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
^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.
PMID17012620.
S2CID22699604.
^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.
PMID15830230.
S2CID21952312.
^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.
PMID16120478.
^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.
PMID19324084.
^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.
PMID19059885.
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
^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.
PMID17012620.
S2CID22699604.
^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.
PMID15830230.
S2CID21952312.
^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.
PMID16120478.
^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.
PMID19324084.
^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.
PMID19059885.