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Literature summary for 4.6.1.1 extracted from
- Stable expression of adenylyl cyclase 2 leads to the functional rescue of human 5-HT6 receptor in a CHODUKX cell line (2007), J. Pharmacol. Toxicol. Methods, 55, 323-331.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| 5-CT | h5-HT6/rAC2 cell line highly responsive | Rattus norvegicus |  |
| 5-HT | h5-HT6/rAC2 cell line highly responsive | Rattus norvegicus | |
| lisuride | h5-HT6/rAC2 cell line highly responsive | Rattus norvegicus | |
| phorbol 12-myristate 13-acetate | PKC-selective activator, stimulates AC2 | Rattus norvegicus | |
| serotonin | AC2 stimulation followed by cAMP accumulation, no effect on AC5. AC2 co-transfected with Gs protein shows a synergistic effect on both baseline and agonist-stimulated cAMP accumulation. In the combined presence of Golf and AC2, the level of cAMP accumulation is enhanced in the agonist-stimulated cell line to levels equaling those of the AC2-expressing cell line only, with no effect on baseline activity. Similarly, when AC5 is co-expressed with Gs a synergistic effect with this pairing on both baseline and agonist-stimulated cAMP accumulation versus control can be observed. Because baseline activity is so high with the AC5/Gs pairing, the difference between stimulated and non-stimulated treatments is not significant. The AC5/Golf pairing fails to show any enhancement in cAMP accumulation upon serotonin stimulation, and no effect on baseline activity | Rattus norvegicus | |
| sumatriptan | h5-HT6/rAC2 cell line highly responsive | Rattus norvegicus | |
Application
| Application | Comment | Organism |
|---|---|---|
| drug development | stable AC2-expressing CHODUKX cell line in which the generation of high expressing GPCR receptor/AC2 lines can retain their functional responsiveness and can provide pharmacological drug comparisons between the same host line for screening purposes and measurement of multiple cellular parameters | Rattus norvegicus |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| h5-HT6 pHTop CHODUKX-A2 cells transiently transfected with human Golf, Gs proteins and rat AC2, AC5 full-length isoforms | Rattus norvegicus |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| additional information | selective PKC inhibitor, abolishes cAMP accumulation by AC2 | Rattus norvegicus |
Molecular Weight [Da]
| Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
|---|---|---|---|
| 123000 | - |
AC2, Western immunoblotting | Rattus norvegicus |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Rattus norvegicus | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| brain | - |
Rattus norvegicus | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP | stable co-expression of AC2 with h5-HT6 receptor in CHODUKX cell line displays dose-dependent cAMP accumulation following agonist treatment | Rattus norvegicus | 3',5'-cAMP + diphosphate | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| AC2 | - |
Rattus norvegicus |
| AC5 | - |
Rattus norvegicus |
| adenylyl cyclase 2 | - |
Rattus norvegicus |
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