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Literature summary for 4.6.1.2 extracted from

  • Robinson, J.W.; Potter, L.R.
    ATP potentiates competitive inhibition of guanylyl cyclase A and B by the staurosporine analog, Go6976: Reciprocal regulation of ATP and GTP binding (2011), J. Biol. Chem., 286, 33841-33844.
    View publication on PubMedView publication on EuropePMC

Activating Compound

Activating Compound Comment Organism Structure
additional information neither staurosporine nor Go6976 activate isoforms GC-A or GC-B Homo sapiens
natriuretic peptide
-
Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
Go6976 competitive inhibitor. Go6976 reduces GTP binding to the catalytic site of isoforms GC-A and GC-B. Inhibition of isoform GC-B is minimal in the absence of ATP and 1 mM ATP increases the inhibition 4fold Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HEK-293T cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
GTP
-
Homo sapiens 3',5'-cyclic-GMP + diphosphate
-
?

Synonyms

Synonyms Comment Organism
GC-A isoform Homo sapiens
GC-B isoform Homo sapiens
guanylyl cyclase A
-
Homo sapiens
guanylyl cyclase B
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP ATP activates guanylyl cyclase isoforms GC-A and GC-B. 0.01 mM Go6976 increases the potency of ATP for isoform GC-B 4fold Homo sapiens
heme
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.001
-
Go6976 in the presence of 1 mM ATP, isozyme GC-A, in 25 mM HEPES (pH 7.4), 50 mM NaCl, 0.1% (w/v) bovine serum albumin, 0.5 mM isobutylmethyl xanthine, 1 mM EDTA, 0.5 mM microcystin and 5 mM MgCl2, at 37°C Homo sapiens
0.0013
-
Go6976 in the presence of 1 mM ATP, isozyme GC-B, in 25 mM HEPES (pH 7.4), 50 mM NaCl, 0.1% (w/v) bovine serum albumin, 0.5 mM isobutylmethyl xanthine, 1 mM EDTA, 0.5 mM microcystin and 5 mM MgCl2, at 37°C Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.002
-
in the presence of 1 mM ATP, isozyme GC-B, in 25 mM HEPES (pH 7.4), 50 mM NaCl, 0.1% (w/v) bovine serum albumin, 0.5 mM isobutylmethyl xanthine, 1 mM EDTA, 0.5 mM microcystin and 5 mM MgCl2, at 37°C Homo sapiens Go6976