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Radiolabeled Agents for Molecular Imaging and/or Therapy
Published in George C. Kagadis, Nancy L. Ford, Dimitrios N. Karnabatidis, George K. Loudos, Handbook of Small Animal Imaging, 2018
Dimitrios Psimadas, Eirini A. Fragogeorgi
Bombesin (BN) is a small neuropeptide of 14 amino acids originally isolated from frog skin. One of its mammalian counterparts is the 27-amino acid gastrin-releasing peptide (GRP). Both peptides show similar biological behavior in humans. GRP and bombesin can bind to GRP receptors (GRPR), which are G-protein coupled receptors (GPCRs) and are present on cells of many human cancer types, such as prostate, breast, and pancreatic cancer and small-cell lung carcinoma, making radiolabeled BN analogs attractive candidates for targeting GRPR (Fani and Maecke 2012). The half-life of natural BN is about 2–3 min and, therefore, more resistant analogs have been developed as molecular imaging tracers. The binding site of BN consists of eight amino acid residues, and in the literature peptides that incorporate these eight peptides are usually termed BN. Radiolabeled BN analogs are usually based on the eight amino acid sequence peptide analogs that have modified amino acid residues in order to improve their stability and allow conjugation of chelators for radiolabeling.
Advanced materials and technologies for oral diseases
Published in Science and Technology of Advanced Materials, 2023
Hao Cui, Yan You, Guo-Wang Cheng, Zhou Lan, Ke-Long Zou, Qiu-Ying Mai, Yan-Hua Han, Hao Chen, Yu-Yue Zhao, Guang-Tao Yu
Optical imaging systems have been intensively studied for cancer diagnosis, respectively. Gastrin-releasing peptide receptor (GRPR) is an important target for OSCC imaging and therapy [243]. Li et al. successfully prepared gastrin-releasing peptide receptor-specific nGO nanoprobes for near-infrared fluorescence imaging of OSCC. The probe has the characteristics of large surface area, good water dispersibility, good biocompatibility, easy surface modification, and low manufacturing cost. Furthermore, it has a high binding affinity and specificity to GRPR-positive HSC-3 cells, which enhances the imaging effect [244]. In our previous experiments, we used the quantum dot (QD)-based overlap-free emission nanoprobes in a second NIR window (NIR-II, 1000) for analyzing the dynamic expression of MDSCs in the tumor microenvironment (TME) (Figure 10(b)). The result shows that NIR-II fluorescent nanoprobes with molecular targeting capability can be used as a real-time monitor for changes in the in vivo immune cell population to assess tumor progression [234]. These experimental results demonstrate the considerable potential of optical imaging systems for diagnosing oral cancer.
Engineering of 177Lu-labeled gold encapsulated into dendrimeric nanomaterials for the treatment of lung cancer
Published in Journal of Biomaterials Science, Polymer Edition, 2022
Zheng Wang, Minhua Ye, Dehua Ma, Jianfei Shen, Fang Fang
Bombesin and GRP-similar peptides have been implicated as growth factors in various kinds of carcinoma over the last two decades. Most of the lung cancer tissues overexpress the gastrin-releasing peptide receptors [41–44]. Several bombesin derivatives with solid potential for GRPR have explored in clinical investigations for specific receptors treatment and imaging. Radionuclide imaging of lung cancers has been successfully performed using radio-bombesin analogues in clinical trials [45–47]. Therefore, HEL-299 human lung cells have been utilized as tumour models to assess novel bombesin probes [48]. A membrane-bound protein with a great affinity for binding and delivering folate into cells, folate receptor-α (FR-α) is a folate receptor. Enhanced control of cell metabolism, folate is also involved in DNA synthesis and repair and cellular respiration. Antifolates are often used in cancer treatment because cancer cells, which quickly increase, have higher folate requirements to retain DNA engineering. All lung cancer subtypes and overexpress FRs. FRs are significantly expressed in HEL-299 cells, according to current polymerase chain reaction (PCR) investigations [49–52].
Theranostic approaches in nuclear medicine: current status and future prospects
Published in Expert Review of Medical Devices, 2020
Luca Filippi, Agostino Chiaravalloti, Orazio Schillaci, Roberto Cianni, Oreste Bagni
Beyond the theranostic applications based on the clinical use of radionuclide pairs (diagnostic/therapeutic), theranostics also consist in the detection of specific biomarkers (i.e. receptors, transporters), that can be successfully exploited for targeted therapy. As specifically concerns breast cancer (BC), in the past years many advances have been made for the identification of several molecular targets linked to specific tumor biology and behavior, such as human epidermal growth factor 2 (HER-2), hormone receptors, gastrin releasing peptide receptor (GRPR), folate receptor (FR), etc. [78]. In particular, 16alpha-[(18)F]fluoroestradiol-17beta (18 F-FES) has been applied for the PET detection of estradiol receptor (ER) in patients affected by advanced BC. In a study performed by Dehdashti et al., a cohort of 51 post-menopausal women with advanced estrogen-receptor positive BC was submitted to PET/CT scan with 18 F-FES before treatment with estradiol, among the enrolled subjects, 17 responded and 31 did not respond to hormone therapy [79]. Of note, responders showed higher SUV values in tumors than non-responders, thus suggesting that PET with 18 F-FES may present a predictive value on the response to hormone therapy.