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Literature summary for 2.7.11.12 extracted from
- (D)-Amino acid analogues of DT-2 as highly selective and superior inhibitors of cGMP-dependent protein kinase Ialpha (2010), Biochim. Biophys. Acta, 1804, 524-532.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| cGMP | - |
Mus musculus |  |
| cGMP | - |
Homo sapiens | |
| cGMP | - |
Rattus norvegicus | |
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | all-D-YGRKKRRQRRRPPLRKKKKKH may help our understanding of how blood vessels constrict and dilate and may also aid the development of new strategies and therapeutic agents targeted to the prevention and treatment of vascular disorders | Mus musculus |
| medicine | all-D-YGRKKRRQRRRPPLRKKKKKH may help our understanding of how blood vessels constrict and dilate and may also aid the development of new strategies and therapeutic agents targeted to the prevention and treatment of vascular disorders | Homo sapiens |
| medicine | all-D-YGRKKRRQRRRPPLRKKKKKH may help our understanding of how blood vessels constrict and dilate and may also aid the development of new strategies and therapeutic agents targeted to the prevention and treatment of vascular disorders | Rattus norvegicus |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| recombinant PKG Ialpha is expressed using SF9 insect cells | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| all-D-YGRKKRRQRRRPPLRKKKKKH | - |
Homo sapiens | |
| all-D-YGRKKRRQRRRPPLRKKKKKH | - |
Mus musculus | |
| all-D-YGRKKRRQRRRPPLRKKKKKH | - |
Rattus norvegicus | |
| retro-inverso-all-D-YGRKKRRQRRRPPLRKKKKKH | - |
Homo sapiens | |
| retro-inverso-all-D-YGRKKRRQRRRPPLRKKKKKH | - |
Mus musculus | |
| retro-inverso-all-D-YGRKKRRQRRRPPLRKKKKKH | - |
Rattus norvegicus | |
| YGRKKRRQRRRPPLRKKKKKH | - |
Homo sapiens | |
| YGRKKRRQRRRPPLRKKKKKH | - |
Mus musculus | |
| YGRKKRRQRRRPPLRKKKKKH | - |
Rattus norvegicus | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + a protein | Mus musculus | - |
ADP + a phosphoprotein | - |
? | |
| ATP + a protein | Homo sapiens | - |
ADP + a phosphoprotein | - |
? | |
| ATP + a protein | Rattus norvegicus | - |
ADP + a phosphoprotein | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
| Mus musculus | - |
male C57BL6 mouse | - |
| Rattus norvegicus | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| artery | - |
Mus musculus | - |
| artery | - |
Rattus norvegicus | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + a protein | - |
Mus musculus | ADP + a phosphoprotein | - |
? | |
| ATP + a protein | - |
Homo sapiens | ADP + a phosphoprotein | - |
? | |
| ATP + a protein | - |
Rattus norvegicus | ADP + a phosphoprotein | - |
? | |
| ATP + TQAKRKKSLAMA | substrate in activity assay | Homo sapiens | ADP + phosphorylated TQAKRKKSLAMA | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| cGMP-dependent protein kinase Ialpha | - |
Mus musculus |
| cGMP-dependent protein kinase Ialpha | - |
Homo sapiens |
| cGMP-dependent protein kinase Ialpha | - |
Rattus norvegicus |
| cGMP-dependent protein kinase type I | - |
Mus musculus |
| cGMP-dependent protein kinase type I | - |
Homo sapiens |
| cGMP-dependent protein kinase type I | - |
Rattus norvegicus |
| PKG I | - |
Mus musculus |
| PKG I | - |
Homo sapiens |
| PKG I | - |
Rattus norvegicus |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0000005 | - |
all-D-YGRKKRRQRRRPPLRKKKKKH | Cheng-Prusoff inhibition constant derived from IC50 value | Homo sapiens | |
| 0.0000008 | - |
all-D-YGRKKRRQRRRPPLRKKKKKH | Dixon plot analysis | Homo sapiens | |
| 0.0000028 | - |
retro-inverso-all-D-YGRKKRRQRRRPPLRKKKKKH | Cheng-Prusoff inhibition constant derived from IC50 value | Homo sapiens | |
| 0.0000055 | - |
retro-inverso-all-D-YGRKKRRQRRRPPLRKKKKKH | Dixon plot analysis | Homo sapiens | |
| 0.0000125 | - |
YGRKKRRQRRRPPLRKKKKKH | Dixon plot analysis | Homo sapiens | |
| 0.0000139 | - |
YGRKKRRQRRRPPLRKKKKKH | Cheng-Prusoff inhibition constant derived from IC50 value | Homo sapiens | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.000012 | - |
- |
Homo sapiens | all-D-YGRKKRRQRRRPPLRKKKKKH | |
| 0.000054 | - |
- |
Homo sapiens | retro-inverso-all-D-YGRKKRRQRRRPPLRKKKKKH | |
| 0.000332 | - |
- |
Homo sapiens | YGRKKRRQRRRPPLRKKKKKH | |
General Information
| General Information | Comment | Organism |
|---|---|---|
| physiological function | cGMP-dependent protein kinase type I is an essential regulator of cellular function in blood vessels throughout the body | Mus musculus |
| physiological function | cGMP-dependent protein kinase type I is an essential regulator of cellular function in blood vessels throughout the body | Homo sapiens |
| physiological function | cGMP-dependent protein kinase type I is an essential regulator of cellular function in blood vessels throughout the body | Rattus norvegicus |
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Release 2023.1 (January 2023)
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