A high-affinity peptide substrate for G protein-coupled receptor kinase 2 (GRK2).
Amino Acids
; 51(6): 973-976, 2019 Jun.
Article
in En
| MEDLINE
| ID: mdl-31004228
ABSTRACT
We synthesized a previously identified ß-tubulin-derived G protein-coupled receptor kinase 2 (GKR2) peptide (GR-11-1; DEMEFTEAESNMN) and its amino-terminal extension (GR-11-1-N; GEGMDEMEFTEAESNMN) and carboxyl-terminal extension (GR-11-1-C; DEMEFTEAESNMNDLVSEYQ) peptides with the aim of finding a high-affinity peptide substrate for GRK2. GR-11-1-C showed high affinity for GRK2, but very low affinity for GKR5. Its specificity and sensitivity for GKR2 were greater than those of GR-11-1 and GR-11-1-N. These findings should be useful in designing tools for probing GKR2-mediated intracellular signaling pathways, as well as GRK2-specific drugs.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Peptides
/
G-Protein-Coupled Receptor Kinase 2
/
G-Protein-Coupled Receptor Kinase 5
Type of study:
Prognostic_studies
Limits:
Animals
/
Humans
Language:
En
Journal:
Amino Acids
Journal subject:
BIOQUIMICA
Year:
2019
Type:
Article
Affiliation country:
Japan