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基于肽的血小板衍生生长因子受体β靶向。

Peptide-based targeting of the platelet-derived growth factor receptor beta.

机构信息

Department of Radiation Oncology, University of Heidelberg and German Cancer Research Center, Heidelberg, Germany.

出版信息

Mol Imaging Biol. 2013 Apr;15(2):212-21. doi: 10.1007/s11307-012-0578-7.

DOI:10.1007/s11307-012-0578-7
PMID:22791264
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3591530/
Abstract

PURPOSE

The aim of this work is to identify new ligands targeting the platelet-derived growth factor receptor beta (PDGFRβ).

PROCEDURES

Biopanning was carried out with a 12-amino-acid phage display library against the recombinant extracellular domain of PDGFRβ. The identified peptide PDGFR-P1 was chemically synthesized and labeled with (125)I or (131)I. In vitro studies were performed on the PDGFRβ-expressing cell lines BxPC3 and MCF7 and on PDGFRβ-transfected HEK cells in comparison to negative control wtHEK293 and CaIX-transfected HEK cells. Biodistribution experiments were performed in Balb/c nude mice, carrying subcutaneously BxPC3 tumors.

RESULTS

In vitro studies demonstrated a higher binding to BxPC3, MCF7, and PDGFRβ-tr-HEK cells in comparison to negative control cell lines. Binding was inhibited up to 90% by the unlabeled PDGFR-P1 peptide. Organ distribution studies revealed a higher accumulation in BxPC3 tumors than in most organs.

CONCLUSIONS

PDGFR-P1 is a promising candidate for targeting human PDGFRβ.

摘要

目的

本研究旨在寻找针对血小板衍生生长因子受体 β（PDGFRβ）的新配体。

方法

用针对 PDGFRβ 重组细胞外结构域的 12 肽噬菌体展示文库进行生物淘选。鉴定出的肽 PDGFR-P1 经化学合成后用 (125)I 或 (131)I 标记。在表达 PDGFRβ 的细胞系 BxPC3 和 MCF7 以及转染 PDGFRβ 的 HEK 细胞上进行体外研究，并与阴性对照 wtHEK293 和转染 CaIX 的 HEK 细胞进行比较。在携带皮下 BxPC3 肿瘤的 Balb/c 裸鼠中进行生物分布实验。

结果

体外研究表明，与阴性对照细胞系相比，PDGFR-P1 与 BxPC3、MCF7 和 PDGFRβ-tr-HEK 细胞的结合更高。未标记的 PDGFR-P1 肽可抑制结合达 90%。器官分布研究表明，PDGFR-P1 在 BxPC3 肿瘤中的积累高于大多数器官。

结论

PDGFR-P1 是一种有前途的靶向人 PDGFRβ 的候选药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dca2/3591530/da532142f6b2/11307_2012_578_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dca2/3591530/93b52528197a/11307_2012_578_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dca2/3591530/4bcfd507da0b/11307_2012_578_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dca2/3591530/fe8e534818b5/11307_2012_578_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dca2/3591530/7211ff68b126/11307_2012_578_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dca2/3591530/b8d7c002966a/11307_2012_578_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dca2/3591530/da532142f6b2/11307_2012_578_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dca2/3591530/93b52528197a/11307_2012_578_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dca2/3591530/4bcfd507da0b/11307_2012_578_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dca2/3591530/fe8e534818b5/11307_2012_578_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dca2/3591530/7211ff68b126/11307_2012_578_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dca2/3591530/b8d7c002966a/11307_2012_578_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dca2/3591530/da532142f6b2/11307_2012_578_Fig6_HTML.jpg

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