Proteolytic stability of neuropeptide Y analogues with high binding affinity for Y_1 and Y_2 receptors

摘要

Overexpression of selected peptide receptors in human tumours has been shown to represent clinically relevant targets for cancer diagnosis and therapy.During the past decade this concept has led to the proof of the principle that peptide receptors can be used successfully for in vivo targeting of human cancers.NPY is a 36 amino acid peptide of the pancreatic polypeptide family,which is expressed in the peripheral and central nervous system.It has been shown recently that NPY might play an important role in tumours.The characterisation of the two best-investigated NPY receptor subtypes,Y_1 and Y_2 in human breast tumour and metastasis samples at the mRNA and protein levels,suggests a predominant occurrence of the Y_1 receptor subtype.In this study the proteolytic stability of NPY Y_1 and Y_2 receptor selective analogues has been determined in human blood plasma so that they could be used as feasible diagnostic/therapeutic agents for breast cancer targeting.