Novel 64Cu Labeled RGD2-BBN Heterotrimers for PET Imaging of Prostate Cancer
| Autor: | Hongguang Liu, Marcello Leopoldo, Ermelinda Lucente, Yang Liu, Zhen Cheng, Enza Lacivita, Xiang Hu |
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| Rok vydání: | 2018 |
| Předmět: |
0301 basic medicine
Pharmacology chemistry.chemical_classification biology Dimer Organic Chemistry Integrin Biomedical Engineering Pharmaceutical Science Bombesin Bioengineering Peptide Bombesin receptor 03 medical and health sciences chemistry.chemical_compound 030104 developmental biology 0302 clinical medicine chemistry In vivo 030220 oncology & carcinogenesis biology.protein Biophysics Molecular imaging Linker Biotechnology |
| Zdroj: | Bioconjugate Chemistry. 29:1595-1604 |
| ISSN: | 1520-4812 1043-1802 |
| DOI: | 10.1021/acs.bioconjchem.8b00113 |
| Popis: | Bombesin receptor 2 (BB2) and integrin αvβ3 receptor are privileged targets for molecular imaging of cancer because of their overexpression in a number of tumor tissues. The most recent developments in heterodimer-based radiopharmaceuticals concern BB2- and integrin αvβ3-targeting compounds, consisting of bombesin (BBN) and cyclic arginine-glycine-aspartic acid peptides (RGD), connected through short length linkers. Molecular imaging probes based on RGD-BBN heterodimer design exhibit improved tumor targeting efficacy compared to the single-receptor targeting peptide monomers. However, their application in clinical study is restricted because of inefficient synthesis or unfavorable in vivo properties, which could depend on the short linker nature. Thus, the aim of the present study was to develop a RGD2-BBN heterotrimer, composed of (7-14)BBN-NH2 peptide (BBN) linked to the E[c(RGDyK)]2 dimer peptide (RGD2), bearing the new linker type [Pro-Gly]12. The heterodimer E[c(RGDyK)]2-PEG3-Glu-(Pro-Gly)12-BBN(7-14... |
| Databáze: | OpenAIRE |
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