Abstract
Over the past two decades, peptide receptor radionuclide therapy (PRRT) has been developed as a valid approach for cancer adjuvant treatment. 177Lu is an excellent radionuclide suitable for radionuclide therapy of tumors and metastases, which highlights the advantages of using PRRT for cancer treatment, subsequently encourages scientists to explore many different types of peptides for tumor radionuclide therapy. Arg-Gly-Asp (RGD) and bombesin (BBN) heterodimers have been investigated for dual targeting of tumor integrin αvβ3 receptors and gastrin-releasing peptide receptors. In this chapter, we present the potential application of 177Lu-labeled RGD-BBN heterodimer for targeting prostate cancer.
This is a preview of subscription content, log in via an institution.
Buying options
Tax calculation will be finalised at checkout
Purchases are for personal use only
Learn about institutional subscriptionsReferences
Lantry LE, Cappelletti E, Maddalena ME et al (2006) 177Lu-AMBA: synthesis and characterization of a selective 177Lu-labeled GRP-R agonist for systemic radiotherapy of prostate cancer. J Nucl Med 47:1144–1152
di Sant’Agnese PA (1998) Neuroendocrine cells of the prostate and neuroendocrine differentiation in prostatic carcinoma: a review of morphologic aspects. Urology 51:121–124
Glover SC, Tretiakova MS, Carroll RE et al (2003) Increased frequency of gastrin-releasing peptide receptor gene mutations during colonadenocarcinoma progression. Mol Carcinog 37:5–15
Vashchenko N, Abrahamsson PA (2005) Neuroendocrine differentiation in prostate cancer: implications for new treatment modalities. Eur Urol 47:147–155
Hynes RO (1992) Integrins: versatility, modulation, and signaling in cell adhesion. Cell 69:11–25
Brooks PC, Clark RA, Cheresh DA (1994) Requirement of vascular integrin avb3 for angiogenesis. Science 264:569–571
Liu S (2009) Radiolabeled cyclic RGD peptides as integrin alpha(v)beta(3)-targeted radiotracers: maximizing binding affinity via bivalency. Bioconjug Chem 20:2199–2213
Li Z, Wu Z, Chen K et al (2008) 18F-labeled BBN-RGD heterodimer for prostate cancer imaging. J Nucl Med 49:453–461
Liu Z, Li ZB, Cao Q et al (2009) Small-animal PET of tumors with 64Cu-labeled RGD-bombesin heterodimer. J Nucl Med 50:1168–1177
Liu Z, Yan Y, Chin FT et al (2009) Dual integrin and gastrin-releasing peptide receptor targeted tumor imaging using 18F-labeled PEGylated RGD-bombesin heterodimer 18F-FB-PEG3-Glu-RGD-BBN. J Med Chem 52:425–432
Liu Z, Niu G, Wang F et al (2009) 68Ga-labeled NOTA-RGD-BBN peptide for dual integrin and GRPR-targeted tumor imaging. Eur J Nucl Med Mol Imaging 36:1483–1494
Liu Z, Yan Y, Liu S et al (2009) 18F, 64Cu, and 68Ga labeled RGD-bombesin heterodimeric peptides for PET imaging of breast cancer. Bioconjug Chem 20:1016–1025
Yan Y, Chen K, Yang M et al (2011) A new 18F-labeled BBN-RGD peptide heterodimer with a symmetric linker for prostate cancer imaging. Amino Acids 41:439–447
Liu Z, Huang J, Dong C et al (2012) 99mTc-labeled RGD-BBN peptide for small-animal SPECT/CT of lung carcinoma. Mol Pharm 9:1409–1417
Weiner RE, Thakur ML (2005) Radiolabeled peptides in oncology: role in diagnosis and treatment. BioDrugs 19:145–163
Cremonesi M, Ferrari M, Di Dia A et al (2011) Recent issues on dosimetry and radiobiology for peptide receptor radionuclide therapy. Q J Nucl Med Mol Imaging 55:155–167
Hoppmann S, Qi S, Miao Z et al (2012) 177Lu-DO3AHSA-ZEGFR:1907: characterization as a potential radiopharmaceutical for radionuclide therapy of EGFR-expressing head and neck carcinomas. J Biol Inorg Chem 17:709–718
Kwekkeboom DJ, Bakker WH, Kooij PP et al (2001) [177Lu-DOTAOTyr3]octreotate: comparison with [111InDTPAo]octreotide in patients. Eur J Nucl Med Mol Imaging 28:1319–1325
Jiang L, Miao Z, Kimura RH et al (2011) Preliminary evaluation of 177Lu-labeled knottin peptides for integrin receptors-targeted radiotherapy. Eur J Nucl Med Mol Imaging 38:613–622
Jiang L, Kimura RH, Miao Z et al (2010) Evaluation of a 64Cu-labeled cystine-knot peptide based on agouti related protein scaffold for tumor avb3 integrin PET imaging. J Nucl Med 51:251–258
Stabin MG, Sparks RB, Crowe E (2005) OLINDA/EXM: the second generation personal computer software for internal dose assessment in nuclear medicine. J Nucl Med 46:1023–1027
Romer A, Seiler D, Marincek N et al (2014) Somatostatin-based radiopeptide therapy with [177Lu-DOTA]-TOC versus [90Y-DOTA]-TOC in neuroendocrine tumors. Eur J Nucl Med Mol Imaging 41:214–222
D’Huyvetter M, Vincke C, Xavier C et al (2014) Targeted radionuclide therapy with a 177Lu-labeled anti-HER2 nanobody. Theranostics 4:708–720
Acknowledgments
This work was supported by DOD-PCRP-NIA PC094646 and sponsored by Shanghai Pujiang Program. The production of 177Lu was supported by Department of Energy Grant 84900-001-10.
Author information
Authors and Affiliations
Corresponding author
Editor information
Editors and Affiliations
Rights and permissions
Copyright information
© 2015 Springer Science+Business Media New York
About this protocol
Cite this protocol
Jiang, L., Cheng, Z. (2015). 177Lu-Labeled RGD-BBN Peptide for Targeting Prostate Cancer. In: Patsenker, E. (eds) Integrin Targeting Systems for Tumor Diagnosis and Therapy. Methods in Pharmacology and Toxicology. Humana Press, New York, NY. https://doi.org/10.1007/7653_2015_50
Download citation
DOI: https://doi.org/10.1007/7653_2015_50
Published:
Publisher Name: Humana Press, New York, NY
Print ISBN: 978-1-4939-7443-6
Online ISBN: 978-1-4939-7445-0
eBook Packages: Springer Protocols