Bombesin (BBN), an analog of gastrin-releasing peptide (GRP), specifically binds to GRP receptors, which are overexpressed in human prostate cancer (PC). Here, we synthesized a BBN-modified gadolinium oxide (GdO) nanoprobe containing fluorescein (GdO-5(6)-carboxyfluorescein [FI]-polyethylene glycol [PEG]-BBN) for targeted magnetic resonance (MR)/optical dual-modality imaging of PC. The GdO-FI-PEG-BBN nanoparticles exhibited a relatively uniform particle size with an average diameter of 52.3 nm and spherical morphology as depicted by transmission electron microscopy. The longitudinal relaxivity (r) of GdO-FI-PEG-BBN (r =4.23 mMs) is comparable to that of clinically used Magnevist (Gd-DTPA). Fluorescence microscopy and in vitro cellular MRI demonstrated GRP receptor-specific and enhanced cellular uptake of the GdO-FI-PEG-BBN in PC-3 tumor cells. Moreover, GdO-FI-PEG-BBN showed more remarkable contrast enhancement than the corresponding nontargeted GdO-FI-PEG according to in vivo MRI and fluorescent imaging. Tumor immunohistochemical analysis further demonstrated improved accumulation of the targeted nanoprobe in tumors. BBN-conjugated GdO may be a promising nanoplatform for simultaneous GRP receptor-targeted molecular cancer diagnosis and antitumor drug delivery in future clinical applications.
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http://dx.doi.org/10.2147/IJN.S139246 | DOI Listing |
Biochem Med (Zagreb)
February 2025
Clinical Institute of Laboratory Diagnostics, University Hospital Centre Osijek, Osijek, Croatia.
Introduction: Higher concentrations of the small-cell lung cancer (SCLC) serum marker, pro-gastrin-releasing peptide (proGRP), in lung inflammations has been indicated in literature. The objective of this study was to compare serum proGRP concentration in pneumonia, chronic obstructive pulmonary disease (COPD) and early-stage primary lung cancers.
Materials And Methods: An observational study was performed to assess serum proGRP against other lung cancer markers in pneumonia, COPD and in stage 1/2 carcinomas.
Cell Mol Gastroenterol Hepatol
December 2024
Key Laboratory of Cellular Physiology at Shanxi Medical University, Ministry of Education; Department of Physiology, Shanxi Medical University, Taiyuan, China, 030001. Electronic address:
Background & Aims: Sleep disorders (SDs) are common in chronic liver diseases (CLDs). Some SDs arise from impaired internal clock and are hence circadian rhythm SDs (CRSDs). Bile acids (BAs), whose levels are increased in many CLDs, reciprocally interact with circadian rhythm.
View Article and Find Full Text PDFTheranostics
December 2024
Department of Nuclear Medicine, Inselspital, University of Bern, Bern, Switzerland.
Radiopharmaceutical therapy (RPT) is an emerging prostate cancer treatment that delivers radiation to specific molecules within the tumor microenvironment (TME), causing DNA damage and cell death. Given TME heterogeneity, it's crucial to explore RPT dosimetry and biological impacts at the cellular level. We integrated spatial transcriptomics (ST) with computational modeling to investigate the effects of RPT targeting prostate-specific membrane antigen (PSMA), fibroblast activation protein (FAP), and gastrin-releasing peptide receptor (GRPR) each labelled with beta-emitting lutetium-177 (Lu) and alpha-emitting actinium-225 (Ac).
View Article and Find Full Text PDFFront Pharmacol
November 2024
Department of Bioorganic Chemistry, Leibniz Institute of Plant Biochemistry, Halle (Saale), Germany.
Peptide-drug conjugates (PDCs) have recently gained significant attention for the targeted delivery of anticancer therapeutics, mainly due to their cost-effective and chemically defined production and lower antigenicity compared to ADCs, among other benefits. In this study, we designed and synthesized novel PDCs by conjugating new thiol-functionalized tubulysin analogs (tubugis) to bombesin, a peptide ligand with a relevant role in cancer research. Two tubulysin analogs bearing ready-for-conjugation thiol groups were prepared by an on-resin multicomponent peptide synthesis strategy and subsequently tested for their stand-alone anti-proliferative activity against human cancer cells, which resulted in IC values in the nanomolar range.
View Article and Find Full Text PDFPharmaceutics
October 2024
Immunology and Molecular Oncology Diagnostics Unit, Veneto Institute of Oncology IOV-IRCCS, 35128 Padua, Italy.
Prostate cancer (PC) represents the second most diagnosed form of cancer in men on a global scale. Despite the theranostic efficacy of prostate-specific membrane antigen (PSMA) radioligands, there is a spectrum of PC disease in which PSMA expression is low or absent. The gastrin-releasing peptide receptor (GRPR), also known as the bombesin type 2 receptor, has been identified as a target in both the early and advanced stages of PC.
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