase) (199); 0.2 μMc (EF1-ATPase) (424); <10 nMc and 1-2 μMc (bovine heart MF1-ATPase) (428) |
| AP4A | 18 μMa (bovine heart MF1-ATPase) (417) |
| AP5A | ∼60% inhibition at 520 μM in 10 min (bovine heart MF1-ATPase) (417); no inhibition up to 100 μM (bovine heart MF1-ATPase) (325) |
| AP6A | ∼80% inhibition at 520 μM in 80 min (bovine heart MF1-ATPase) (417) |
| AMP-PNP | 0.5 μMb (37), 0.33 μMb (306), 0.32 μMb (361), 14 nMb (84) (bovine heart MF1-ATPase); 0.16 μMb (bovine heart SMP-ATPase) (306); 0.92 μMb (255), 0.3 μMb (361) (rat liver MF1-ATPase); 1.3 μMb (rat liver SMP-ATPase) (255); 0.6b (EF1-ATPase) (436) |
| GMP-PNP | 12.3 μMb (bovine heart MF1-ATPase) (37); 300 μMb (rat liver MF1-ATPase) (361) |
| IMP-PNP | 105 μMb with bicarbonate (bovine heart MF1-ATPase) (362) |
| AMP(CH2)P | Km, 2.8 μM in the presence of 1 mM inhibitor from 0.85 μM in its absence (pea SMP-ATP synthesis) (254) |
| RhATP | Bi- and tridentate RhATP, 300 μMb (bovine heart MF1-ATPase) (383) |
| CrATP or Cr(NH3)4ATP | Monodentate CrATP, 78 μMb (bovine heart MF1-ATPase) (383); monodentate Cr(NH3)4ATP, 500 μMb (bovine heart MF1-ATPase) (383); bidentate CrATP, 1 mMb (bovine heart MF1-ATPase) (383) and 170 μMb (S. cerevisiae MF1-ATPase) (432); bidentate Cr(NH3)4ATP, 100 μMb (bovine heart MF1-ATPase) (383); tridentate CrATP, 150 μMb (S. cerevisiae MF1-ATPase) (432) |
| Co(NH3)4ATP | Bidentate Co(NH3)4ATP, 400 μMb (bovine heart MF1-ATPase) (384) |
| 3′-O-Acetyl-ATP | 400 nMb (bovine heart MF1-ATPase) (394) |
| 3′-O-Acetyl-ADP | 55.3-85 μMa (bovine heart SMP, oxidative phosphorylation) (355, 356) |
| 3′-O-Caproyl-ADP | 1.7 μMa (bovine heart SMP-oxidative phosphorylation) (355) |
| 3′-O-Enanthyl-ADP | 2.7 μMa (bovine heart SMP-oxidative phosphorylation) (355) |
| 3′-O-Caprylyl-ADP | 1.7 μMa (bovine heart SMP-oxidative phosphorylation) (355) |
| DMAN-ADP/F-ADP | 0.25 μMa (bovine heart SMP-oxidative phosphorylation) (356); 40 nMb (bovine heart SMP-oxidative phosphorylation) (356); 9.8 μMb (bovine heart SMP-uncoupled ATPase) (356); 50 nMc (bovine heart MF1-ATPase) (397) |
| F-ATP | 2.1 μMa (bovine heart SMP-oxidative phosphorylation) (356); 0.3 μMb (bovine heart SMP, oxidative phosphorylation) (356); 12-27 μMb (bovine heart SMP-uncoupled ATPase) (356) |
| 3′-O-(1-Naphthoyl)-ADP/N-ADP | 300-350 nMa (bovine heart SMP-oxidative phosphorylation) (355, 356); 4.6 μMb (bovine MF1-ATPase) (240); 9 μMb (bovine heart SMP-ATPase) (240); 48 nMb (bovine heart SMP-oxidative phosphorylation) (355); 20-50 nMc (bovine MF1-ATPase) (397) |
| 3′-O-(1-Naphthoyl)-ATP | 2.0 μMa (bovine heart SMP-oxidative phosphorylation) (356) |
| 3′-O-(2-Naphthoyl)-ADP | 5.0 μMa (bovine heart SMP-oxidative phosphorylation) (356) |
| BzATP | 0.85 μMb (bovine heart MF1-ATPase) (3); ∼6 μMb (TF1-ATPase) (8); 1.6 μMc (bovine heart MF1-ATPase) (3) |
| BzADP | 0.72 μMb (bovine heart MF1-ATPase) (3) |
| t-butylacetyl-ADP | 1.5 μMa (bovine heart SMP-oxidative phosphorylation) (355) |
| 3′-O-Phenylacetyl-ADP | 3.2-3.6 μMa (bovine heart SMP-oxidative phosphorylation) (355, 356) |
| 3′-O-Phenylbutyryl-ADP | 1.3-4.6 μMa (bovine heart SMP-oxidative phosphorylation) (355, 356); 0.2 μMb (bovine heart SMP-oxidative phosphorylation) (355) |
| 3′-O-Benzoyl-ADP | 6.0 μMa (bovine heart SMP-oxidative phosphorylation) (355, 356) |
| 3′-O-[N-(2-Nitrophenyl)-γ− aminobutyryl]-ADP | 0.55 μMa (bovine heart SMP-oxidative phosphorylation) (356) |
| 3′-O-[N-(4-Nitrophenyl)-γ− aminobutyryl]-ADP | 0.76 μMa (bovine heart SMP-oxidative phosphorylation) (356) |
| 3′-O-(1-Naphthylacetyl)-ADP | 0.8 μMa (bovine heart SMP-oxidative phosphorylation) (356) |
| 3′-O-(2-Naphthylacetyl)-ADP | 0.8 μMa (bovine heart SMP-oxidative phosphorylation) (356) |
| 3′-O-(1-Anthranoyl)-ADP | 0.56 μMa (bovine heart SMP-oxidative phosphorylation) (356) |
| 3′-O-(9-Anthranoyl)-ADP | 5.9 μMa (bovine heart SMP-oxidative phosphorylation) (355, 356, 397); 1.1 μMb (bovine heart SMP-oxidative phosphorylation) (355) |
| FSBI | 0.5 mMc for reversible binding (bovine heart MF1-ATPase) (49) |
| FSBA | 45% (1 h) and 65% (2 h) inhibition at 0.8 mM (bovine heart SMP-ATPase) (51); 0.23 mMc for reversible binding (pig heart MF1-ATPase) (101) |
| FSBεA | 250 μMc (bovine heart MF1-ATPase) (414) |
| AP2-PL | ∼150 μMc (α subunit of EF1-ATPase) (326); 30% inhibition at 50 μM (EF1-ATPase) (288) |
| AP3-PL | 18 μMa (EF1-ATPase) (288); 2.5 μMa with Mg2+ and 10 μMa without Mg2+ (EF1-ATPase) (184) |
| AP4-PL | 18 μMa (EF1-ATPase) (288) |
| oATP | 10 mMb (M. phlei F1-ATPase) (219); 1.05 mol/mol of ATPasea (ox heart MF1-ATPase) (239); 40% inhibition at 1 mol/mol ATPase without ADP and 60 min incubation (ox heart MF1-ATPase) (239) |
| oADP | 80 μMc (bovine heart MF1-ATPase) (217) |
| oAMP | 90% inhibition at 3 mM (bovine heart MF1-ATPase) (95) |
| Cibacron blue | 600 μMa (rat liver MF1-ATPase) (28) |
| BzAF | 50 μMb in the dark (bovine heart MF1-ATPase) (297); 58 μMc (bovine heart MF1-ATPase) (297) |
a
I50.
b
Ki.
c
Kd.