Chemistry:CCG-4986
From HandWiki
Short description: Chemical compound
 | |
| Identifiers | |
|---|---|
| |
| CAS Number | |
| PubChem CID | |
| ChemSpider | |
| UNII | |
| Chemical and physical data | |
| Formula | C13H11ClN2O5S2 |
| Molar mass | 374.81 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
| (verify) | |
CCG-4986 is a drug which is the first non-peptide compound discovered that acts as a selective inhibitor of the regulator of G protein signalling protein subtype RGS4.[1][2] Regulators of G protein signalling are proteins which act to limit and shorten the response produced inside a cell following activation of a G protein-coupled receptor. Since different RGS subtypes are expressed in different tissues and are associated with particular receptors, this makes it possible for selective inhibitors of RGS proteins to be developed, which should be able to enhance the activity of a particular receptor in a defined target tissue, but not elsewhere in the body.[3][4][5][6][7][8][9][10]
References
- ↑ "Identification of small-molecule inhibitors of RGS4 using a high-throughput flow cytometry protein interaction assay". Molecular Pharmacology 71 (1): 169–75. January 2007. doi:10.1124/mol.106.028670. PMID 17012620.
- ↑ "The RGS protein inhibitor CCG-4986 is a covalent modifier of the RGS4 Gα-interaction face". Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics 1774 (9): 1213–20. September 2007. doi:10.1016/j.bbapap.2007.06.002. PMID 17660054.
- ↑ "Effector antagonism by the regulators of G protein signalling (RGS) proteins causes desensitization of mu-opioid receptors in the CNS". Psychopharmacology 180 (1): 1–11. June 2005. doi:10.1007/s00213-005-2248-9. PMID 15830230.
- ↑ "Selective interactions between G protein subunits and RGS4 with the C-terminal domains of the mu- and delta-opioid receptors regulate opioid receptor signaling". Cellular Signalling 18 (6): 771–82. June 2006. doi:10.1016/j.cellsig.2005.07.003. PMID 16120478.
- ↑ "Interleukin-1beta up-regulates RGS4 through the canonical IKK2/IkappaBalpha/NF-kappaB pathway in rabbit colonic smooth muscle". The Biochemical Journal 412 (1): 35–43. May 2008. doi:10.1042/BJ20080042. PMID 18260825.
- ↑ "Mapping the Regulator of G Protein Signaling 4 (RGS4): Presynaptic and Postsynaptic Substrates for Neuroregulation in Prefrontal Cortex". Cerebral Cortex 19 (9): 2145–55. January 2009. doi:10.1093/cercor/bhn235. PMID 19153107.
- ↑ "RGS4 Polymorphisms Associated With Variability of Cognitive Performance in a Family-Based Schizophrenia Sample". Schizophrenia Bulletin 36 (5): 983–90. March 2009. doi:10.1093/schbul/sbp002. PMID 19282471.
- ↑ "Upregulation of RGS4 expression by IL-1β in colonic smooth muscle is enhanced by ERK1/2 and p38 MAPK and inhibited by the PI3K/Akt/GSK3β pathway". American Journal of Physiology. Cell Physiology 296 (6): C1310–20. June 2009. doi:10.1152/ajpcell.00573.2008. PMID 19369446.
- ↑ "Regulator of G protein signaling 4 confers selectivity to specific G proteins to modulate mu- and delta-opioid receptor signaling". Cellular Signalling 21 (7): 1218–28. July 2009. doi:10.1016/j.cellsig.2009.03.013. PMID 19324084.
- ↑ "Regulator of G-protein signaling 4 suppresses LPS-induced MUC5AC overproduction in the airway". American Journal of Respiratory Cell and Molecular Biology 41 (1): 40–9. July 2009. doi:10.1165/rcmb.2008-0280OC. PMID 19059885.
 |  |
