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The Labeling of Peptides with Positron-Emitting Radionuclides: The Importance of PET in Cancer Diagnosis
Published in Marco Chinol, Giovanni Paganelli, Radionuclide Peptide Cancer Therapy, 2016
Stefano Papi, Nicoletta Urbano, Esteban R. Obenaus, Marco Chinol
Different 64Cu-SS analogs were evaluated in animal models (28–30) and in patients with neuroendocrine tumors (4). Overexpression of the gastrin-releasing peptides receptor (GRPR) in a variety of neoplasms, such as breast, prostate, pancreatic, and small cell lung cancers, prompted the development of 64Cu-labeled GRP analogs for PET imaging of GRPR-positive tumors. Recently, 64Cu has been also used to label BN analogs for the detection of GRPR-positive tumors in a mouse model of human prostate cancer (26,39), VIP analogs in preclinical PET imaging studies of oncogene receptors overexpressed in breast and other cancers (40) and cyclic RGD peptide for PET imaging of αv-integrin expression in breast cancer (8,41).
Pruritus in Atopic Dermatitis: Pathophysiology and Treatment Options
Published in Donald Rudikoff, Steven R. Cohen, Noah Scheinfeld, Atopic Dermatitis and Eczematous Disorders, 2014
Tejesh Surendra Patel, Gil Yosipovitch
The concept of a dedicated neural pathway for itch in the central nervous system (CNS), in addition to the peripheral nervous system, has been an area of recent research interest. There are new data suggesting that neurons expressing gastrin-releasing peptide receptor (GRPR) may transmit only itch but not pain (Sun and Chen 2007). In a mouse model of chronic pruritus and atopic dermatitis-like skin lesions, pretreatment of mice with a GRPR antagonist prevented itch.
Respiratory Tract Cancer
Published in Peter G. Shields, Cancer Risk Assessment, 2005
Women may be particularly sensitive to certain carcinogenic compounds in tobacco smoke (68). Several recent epidemiological studies indicate that women may have a higher risk of lung cancer than men (69,70). These studies are supported by data showing a higher level of hydrophobic DNA adduct in female lung compared to men (71,72). Moreover, a higher frequency of G to T mutations in the p53 gene in lung tumors of females than in males was observed (73,74). In human lung, CYP1A1 mRNA are induced by PAH in tobacco smoke. One study showed that women smokers have significantly higher expression of lung CYP1A1 (72). In the same study, hydrophobic DNA adducts were found to be significantly associated to the level of CYP1A1 expression. Together, these data indicate that women may be more susceptible for lung cancer than males. The mechanism(s) is unknown but hormones may be involved, modulating the expression of enzymes involved in the metabolism of PAH. Estrogen receptors (ER-alpha and ER-beta) have been identified in human lung cells (75). There is also recently presented evidence that the observed sex difference in lung cancer risk may be explained by the expression of gastrin-releasing peptide receptor (GRPR) at a significant lower exposure to tobacco smoke in females than males (76). Studies have shown that bombesin-like peptides such as GRP induce cell proliferation in several cell types, also human bronchial cells and may thereby stimulate promotion in lung carcinogenesis (77).
Therapeutic Perspective of Temozolomide Resistance in Glioblastoma Treatment
Published in Cancer Investigation, 2021
Qin Xia, Liqun Liu, Yang Li, Pei Zhang, Da Han, Lei Dong
Neoplastic cerebral organoid contributes to investigations of aspects of tumor biology and evaluation of drug effects. The heterogeneity of GB complicates the development of effective therapeutic methods, and most in vitro models are limited in maintaining the mutational and cellular diversity. Organoid models preserve the cellular heterogeneity, self-renewal capacity, and histological characteristics of the primary tumor (124,125), and can be used to study tumor biology and responses to specific drugs effectively. The use of TMZ showed preferential cytotoxicity of this drug in c-met-mutated neuronal-like organoids same as in GB patients (126). Gastrin peptide-related receptor (GRPR) is one of the highly expressed genes in c-met-mutated organoids (126), a major target in GB (127). Indeed, the inhibition of GRPR induces senescence in GB cells (127), and the GRPR antagonist exhibits synergistic effects with TMZ in GB (128). Unfortunately, although organoid models exhibit great potential in vitro studies to screen suitable drugs, they are not suitable for providing direct treatment for GB patients.
Screening and characterisation of a novel efficient tumour cell-targeting peptide derived from insulin-like growth factor binding proteins
Published in Journal of Drug Targeting, 2023
Min-Lin He, Jin Lei, Xue-Wei Cao, Jian Zhao, Fu-Jun Wang
Cancer is one of the main reasons for the current increase in mortality [42]. Current diagnostic and therapeutic modalities provide minimal specificity for cancer cells and affect normal healthy cells. Targeted drug delivery systems have shown higher efficiency in the diagnosis and treatment of various cancers because targeted drugs are specifically transported to tumour cells with minimal adverse effects on normal healthy cells [43]. Tumour-homing peptides are widely used in the delivery of antitumor drugs due to their small molecular weight, simple and economical production, high specificity, and flexibility in sequence and conjugates [44]. In general, natural ligands are the main source of tumour-targeting peptide screening, and corresponding receptors overexpressed on the surface of tumour cells can be used as targets for tumour-targeting peptides [45]. For example, bombesin derived from amphibian neuropeptide has the ability to target gastrin-releasing peptide receptor (GRPR) [46] and octreotide (DFCFDWKTCT) derived from somatostatin peptide (SST) can target somatostatin receptor body (SSTR) [47]. In addition, some new tumour-homing peptides, such as RGD peptide [48], LyP-1 peptide (CGNKRTRGC) [49], and M2pep (YEQDPWGVKWWY) [50], etc., can also be obtained by phage display and other techniques. This paper describes our screening and identification of a novel tumour-homing peptide from a ‘third class of proteins’ that modulate ligand-receptor binding, which has the ability to target binding to receptor-expressing cells, carrying cargo molecules into cell. In a sense, we tried a new way to identify and obtain novel tumour-targeting peptides.
Evaluation of 99mTc-HYNIC-(ser)3-LTVPWY peptide for glioblastoma imaging
Published in International Journal of Radiation Biology, 2020
Shima Shahsavari, Zahra Shaghaghi, Seyed Mohammad Abedi, Seyed Jalal Hosseinimehr
Radiolabeled RGD (arginine–glycine–aspartic acid) peptide and its derivatives have been widely used for αvβ3 integrin targets in preclinical glioma targeting. The αvβ3 integrin is expressed by angiogenic epithelium and some tumor cells and is attractive for imaging and therapy (Danhier et al. 2012; Shi et al. 2016). 99mTc-NC100692, a cyclic RGD peptide, showed a tumor uptake of 2.81 ± 0.74%ID/g at 1 h and then decreased by 2 h (1.01 ± 0.09%ID/g) in glioblastoma (U87MG) tumor model, while kidney uptake was 2.27 ± 1.05%ID/g. The brain uptake was lowest between normal tissues (Dearling et al. 2013). Our radiolabeled peptide showed slightly lower tumor uptakes (2.08 ± 0.07%ID/g and 0.93 ± 0.03%ID/g at 1 h and 2 h, respectively) than 99mTc-NC100692, while tumor-muscle ratio was more (6.6) for 99mTc-HYNIC-(Ser)3-LTVPWY than 99mTc-NC100692 (about 3.5) at 1 h after injection. The low activities in normal tissues are probably associated to fast washout and low uptakes of 99mTc-HYNIC-(Ser)3-LTVPWY in normal organs. 99mTc-Galacto-RGD2 (dimer) showed a tumor uptake of 6.86 ± 1.33%ID/g with a tumor-muscle ratio of 9.40 ± 5.11 in glioblastoma (U87MG) tumor model that were higher than 99mTc-HYNIC-(Ser)3-LTVPWY (Ji et al. 2013). It is established that RGD dimerization improves tumor uptake. In a clinical study, 68Ga-labeled bombesin (BBN) peptide derivative was used for gastrin-releasing peptide receptor (GRPR)-targeting for assessment the level of receptor expression in glioma patients. 68Ga-BBN as PET tracer has potential value in both high-grade glioma and low-grade glioma as a biomarker of GRPR expression (Zhang et al. 2016). It is documented that radiolabeled peptide is interesting tracer for glioma targeting and imaging as well as assessment of the level of receptor expression.