An Update of Radiolabeled Bombesin Analogs for Gastrin-Releasing Peptide Receptor Targeting

Zilin Yu, Hildo J. K. Ananias, Giuseppe Carlucci, Hilde D. Hoving, Wijnand Helfrich, Rudi A. J. O. Dierckx, Fan Wang, Igle J. de Jong, Philip H. Elsinga*

*Corresponding author for this work

Research output: Contribution to journalArticleAcademicpeer-review

41 Citations (Scopus)

Abstract

Prostate cancer is a critical public health problem in USA and Europe. New non-invasive imaging methods are urgently needed, due to the low accuracy and specificity of current screen methods and the desire of localizing primary prostate cancer and bone metastasis. Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) are the non-invasive and sensitive imaging methods which have been widely used for diagnosing diseases in the clinic. Lack of suitable radiotracers is the major issue for nuclear imaging of prostate cancer, although radiolabeled bombesin (BN) peptides targeting the Gastrin-Releasing Peptide Receptor (GRPR) on tumor cells are widely investigated. In this review we discuss the recent trends in the development of GRPR-targeted radiopharmaceuticals based on BN analogs with regard to their potential for imaging and therapy of GRPR-expressing malignancies. Following a brief introduction of GRPR and bombesin peptides, we summarize the properties of prostate cancer specific radiolabeled bombesins. New bombesin tracers published in the last five years are reviewed and compared according to their novelties in biomolecules, radionuclides, labeling methods, bifunctional chelators and linkers. Hot topics such as multimerization, application of agonists and antagonists are highlighted in the review. Lastly, a few clinical trials of cancer nuclear imaging with radiolabeled bombesin have been discussed.

Original languageEnglish
Pages (from-to)3329-3341
Number of pages13
JournalCurrent Pharmaceutical Design
Volume19
Issue number18
Publication statusPublished - Jun-2013

Keywords

  • Bombesin
  • GRPR
  • prostate cancer
  • bone metastasis
  • PET
  • SPECT
  • targeting
  • imaging
  • POSITRON-EMISSION-TOMOGRAPHY
  • IMPROVING TUMOR UPTAKE
  • PROSTATE-CANCER
  • POSITIVE TUMORS
  • BIFUNCTIONAL CHELATORS
  • BIOLOGICAL EVALUATION
  • PEG(4) LINKERS
  • IMAGING AGENT
  • BREAST-CANCER
  • RGD DIMERS

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