Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 4.6.1.1 extracted from

  • Schlicker, C.; Rauch, A.; Hess, K.C.; Kachholz, B.; Levin, L.R.; Buck, J.; Steegborn, C.
    Structure-based development of novel adenylyl cyclase inhibitors (2008), J. Med. Chem., 51, 4456-4464.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
expression of the N-terminally His-tagged catalytic domain of CyaC Arthrospira platensis
expression of transmembrane isozymes in HEK293T cells, expression of GST-tagged soluble isozyme Homo sapiens
expression of transmembrane isozymes in HEK293T cells, expression of His-tagged soluble isozyme Rattus norvegicus

Crystallization (Commentary)

Crystallization (Comment) Organism
crystal structure analysis Arthrospira platensis

Inhibitors

Inhibitors Comment Organism Structure
1,2,3,4,5,6,7,8,13,13,14,14-dodecachloro-1,4,4a,4b,5,8,8a,12b-octahydro-11-sulfo-1,4:5,8-dimethanotriphenylene-10-carboxylic acid the compound defines an AC inhibitor scaffold with high affinity for human soluble isozyme and less inhibitory effect on mammalian transmembrane isozymes Arthrospira platensis
1-(bromo(1-naphthyl)methyl)naphthalene
-
Arthrospira platensis
17beta-estra-1(10),2,4-triene-2,3,17-triol
-
Arthrospira platensis
2,3,6,23-tetrahydroxyurs-12-en-28-oic acid
-
Arthrospira platensis
2,3-dibromo-1-(4-(hydroxy(oxido)amino)phenyl)-3-(4-quinolinyl)-1-propanone
-
Arthrospira platensis
3,20-dioxopregn-4-en-21-yl 4-bromobenzenesulfonate discriminates between soluble isozyme and transmembrane isozymes, and appears to simultaneously block the original binding pocket and a neighboring interaction site Arthrospira platensis
4,5,6,7-tetrachloro-3,3-bis(6-hydroxy[1,1'-biphenyl]-3-yl)-2-benzofuran-1(3H)-one
-
Arthrospira platensis
5'-benzyl-12'-hydroxy-2'-methyl-3',6',18-trioxoergotaman
-
Arthrospira platensis
additional information structure-based development of adenylyl cyclase inhibitors, compounds exploiting the catechol estrogen binding site can produce potent, isoform discriminating adenylyl cyclase inhibitors, inhibitory potency of compounds, overview Arthrospira platensis
additional information structure-based development of adenylyl cyclase inhibitors, compounds exploiting the catechol estrogen binding site can produce potent, isoform discriminating adenylyl cyclase inhibitors, inhibitory potency of compounds, overview Homo sapiens
additional information structure-based development of adenylyl cyclase inhibitors, compounds exploiting the catechol estrogen binding site can produce potent, isoform discriminating adenylyl cyclase inhibitors, overview Rattus norvegicus

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane transmembrane isozymes Rattus norvegicus 16020
-
membrane transmembrane isozymes Homo sapiens 16020
-
soluble soluble isozyme Rattus norvegicus
-
-
soluble soluble isozyme Homo sapiens
-
-

Metals/Ions

Metals/Ions Comment Organism Structure
bicarbonate activates Rattus norvegicus
bicarbonate activates Homo sapiens
Ca2+ activates Rattus norvegicus
Ca2+ activates Homo sapiens
Mg2+ activates Rattus norvegicus
Mg2+ activates Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP Rattus norvegicus
-
3',5'-cyclic-AMP + diphosphate
-
?
ATP Homo sapiens
-
3',5'-cyclic-AMP + diphosphate
-
?
ATP Arthrospira platensis
-
3',5'-cyclic-AMP + diphosphate
-
?

Organism

Organism UniProt Comment Textmining
Arthrospira platensis O32393 gene cyaC
-
Homo sapiens Q96PN6
-
-
Rattus norvegicus
-
-
-

Purification (Commentary)

Purification (Comment) Organism
soluble isozyme Rattus norvegicus
soluble isozyme Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP
-
Rattus norvegicus 3',5'-cyclic-AMP + diphosphate
-
?
ATP
-
Homo sapiens 3',5'-cyclic-AMP + diphosphate
-
?
ATP
-
Arthrospira platensis 3',5'-cyclic-AMP + diphosphate
-
?

Synonyms

Synonyms Comment Organism
class III adenylate cyclase
-
Arthrospira platensis
cyaC
-
Arthrospira platensis
More the enzyme belongs to the class III adenylyl cyclase superfamily Arthrospira platensis
sAC
-
Rattus norvegicus
sAC
-
Homo sapiens
soluble adenylate cyclase
-
Rattus norvegicus
soluble adenylate cyclase
-
Homo sapiens
tmAC
-
Rattus norvegicus
tmAC
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Rattus norvegicus
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
assay at Rattus norvegicus
7.5
-
assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.001
-
-
Arthrospira platensis 17beta-estra-1(10),2,4-triene-2,3,17-triol
0.005
-
-
Arthrospira platensis 1,2,3,4,5,6,7,8,13,13,14,14-dodecachloro-1,4,4a,4b,5,8,8a,12b-octahydro-11-sulfo-1,4:5,8-dimethanotriphenylene-10-carboxylic acid
0.015
-
-
Arthrospira platensis 3,20-dioxopregn-4-en-21-yl 4-bromobenzenesulfonate
0.07
-
about Arthrospira platensis 5'-benzyl-12'-hydroxy-2'-methyl-3',6',18-trioxoergotaman
0.1
-
about Arthrospira platensis 2,3-dibromo-1-(4-(hydroxy(oxido)amino)phenyl)-3-(4-quinolinyl)-1-propanone
0.1
-
about Arthrospira platensis 4,5,6,7-tetrachloro-3,3-bis(6-hydroxy[1,1'-biphenyl]-3-yl)-2-benzofuran-1(3H)-one
0.1
-
about Arthrospira platensis 2,3,6,23-tetrahydroxyurs-12-en-28-oic acid
0.2
-
about Arthrospira platensis 1-(bromo(1-naphthyl)methyl)naphthalene