Dual Labeled Peptides as Tools to Study Receptors:Nanomolar Affinity Derivatives of TIPP(Tyr-Tic-Phe-Phe)Containing an Affinity Label and Biotin as Probes of delta Opioid Receptors

摘要

A general strategy for the design of dual labeled peptides was developed,and derivatives of the delta opioid receptor(DOR)selective antagonist TIPP(Tyr-Tic-Phe-PheOH)containing both an affinity label and biotin were prepared by solid-phase synthesis.Tyr-Tic-Phe-Phe(p-X)-Asp-NH(CH2CH2O)2-CH2CH2NH-biotin(where X=N=C=S or NHCOCH2Br)exhibit nanomolar DOR affinity.The ability to detect receptors labeled with these peptides following solubilization and SDS-PAGE demonstrate the applicability of this design approach for dual labeled peptide derivatives.