GRK2-ct

GRK2-ct (also known as βARKct) is a peptide inhibitor derived from the carboxyl-terminal domain of G protein-coupled receptor kinase 2 (GRK2). It acts as a scavenger of Gβγ subunits of heterotrimeric G proteins, thereby preventing the membrane translocation and activation of endogenous GRK2. By sequestering Gβγ, GRK2-ct inhibits GRK2-mediated phosphorylation and desensitization of G protein-coupled receptors (GPCRs), such as β-adrenergic receptors, and blocks Gβγ-dependent downstream signaling pathways (including PI3Kγ, PLCβ, and MAPK). GRK2-ct is widely utilized as a research tool to study GPCR regulation and Gβγ-mediated signaling, and has been investigated in preclinical gene therapy models (such as AAV6-mediated delivery) for the treatment of heart failure, cardiac hypertrophy, and breast cancer metastasis.

Other names

beta-ARKctcarboxyl-terminus of beta-adrenergic receptor kinaseGRK2 carboxyl-terminal peptideGRK-2 carboxyl-terminal peptideGRK 2 carboxyl-terminal peptideGRK2-CTGRK-2-CTGRK 2-CTβARKct