CCG-4986

Last updated
CCG-4986
Structure of CCG-4986.png
Identifiers
  • methyl-N-[(4-chlorophenyl)sulfonyl]-4-nitrobenzenesulfinimidoate
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
ECHA InfoCard 100.161.330 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C13H11ClN2O5S2
Molar mass 374.81 g·mol−1
3D model (JSmol)
  • O=[N](=O)c1ccc(cc1)\S(\OC)=N\S(=O)(=O)c(cc2)ccc2Cl
  • InChI=1S/C13H11ClN2O5S2/c1-21-22(12-6-4-11(5-7-12)16(17)18)15-23(19,20)13-8-2-10(14)3-9-13/h2-9H,1H3
  • Key:GIFNUYPIOIDEGE-UHFFFAOYSA-N
   (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

  1. ↑ Roman DL, Talbot JN, Roof RA, Sunahara RK, Traynor JR, Neubig RR (January 2007). "Identification of small-molecule inhibitors of RGS4 using a high-throughput flow cytometry protein interaction assay". Molecular Pharmacology. 71 (1): 169–75. doi:10.1124/mol.106.028670. PMID   17012620. S2CID   22699604.
  2. ↑ Kimple AJ, Willard FS, Giguère PM, Johnston CA, Mocanu V, Siderovski DP (September 2007). "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. doi:10.1016/j.bbapap.2007.06.002. PMC   2084260 . PMID   17660054.
  3. ↑ Garzón J, Rodríguez-Muñoz M, de la Torre-Madrid E, Sánchez-Blázquez P (June 2005). "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. doi:10.1007/s00213-005-2248-9. hdl: 10261/154655 . PMID   15830230. S2CID   21952312.
  4. ↑ Georgoussi Z, Leontiadis L, Mazarakou G, Merkouris M, Hyde K, Hamm H (June 2006). "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. doi:10.1016/j.cellsig.2005.07.003. PMID   16120478.
  5. ↑ Hu W, Li F, Mahavadi S, Murthy KS (May 2008). "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. doi:10.1042/BJ20080042. PMC   3707494 . PMID   18260825.
  6. ↑ Paspalas CD, Selemon LD, Arnsten AF (January 2009). "Mapping the Regulator of G Protein Signaling 4 (RGS4): Presynaptic and Postsynaptic Substrates for Neuroregulation in Prefrontal Cortex". Cerebral Cortex. 19 (9): 2145–55. doi:10.1093/cercor/bhn235. PMC   2722426 . PMID   19153107.
  7. ↑ Prasad KM, Almasy L, Gur RC, Gur RE, Pogue-Geile M, Chowdari KV, Talkowski ME, Nimgaonkar VL (March 2009). "RGS4 Polymorphisms Associated With Variability of Cognitive Performance in a Family-Based Schizophrenia Sample". Schizophrenia Bulletin. 36 (5): 983–90. doi:10.1093/schbul/sbp002. PMC   2930339 . PMID   19282471.
  8. ↑ Hu W, Li F, Mahavadi S, Murthy KS (June 2009). "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. doi:10.1152/ajpcell.00573.2008. PMC   2692422 . PMID   19369446.
  9. ↑ Leontiadis LJ, Papakonstantinou MP, Georgoussi Z (July 2009). "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. doi:10.1016/j.cellsig.2009.03.013. PMID   19324084.
  10. ↑ Song KS, Kim HJ, Kim K, Lee JG, Yoon JH (July 2009). "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. doi:10.1165/rcmb.2008-0280OC. PMID   19059885.


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