Article
Activation of G protein-coupled receptor kinase 1 involves interactions between its N-terminal region and its kinase domain.
Biochemistry - 22 Mar 2011
Huang Chih-Chin, Orban Tivadar, Jastrzebska Beata, Palczewski Krzysztof, Tesmer John J G
Abstract excerpt
G protein-coupled receptor kinases (GRKs) phosphorylate activated G protein-coupled receptors (GPCRs) to initiate receptor desensitization. In addition to the canonical phosphoacceptor site of the kinase domain, activated receptors bind to a distinct docking site that confers higher affinity and activates GRKs allosterically. Recent mutagenesis and structural studies support a model in which receptor docking...
Topics
- Amino Acid Sequence
- Binding Sites
- G-Protein-Coupled Receptor Kinase 1
- Models, Molecular
- Molecular Sequence Data
- Mutagenesis, Site-Directed
- Mutation
- Protein Structure, Tertiary