| + |
PKA | up-regulates activity 
phosphorylation
|
PDE11A |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-276153 |
Ser117 |
GNLQRRAsQKELRKS |
in vitro |
|
| pmid |
sentence |
| 18312413 |
The N-terminus has two phosphorylation sites for cyclic nucleotide monophosphate-dependent protein kinases (Ser117, Ser168). Phosphorylation of both by cAMP-dependent protein kinase decreased the EC50 value for cGMP from 72 to 23 μm. Effect of phosphorylations at Ser117 and Ser162. Here, serine phosphorylation by the catalytic subunit of cAK, albeit not known whether at position 117, 162 or both, increased cGMP affinity about threefold. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-276179 |
Ser162 |
RALLRKAsSLPPTTA |
in vitro |
|
| pmid |
sentence |
| 18312413 |
The N-terminus has two phosphorylation sites for cyclic nucleotide monophosphate-dependent protein kinases (Ser117, Ser168). Phosphorylation of both by cAMP-dependent protein kinase decreased the EC50 value for cGMP from 72 to 23 μm. Effect of phosphorylations at Ser117 and Ser162. Here, serine phosphorylation by the catalytic subunit of cAK, albeit not known whether at position 117, 162 or both, increased cGMP affinity about threefold. |
|
| Publications: |
2 |
Organism: |
In Vitro |
| + |
tadalafil | down-regulates activity 
chemical inhibition
|
PDE11A |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-257888 |
|
|
Homo sapiens |
MDA-MB-231 Cell |
| pmid |
sentence |
| 21189023 |
All of the final compounds and intermediates synthesized were screened for in vitro tumor cell growth inhibition activity using the human MDA-MB-231 breast tumor cell line and for inhibition of recombinant human PDE5 at a single concentration of 10 μM. For compounds showing >60% inhibition, the IC50 was determined by testing a range of eight concentrations with quadruple replicates per concentration, tadalafil used as a positive control.| Conversely, tadalafil possessed a selectivity index of just 16.6 for PDE5 versus PDE11 |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
3.0
PDE11A
- 
- 