The first selective non-peptide inhibitor of the regulator of G protein signaling protein subtype RGS4. It covalently modifies RGS4 by inhibiting its interaction with Gα (IC50 = 3-5 µM) and suppressing GTPase activity. Intratympanic administration of CCG-4986 was shown to rescue cochlear injury...
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The first selective non-peptide inhibitor of the regulator of G protein signaling protein subtype RGS4. It covalently modifies RGS4 by inhibiting its interaction with Gα (IC50 = 3-5 µM) and suppressing GTPase activity. Intratympanic administration of CCG-4986 was shown to rescue cochlear injury and hearing loss induced by acoustic overexposure and represents a novel paradigm for the treatment of sensorineural hearing loss via pharmacological regulation of GPCR signaling. A novel tool for exploring the involvement of RGS4 in physiological processes
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