CCG-4986 explained

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]}

Notes and References

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2. Kimple AJ, Willard FS, Giguère PM, Johnston CA, Mocanu V, Siderovski DP . 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 . 17660054 . 2084260 . 10.1016/j.bbapap.2007.06.002 .
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7. Prasad KM, Almasy L, Gur RC, Gur RE, Pogue-Geile M, Chowdari KV, Talkowski ME, Nimgaonkar VL . RGS4 Polymorphisms Associated With Variability of Cognitive Performance in a Family-Based Schizophrenia Sample . Schizophrenia Bulletin . 36. 5. 983–90. March 2009 . 19282471 . 2930339 . 10.1093/schbul/sbp002 .
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10. Song KS, Kim HJ, Kim K, Lee JG, Yoon JH . 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 . 19059885 . 10.1165/rcmb.2008-0280OC .