Potent and Metabolically Stable Modified Peptide Agonists of Protease‐activated Receptor 2

Bulletin of the Korean Chemical Society

Jong Il Park¹  SangYong Song² 

[1] Department of Bio Nanomaterials Bio Campus of Korea Polytechnics Chungnam 32943 Republic of Korea;Peptron, Inc. Daejeon Chungnam 32949, Republic of Korea

关键词: Protease‐;    activated receptor‐;    2;    Peptide;    Peptoid;    Peptide–;    peptoid hybrid;   

DOI  :  10.1002/bkcs.11407

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

Protease‐activated receptor 2 (PAR‐2) is an important target for drug discovery in the pharmaceutical and cosmetic industries. Although many peptide agonists have been developed, they are active at micromolar concentrations or are metabolically unstable. In this study, we designed novel peptide agonists by peptoid technology and synthesized them by standard Fmoc SPPS (Solid Phase Peptide Synthesis) procedures. One of them, Furo‐LIGK‐nV‐NH2, showed very good agonist activity at nanomolar concentrations and showed markedly increased stability in rat plasma compared to that of the control agonist.

【 授权许可】

Unknown