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Literature summary for 4.6.1.1 extracted from

  • Mou, T.C.; Gille, A.; Suryanarayana, S.; Richter, M.; Seifert, R.; Sprang, S.R.
    Broad specificity of mammalian adenylyl cyclase for interaction with 2,3-substituted purine- and pyrimidine nucleotide inhibitors (2006), Mol. Pharmacol., 70, 878-886.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
forskolin catalytic heterodimer VC1-IIC2 Rattus norvegicus
forskolin catalytic heterodimer VC1-IIC2 Canis lupus familiaris
Galphas catalytic heterodimer VC1-IIC2 Rattus norvegicus
Galphas catalytic heterodimer VC1-IIC2 Canis lupus familiaris

Crystallization (Commentary)

Crystallization (Comment) Organism
crystal structures of catalytic domains VC1-IIC2 bound to 2'(3')-O-(N-methylanthraniloyl)-GTP, 2'(3')-O-(N-methylanthraniloyl)-ATP, and 2',3'-(2,4,6-trinitrophenyl)-ATP, at 2.9 to 3.3 A resolution, inhibitors reside in the same binding pocket in the VC1-IIC2 protein complex, but there are substantial differences in interactions of base, fluorophore, and polyphosphate chain of the inhibitors with mAC Rattus norvegicus
crystal structures of catalytic domains VC1-IIC2 bound to 2'(3')-O-(N-methylanthraniloyl)-GTP, 2'(3')-O-(N-methylanthraniloyl)-ATP, and 2',3'-(2,4,6-trinitrophenyl)-ATP, at 2.9 to 3.3 A resolution, inhibitors reside in the same binding pocket in the VC1-IIC2 protein complex, but there are substantial differences in interactions of base, fluorophore, and polyphosphate chain of the inhibitors with mAC Canis lupus familiaris

Inhibitors

Inhibitors Comment Organism Structure
2'(3')-O-(N-methylanthraniloyl)-ATP catalytic heterodimer VC1-IIC2 Canis lupus familiaris
2'(3')-O-(N-methylanthraniloyl)-ATP catalytic heterodimer VC1-IIC2 Rattus norvegicus
2'(3')-O-(N-methylanthraniloyl)-GTP catalytic heterodimer VC1-IIC2 Canis lupus familiaris
2'(3')-O-(N-methylanthraniloyl)-GTP catalytic heterodimer VC1-IIC2, incompletely defined structure 2'- or 3'-substituted nucleoside triphosphate Rattus norvegicus
2',3'-bis[(2-(N-methylanthraniloyl)amino)ethyl-carbamoyl]-ATP
-
Canis lupus familiaris
2',3'-bis[(2-(N-methylanthraniloyl)amino)ethyl-carbamoyl]-ATP catalytic heterodimer VC1-IIC2 Rattus norvegicus
2',3'-di[(2-(N-methylanthraniloyl)amino)ethyl-carbamoyl]-ATP catalytic heterodimer VC1-IIC2 Canis lupus familiaris
2',3'-di[(2-(N-methylanthraniloyl)amino)ethyl-carbamoyl]-ATP
-
Rattus norvegicus
2',3'-O-(2,4,6-trinitrophenyl)-ADP catalytic heterodimer VC1-IIC2 Canis lupus familiaris
2',3'-O-(2,4,6-trinitrophenyl)-ADP catalytic heterodimer VC1-IIC2 Rattus norvegicus
2',3'-O-(2,4,6-trinitrophenyl)-AMP catalytic heterodimer VC1-IIC2 Canis lupus familiaris
2',3'-O-(2,4,6-trinitrophenyl)-AMP catalytic heterodimer VC1-IIC2 Rattus norvegicus
2',3'-O-(2,4,6-trinitrophenyl)-ATP catalytic heterodimer VC1-IIC2 Canis lupus familiaris
2',3'-O-(2,4,6-trinitrophenyl)-ATP catalytic heterodimer VC1-IIC2 Rattus norvegicus
2',3'-O-(2,4,6-trinitrophenyl)-CTP catalytic heterodimer VC1-IIC2 Canis lupus familiaris
2',3'-O-(2,4,6-trinitrophenyl)-CTP catalytic heterodimer VC1-IIC2, incompletely defined structure 2'- or 3'-substituted nucleoside triphosphate Rattus norvegicus
2',3'-O-(2,4,6-trinitrophenyl)-GDP catalytic heterodimer VC1-IIC2 Canis lupus familiaris
2',3'-O-(2,4,6-trinitrophenyl)-GDP catalytic heterodimer VC1-IIC2 Rattus norvegicus
2',3'-O-(2,4,6-trinitrophenyl)-GTP catalytic heterodimer VC1-IIC2 Canis lupus familiaris
2',3'-O-(2,4,6-trinitrophenyl)-GTP catalytic heterodimer VC1-IIC2 Rattus norvegicus
2',3'-O-(2,4,6-trinitrophenyl)-UTP catalytic heterodimer VC1-IIC2 Canis lupus familiaris
2',3'-O-(2,4,6-trinitrophenyl)-UTP catalytic heterodimer VC1-IIC2 Rattus norvegicus
8-[(4-(N-methylanthraniloyl)amino)butyl]amino-ATP catalytic heterodimer VC1-IIC2 Canis lupus familiaris
8-[(4-(N-methylanthraniloyl)amino)butyl]amino-ATP catalytic heterodimer VC1-IIC2 Rattus norvegicus
8-[(6-(N-methylanthraniloyl)amino)hexyl]-amino-ATP catalytic heterodimer VC1-IIC2 Canis lupus familiaris
8-[(6-(N-methylanthraniloyl)amino)hexyl]-amino-ATP catalytic heterodimer VC1-IIC2 Rattus norvegicus
N6-[6-((N-methylanthraniloyl)amino)hexyl]-ATP catalytic heterodimer VC1-IIC2 Canis lupus familiaris
N6-[6-((N-methylanthraniloyl)amino)hexyl]-ATP catalytic heterodimer VC1-IIC2 Rattus norvegicus

Metals/Ions

Metals/Ions Comment Organism Structure
Mn2+ catalytic heterodimer VC1-IIC2 Rattus norvegicus
Mn2+ catalytic heterodimer VC1-IIC2 Canis lupus familiaris

Organism

Organism UniProt Comment Textmining
Canis lupus familiaris
-
-
-
Rattus norvegicus
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP catalytic heterodimer VC1-IIC2 Rattus norvegicus 3',5'-cAMP + diphosphate
-
?
ATP catalytic heterodimer VC1-IIC2 Canis lupus familiaris 3',5'-cAMP + diphosphate
-
?

Synonyms

Synonyms Comment Organism
mAC C1 domain of type V mAC (VC1) Canis lupus familiaris
mAC C2 domain of type II mAC (IIC2) Rattus norvegicus
membrane adenylyl cyclase
-
Rattus norvegicus
membrane adenylyl cyclase
-
Canis lupus familiaris

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000011
-
2'(3')-O-(N-methylanthraniloyl)-ATP VC1-IIC2 in the presence of 0.1 mM forskolin and GTPgammaS-activated Galphas Rattus norvegicus
0.000011
-
2'(3')-O-(N-methylanthraniloyl)-ATP VC1-IIC2 in the presence of 0.1 mM forskolin and GTPgammaS-activated Galphas Canis lupus familiaris
0.000014
-
2'(3')-O-(N-methylanthraniloyl)-GTP VC1-IIC2 in the presence of 0.1 mM forskolin and GTPgammaS-activated Galphas Rattus norvegicus
0.000014
-
2'(3')-O-(N-methylanthraniloyl)-GTP VC1-IIC2 in the presence of 0.1 mM forskolin and GTPgammaS-activated Galphas Canis lupus familiaris
0.000081
-
2',3'-O-(2,4,6-trinitrophenyl)-ATP VC1-IIC2 in the presence of 0.1 mM forskolin and GTPgammaS-activated Galphas Rattus norvegicus
0.000081
-
2',3'-O-(2,4,6-trinitrophenyl)-ATP VC1-IIC2 in the presence of 0.1 mM forskolin and GTPgammaS-activated Galphas Canis lupus familiaris
0.000083
-
2',3'-O-(2,4,6-trinitrophenyl)-GTP VC1-IIC2 in the presence of 0.1 mM forskolin and GTPgammaS-activated Galphas Rattus norvegicus
0.000083
-
2',3'-O-(2,4,6-trinitrophenyl)-GTP VC1-IIC2 in the presence of 0.1 mM forskolin and GTPgammaS-activated Galphas Canis lupus familiaris
0.000092
-
2',3'-O-(2,4,6-trinitrophenyl)-UTP VC1-IIC2 in the presence of 0.1 mM forskolin Rattus norvegicus
0.000092
-
2',3'-O-(2,4,6-trinitrophenyl)-UTP VC1-IIC2 in the presence of 0.1 mM forskolin Canis lupus familiaris
0.000092
-
2',3'-O-(2,4,6-trinitrophenyl)-UTP VC1-IIC2 in the presence of 0.1 mM forskolin and GTPgammaS-activated Galphas Rattus norvegicus
0.000092
-
2',3'-O-(2,4,6-trinitrophenyl)-UTP VC1-IIC2 in the presence of 0.1 mM forskolin and GTPgammaS-activated Galphas Canis lupus familiaris
0.0001
-
2',3'-O-(2,4,6-trinitrophenyl)-ATP VC1-IIC2 in the presence of 0.1 mM forskolin Rattus norvegicus
0.0001
-
2',3'-O-(2,4,6-trinitrophenyl)-ATP VC1-IIC2 in the presence of 0.1 mM forskolin Canis lupus familiaris
0.00011
-
2'(3')-O-(N-methylanthraniloyl)-ATP VC1-IIC2 in the presence of 0.1 mM forskolin Rattus norvegicus
0.00011
-
2'(3')-O-(N-methylanthraniloyl)-ATP VC1-IIC2 in the presence of 0.1 mM forskolin Canis lupus familiaris
0.00011
-
2',3'-O-(2,4,6-trinitrophenyl)-CTP VC1-IIC2 in the presence of 0.1 mM forskolin Rattus norvegicus
0.00011
-
2',3'-O-(2,4,6-trinitrophenyl)-CTP VC1-IIC2 in the presence of 0.1 mM forskolin Canis lupus familiaris
0.00013
-
2'(3')-O-(N-methylanthraniloyl)-GTP VC1-IIC2 in the presence of 0.1 mM forskolin Rattus norvegicus
0.00013
-
2'(3')-O-(N-methylanthraniloyl)-GTP VC1-IIC2 in the presence of 0.1 mM forskolin Canis lupus familiaris
0.00031
-
2',3'-O-(2,4,6-trinitrophenyl)-CTP VC1-IIC2 in the presence of 0.1 mM forskolin and GTPgammaS-activated Galphas Rattus norvegicus
0.00031
-
2',3'-O-(2,4,6-trinitrophenyl)-CTP VC1-IIC2 in the presence of 0.1 mM forskolin and GTPgammaS-activated Galphas Canis lupus familiaris
0.00043
-
2',3'-O-(2,4,6-trinitrophenyl)-GTP VC1-IIC2 in the presence of 0.1 mM forskolin Rattus norvegicus
0.00043
-
2',3'-O-(2,4,6-trinitrophenyl)-GTP VC1-IIC2 in the presence of 0.1 mM forskolin Canis lupus familiaris
0.0013
-
2',3'-O-(2,4,6-trinitrophenyl)-ADP VC1-IIC2 in the presence of 0.1 mM forskolin and GTPgammaS-activated Galphas Rattus norvegicus
0.0013
-
2',3'-O-(2,4,6-trinitrophenyl)-ADP VC1-IIC2 in the presence of 0.1 mM forskolin and GTPgammaS-activated Galphas Canis lupus familiaris
0.002
-
2',3'-O-(2,4,6-trinitrophenyl)-ADP VC1-IIC2 in the presence of 0.1 mM forskolin Rattus norvegicus
0.002
-
2',3'-O-(2,4,6-trinitrophenyl)-ADP VC1-IIC2 in the presence of 0.1 mM forskolin Canis lupus familiaris
0.0055
-
2',3'-bis[(2-(N-methylanthraniloyl)amino)ethyl-carbamoyl]-ATP VC1-IIC2 in the presence of 0.1 mM forskolin Rattus norvegicus
0.0055
-
2',3'-bis[(2-(N-methylanthraniloyl)amino)ethyl-carbamoyl]-ATP VC1-IIC2 in the presence of 0.1 mM forskolin Canis lupus familiaris
0.0067
-
2',3'-di[(2-(N-methylanthraniloyl)amino)ethyl-carbamoyl]-ATP VC1-IIC2 in the presence of 0.1 mM forskolin and GTPgammaS-activated Galphas Rattus norvegicus
0.0067
-
2',3'-di[(2-(N-methylanthraniloyl)amino)ethyl-carbamoyl]-ATP VC1-IIC2 in the presence of 0.1 mM forskolin and GTPgammaS-activated Galphas Canis lupus familiaris
0.0081
-
2',3'-O-(2,4,6-trinitrophenyl)-GDP VC1-IIC2 in the presence of 0.1 mM forskolin Rattus norvegicus
0.0081
-
2',3'-O-(2,4,6-trinitrophenyl)-GDP VC1-IIC2 in the presence of 0.1 mM forskolin Canis lupus familiaris
0.0094
-
2',3'-O-(2,4,6-trinitrophenyl)-GDP VC1-IIC2 in the presence of 0.1 mM forskolin and GTPgammaS-activated Galphas Rattus norvegicus
0.0094
-
2',3'-O-(2,4,6-trinitrophenyl)-GDP VC1-IIC2 in the presence of 0.1 mM forskolin and GTPgammaS-activated Galphas Canis lupus familiaris
0.0094
-
N6-[6-((N-methylanthraniloyl)amino)hexyl]-ATP VC1-IIC2 in the presence of 0.1 mM forskolin and GTPgammaS-activated Galphas Rattus norvegicus
0.0094
-
N6-[6-((N-methylanthraniloyl)amino)hexyl]-ATP VC1-IIC2 in the presence of 0.1 mM forskolin and GTPgammaS-activated Galphas Canis lupus familiaris
0.0094
-
8-[(4-(N-methylanthraniloyl)amino)butyl]amino-ATP VC1-IIC2 in the presence of 0.1 mM forskolin and GTPgammaS-activated Galphas Rattus norvegicus
0.0094
-
8-[(4-(N-methylanthraniloyl)amino)butyl]amino-ATP VC1-IIC2 in the presence of 0.1 mM forskolin and GTPgammaS-activated Galphas Canis lupus familiaris
0.01
-
8-[(4-(N-methylanthraniloyl)amino)butyl]amino-ATP VC1-IIC2 in the presence of 0.1 mM forskolin Rattus norvegicus
0.01
-
8-[(4-(N-methylanthraniloyl)amino)butyl]amino-ATP VC1-IIC2 in the presence of 0.1 mM forskolin Canis lupus familiaris
0.011
-
N6-[6-((N-methylanthraniloyl)amino)hexyl]-ATP VC1-IIC2 in the presence of 0.1 mM forskolin Rattus norvegicus
0.011
-
N6-[6-((N-methylanthraniloyl)amino)hexyl]-ATP VC1-IIC2 in the presence of 0.1 mM forskolin Canis lupus familiaris
0.017
-
2',3'-O-(2,4,6-trinitrophenyl)-AMP VC1-IIC2 in the presence of 0.1 mM forskolin and GTPgammaS-activated Galphas Rattus norvegicus
0.017
-
2',3'-O-(2,4,6-trinitrophenyl)-AMP VC1-IIC2 in the presence of 0.1 mM forskolin and GTPgammaS-activated Galphas Canis lupus familiaris
0.021
-
2',3'-O-(2,4,6-trinitrophenyl)-AMP VC1-IIC2 in the presence of 0.1 mM forskolin Rattus norvegicus
0.021
-
2',3'-O-(2,4,6-trinitrophenyl)-AMP VC1-IIC2 in the presence of 0.1 mM forskolin Canis lupus familiaris
0.058
-
8-[(6-(N-methylanthraniloyl)amino)hexyl]-amino-ATP VC1-IIC2 in the presence of 0.1 mM forskolin Rattus norvegicus
0.058
-
8-[(6-(N-methylanthraniloyl)amino)hexyl]-amino-ATP VC1-IIC2 in the presence of 0.1 mM forskolin Canis lupus familiaris
0.1
-
8-[(6-(N-methylanthraniloyl)amino)hexyl]-amino-ATP VC1-IIC2 in the presence of 0.1 mM forskolin and GTPgammaS-activated Galphas Rattus norvegicus
0.1
-
8-[(6-(N-methylanthraniloyl)amino)hexyl]-amino-ATP VC1-IIC2 in the presence of 0.1 mM forskolin and GTPgammaS-activated Galphas Canis lupus familiaris