Studies on the structural requirement for ligand binding to the neuropeptide Y (NPY) receptor from rat cerebral cortex

FEBS Letters

Baeza, Claudio Rivera¹  Undén, Anders¹ 

[1] Department of Biochemistry, Stockholm University, S-106 91 Stockholm, Sweden

关键词: Cerebral cortex;    Neuropeptide Y;    Peptide hormone receptor;    Synthetic peptide;    Aca;    ϵ-aminocaproic acid;    APP;    avian pancreatic polypeptide;    t-BOC;    tert-butyloxycarbonyl;    BSA;    bovine serum albumin;    Hepes;    (N-[2-hydroxyethyl] piperazine-N″ -[2-ethane-sulfonic acid];    PP;    pancreatic polypeptide;   

DOI  :  10.1016/0014-5793(90)80800-X

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Analogues of the NPY model peptide NPY 1-4-Aca-25-36 were synthesized by solid phase peptide synthesis using the tea-bag method for parallel peptide synthesis. The affinity of the peptides as ligands to the NPY receptor in rat cerebral cortex was investigated. The model compound NPY 1-4-Aca-25-36 was a relatively poor ligand to the NPY receptor in rat brain (IC₅₀ = 0.40 μM). Arg³⁵ and Arg³³ were both important for ligand recognition by the NPY receptor. Substitutions in several positions in the region corresponding to the C-terminal part of NPY resulted in analogues with only minor reduction of the affinity for the NPY receptor.

【 授权许可】

Unknown