Design,synthesis and functional validation of peptide inhibitors based on TRPV1 ion channel agonist RhTx
Objective: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.Conclusion:It is feasible to develop TRPV1 peptide inhibitors by using rational design based on N terminal residues of RhTx.
NETL
NSTL
万方数据
维普
