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Literature summary for 4.6.1.1 extracted from

  • Iwatsubo, K.; Minamisawa, S.; Tsunematsu, T.; Nakagome, M.; Toya, Y.; Tomlinson, J.E.; Umemura, S.; Scarborough, R.M.; Levy, D.E.; Ishikawa, Y.
    Direct inhibition of type 5 adenylyl cyclase prevents myocardial apoptosis without functional deterioration (2004), J. Biol. Chem., 279, 40938-40945.
    View publication on PubMed
Search for more literature for 4.6.1.1

Application

Application Comment Organism
medicine induction of cardiac myocyte apoptosis by high beta-adrenergic receptor stimulation is effectively prevented by type 5 adenylyl cyclase inhibitors. Inhibition of adrenergic signaling at the level of the type 5 adenylyl cyclase isoform by P-site inhibitors may serve as an effective method to prevent cardiac myocyte apoptosis induced by excessive adrenergic stimulation without deleterious effect on cardiac myocyte contraction Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
(4-(6-amino-9H-purin-9-yl)cyclopent-2-en-1-yl)acetic acid i.e. PMC-4, type 2 enzyme, 50% inhibition at 6.998 mM, type 3 enzyme, 50% inhibition at 0.117 mM, type 5 enzyme, 50% inhibition at 0.22 mM Mus musculus
2-(4-(6-amino-9H-purin-9-yl)cyclopent-2-en-1-yl)-N-hydroxyacetamide i.e. PMC-3, type 2 enzyme, 50% inhibition at 3.76 mM, type 3 enzyme, 50% inhibition at 0.098 mM, type 5 enzyme, 50% inhibition at 0.076 mM Mus musculus
2-(6-amino-9H-purin-9-yl)-5-(hydroxymethyl)tetrahydrofuran-3,4-diol i.e. Ara-Ade, type 2 enzyme, 50% inhibition at 7.202 mM, type 3 enzyme, 50% inhibition at 0.375 mM, type 5 enzyme, 50% inhibition at 0.0098mM Mus musculus
2-amino-7-(2-furyl)-7,8-dihydroquinazolin-5(6H)-one i.e. RS-2 or NKY80, type 2 enzyme, 50% inhibition at 2.63 mM, type 3 enzyme, 50% inhibition at 0.2264 mM, type 5 enzyme, 50% inhibition at 0.015 mM Mus musculus
2-amino-7-(4-chlorophenyl)-7,8-dihydroquinazolin-5(6H)-one i.e.RS-4, type 3 enzyme, 50% inhibition at 6.61 mM, type 5 enzyme, 50% inhibition at 1.988 mM Mus musculus
2-amino-7-(4-methoxyphenyl)-7,8-dihydroquinazolin-5(6H)-one i.e. RS-1, type 2 enzyme, 50% inhibition at 2.64 mM, type 3 enzyme, 50% inhibition at 1.32 mM, type 5 enzyme, 50% inhibition at 1.95 mM Mus musculus
2-amino-7-phenyl-7,8-dihydroquinazolin-5(6H)-one i.e. RS-3, type 2 enzyme, 50% inhibition at 6.31 mM, type 3 enzyme, 50% inhibition at 0.56 mM, type 5 enzyme, 50% inhibition at 0.21 mM Mus musculus
3'-AMP type 2 enzyme, 50% inhibition at 0.263 mM, type 3 enzyme, 50% inhibition at 0.030 mM, type 5 enzyme, 50% inhibition at 0.015 mM Mus musculus
3-(6-amino-9H-purin-9-yl)-N-hydroxycyclopentanecarboxamide i.e. PMC-6, type 2 enzyme, 50% inhibition at 0.065 mM, type 3 enzyme, 50% inhibition at 0.011 mM, type 5 enzyme, 50% inhibition at 0.00032 mM Mus musculus
4-(6-amino-9H-purin-9-yl)-N-hydroxybutanamide i.e. PMC-2, type 3 enzyme, 50% inhibition at 0.32 mM, type 5 enzyme, 50% inhibition at 0.13 mM Mus musculus
4-(6-amino-9H-purin-9-yl)-N-hydroxycyclopent-2-ene-1-carboxamide i.e. PMC-5, type 2 enzyme, 50% inhibition at 6.02 mM, type 3 enzyme, 50% inhibition at 0.137 mM, type 5 enzyme, 50% inhibition at 0.046 mM Mus musculus
5-(6-amino-9H-purin-9-yl)-N-hydroxypentanamide i.e. PMC-1, type 2 enzyme, 50% inhibition at 1.303 mM, type 3 enzyme, 50% inhibition at 0.154 mM, type 5 enzyme, 50% inhibition at 0.030 mM Mus musculus
5-(6-amino-9H-purin-9-yl)tetrahydrofuran-3-ol i.e. 2'5'-dd-Ado, type 2 enzyme, 50% inhibition at 2.382 mM, type 3 enzyme, 50% inhibition at 0.253 mM, type 5 enzyme, 50% inhibition at 0.0016 mM Mus musculus
9-(tetrahydrofuran-2-yl)-9H-purin-6-amine i.e. SQ22536, type 2 enzyme, 50% inhibition at 0.285 mM, type 3 enzyme, 50% inhibition at 0.101 mM, type 5 enzyme, 50% inhibition at 0.0022 mM Mus musculus

Organism

Organism UniProt Comment Textmining
Mus musculus
-
 isoforms type 2, type 3 and type 5 adenylyl cyclase
-