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Updated: Jun 30, 2025
Method for Identifying Small Molecule Inhibitors of the Protein-protein Interaction Between HCN1 and TRIP8b
Published on: November 11, 2016
Design, synthesis and functional validation of peptide inhibitors based on TRPV1 ion channel agonist RhTx
Heng Zhang1, Jiawei Wang2, Fan Yang3
1Department of Biophysics, School of Basic Medical Sciences, Zhejiang University School of Medicine, Hangzhou 310058, China. 11918126@zju.edu.cn.
Objectives:
To design and synthesize peptide inhibitors targeting transient receptor potential vanilloid 1 (TRPV1) ion channel, and to validate their function.
Methods:
Based on previous studies on the relation of molecular structure and function of red head toxin (RhTx), a series of peptides were rationally designed and synthesized, with positive charged amino acids linked to the N terminus of RhTx. These Nplus-RhTx peptides were functionally validated by patch-clamp recordings in live cells.
Results:
Among the 8 synthesized Nplus-RhTx peptides, four inhibited TRPV1 ion channel activated by capsaicin with IC50 of (188.3±4.7), (193.6±18.0), (282.8±11.9) and (299.5±6.4) µmol/L, respectively.
Conclusions:
It is feasible to develop TRPV1 peptide inhibitors by using rational design based on N terminal residues of RhTx.
