Radioiodination and Biodistribution of PEGy Lated YP13 Polypeptide

Abstract

Abstract: A dodeca-peptide SVSVGMLPSHAP that targets human CL-187 tumor was identified in vivo by phage display technology. In order to evaluate the potency of YP13 as the imaging agent for diagnosis of tumor and to be easily radioiodinated, peptide YSVSVGMLPSHAP(YP13) with tyramine being added to the N-terminal was synthesized and chemically modified by conjugation with a low molecular weight monomethoxy polyethylene glycol(mPEG, M_w=5000). YP13, mPEG-YP13 and YR13(a nonspecific random 13 peptide as a control peptide) were labeled with ¹³¹I via Iodogen method. The labeled complex ¹³¹I-YP13, ¹³¹I-mPEG-YP13 and ¹³¹I-YR13 were isolated and purified by RP-HPLC. The radiochemical purity was estimated to be better than 95%. The RP-HPLC analysis of the supernatant of ¹³¹I-YP13 and ¹³¹I-mPEG-YP13 in serum collected for 60 min after injection shows that ¹³¹I-mPEG-YP13 in vivo was far more stable than ¹³¹I-YP13. The biodistribution of ¹³¹I-YP13, ¹³¹I-mPEG-YP13 and the control peptide ¹³¹I-YR13 in mice bearing human colon cancinoma was investigated. The experimental results indicate that there was higher uptake of ¹³¹I-YP13 and ¹³¹I-mPEG-YP13 in tumor than that of control peptide YR13 at 1 h and 2 h. The ratios of tumor to blood for ¹³¹I-mPEG-YP13 and ¹³¹I-YP13 increased as time prolonging. The longer serum half-life of mPEG-YP13 improved the uptake in tumor. Therefore, it can be expected that the radioiodinated YP13 and PEGylated YP13 may be a potential tumor-imaging agent.

Key words: Peptide, Phage display technology, PEG , ¹³¹I Radioiodination, Biodistribution

CLC Number:

O615.42
Q785

TrendMD:

SUN Li-Yan, CHU Tai-Wei^*, WANG Yi, WANG Xiang-Yun. Radioiodination and Biodistribution of PEG_y Lated YP13 Polypeptide[J]. Chem. J. Chinese Universities, doi: .

References

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