Hydroxamate based inhibitors of adenylyl cyclase. Part 1: The effect of acyclic linkers on P-site binding
The synthesis of potent acyclic adenylyl cyclase antagonists is reported.
References (20)
- et al.
J. Mol. Cell. Cardiol.
(1998) J. Biol. Chem.
(1998)- et al.
J. Biol. Chem.
(1995) - et al.
J. Biol. Chem.
(1990) - et al.
Trends Pharmacol. Sci.
(1999) - et al.
J. Neurochem.
(1996) - et al.
Braz. J. Med. Biol. Res.
(2002) - Braunwald, E.; Zipes, D. P.; Libby, P. In Heart Disease, 6th ed.; W. B. Saunders Company; Philadelphia,...
- et al.
J. Circ. Res.
(1997) - Susanni, E. E.; Vatner, D. E.; Homcy, C. J. In The Heart and Cardiovascular System, 2nd Ed., Fozzard, H. A., Ed.; Raven...
Cited by (12)
Sphingosine kinase 1 (SK1) allosteric inhibitors that target the dimerization site
2017, Computational Biology and ChemistryCitation Excerpt :For compound 13, the docking scores for the putative allosteric site and the lipid-binding site were comparable with each other and it displayed comparatively lower binding affinity for the off-target proteins. Moreover, this compound 13 was already known to have inhibitory effects on adenylate cyclase (Levy et al., 2002). Ligands 6, 7, 12, 18, 19, 21 were found to be selective for SK1.
Dopamine-sensitive adenylyl cyclases in neuronal development: Physiopathological and pharmacological implications
2011, Drug Discovery TodayCitation Excerpt :Two other FSK-derivatives, 7-deacetyl-7-hydroxaminoFSK and 5,6-dehydroxy-7-deacetyl-7-nicotinoylFSK (FD3 and FD4, respectively, Fig. 4), are selective activators for AC3 with respect to AC2 and AC5 [82], and could be tested in dopaminergic neuronal migration. Among the P-site inhibitors with metal chelating properties (PMC), the derivative 1R,4R-3-(6-aminopurin-9-yl)-cyclopentane-carboxylic acid hydroxamide (PMC-6, Fig. 4) has been identified as a potent AC5 inhibitor that is selective with respect to AC2 and AC3 [88–90]. Moreover, the 2′(3′)-O-(N-methylanthraniloyl) (MANT) nucleotides, such as MANT-guanosine 5′-[γ-thio]triphosphate (MANT-GTPγS) and MANT-inosine 5′-[γ-thio]triphosphate (MANT-ITPγS, Fig. 4) have also been found to be potent AC inhibitors [91], showing weak AC5 selectivity with respect to AC2, but not with respect to AC1 and AC6 [92].
Adenylyl cyclases as innovative therapeutic goals
2009, Drug Discovery TodayHydroxamate based inhibitors of adenylyl cyclase. Part 2: The effect of cyclic linkers on P-site binding
2002, Bioorganic and Medicinal Chemistry Letters