ADRBK1 binds phosphorylated SMO dimer

Stable Identifier
Reaction [binding]
Homo sapiens
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Initial binding and phosphorylation of the SMO C-terminal tail by CSNK1A1 increases the affinity of the tail for ADRBK1/GRK2. Like CSNK1A1, ADRBK1 phosphorylates multiple sites in the SMO tail in a Hh-dependent manner, and this phosphorylation is required for a conformational change that promotes closer association of the two tails in the SMO dimer, analogous to what is seen in Drosophila (Chen et al, 2011; Chen et al, 2010; Zhao et al, 2007; Meloni et al, 2006; Philipp et al, 2008).
Literature References
PubMed ID Title Journal Year
21695114 Sonic Hedgehog dependent phosphorylation by CK1? and GRK2 is required for ciliary accumulation and activation of smoothened

Yue, T, Jia, J, Ma, G, Sasai, N, Briscoe, J, Jiang, J, Chen, Y

PLoS Biol. 2011
20844016 G protein-coupled receptor kinase 2 promotes high-level Hedgehog signaling by regulating the active state of Smo through kinase-dependent and kinase-independent mechanisms in Drosophila

Zhao, Y, Jia, J, Li, S, Tong, C, Liu, Y, Wang, B, Jiang, J, Chen, Y

Genes Dev. 2010
16908539 Smoothened signal transduction is promoted by G protein-coupled receptor kinase 2

Caron, MG, Salahpour, A, Meloni, AR, Wechsler-Reya, RJ, Kelly, P, Fralish, GB, Lefkowitz, RJ, Chen, JK

Mol. Cell. Biol. 2006
18815277 Smoothened signaling in vertebrates is facilitated by a G protein-coupled receptor kinase

Chen, W, Caron, MG, Meloni, AR, Fralish, GB, MacInnes, AW, Barak, LS, Philipp, M

Mol. Biol. Cell 2008
17960137 Hedgehog regulates smoothened activity by inducing a conformational switch

Tong, C, Jiang, J, Zhao, Y

Nature 2007
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