title: Role of amino acid residues surrounding the phosphorylation site in peptide substrates of G protein-coupled receptor kinase 2 (GRK2).
abstract: A series of amino acid substitutions was made in a previously identified β-tubulin-derived GRK2 substrate peptide (404DEMEFTEAESNMN416) to examine the role of amino acid residues surrounding the phosphorylation site. Anionic amino acid residues surrounding the phosphorylation site played an important role in the affinity for GRK2. Compared to the original peptide, a modified peptide (Ac-EEMEFSEAEANMN-NH2) exhibited markedly higher affinity for GRK2, but very low affinity for GRK5, suggesting that it can be a sensitive and selective peptide for GRK2.
authors.affiliation: Department of Microbiology, St. Marianna University School of Medicine, Sugao 2-16-1 Miyamae, Kawasaki, 216-8511, Japan. asai@marianna-u.ac.jp.
authors.forename: Daisuke
authors.initials: D
authors.lastname: Asai
authors.affiliation: Department of Advanced Medical Initiatives, Faculty of Medical Sciences, Kyushu University, 3-1-1 Maidashi, Higashi-ku, Fukuoka, 812-8582, Japan.
authors.forename: Masaharu
authors.initials: M
authors.lastname: Murata
authors.affiliation: Biomedical Research Institute, National Institute of Advanced Industrial Science and Technology (AIST), 1-8-31 Midorioka, Ikeda, Osaka, 563-8577, Japan.
authors.forename: Riki
authors.initials: R
authors.lastname: Toita
authors.affiliation: Department of Advanced Medical Initiatives, Faculty of Medical Sciences, Kyushu University, 3-1-1 Maidashi, Higashi-ku, Fukuoka, 812-8582, Japan.
authors.forename: Takahito
authors.initials: T
authors.lastname: Kawano
authors.affiliation: Department of Microbiology, St. Marianna University School of Medicine, Sugao 2-16-1 Miyamae, Kawasaki, 216-8511, Japan.
authors.forename: Hideki
authors.initials: H
authors.lastname: Nakashima
authors.affiliation: Division of Biopharmaceutics and Pharmacokinetics, National Cerebral and Cardiovascular Center Research Institute, 5-7-1, Fujishiro-dai, Suita, Osaka, 565-8565, Japan. jrjhkang@ncvc.go.jp.
authors.forename: Jeong-Hun
authors.initials: JH
authors.lastname: Kang
mesh_terms: D000595:Amino Acid Sequence / Q000235:genetics; D019943:Amino Acid Substitution / Q000235:genetics*; D054769:G-Protein-Coupled Receptor Kinase 2 / Q000737:chemistry / Q000235:genetics*; D006801:Humans; D010455:Peptides / Q000737:chemistry*; D010766:Phosphorylation; D013379:Substrate Specificity; D014404:Tubulin / Q000737:chemistry*
chemical_list: D010455:Peptides; D014404:Tubulin; C496567:GRK2 protein, human; D054769:G-Protein-Coupled Receptor Kinase 2
keywords: Amino acid residue; Cellular signal transduction pathway; Consensus sequence; G protein-coupled receptor kinase; Phosphorylation