Synthesis and preclinical evaluation of a novel, selective 111In-labelled aminoproline-RGD-peptide for non-invasive melanoma tumor imaging

MedChemComm ◽  
2015 ◽  
Vol 6 (12) ◽  
pp. 2175-2183 ◽  
Author(s):  
Andrea Sartori ◽  
Francesca Bianchini ◽  
Silvia Migliari ◽  
Paola Burreddu ◽  
Claudio Curti ◽  
...  
Keyword(s):  
Tumor Imaging ◽  
Rgd Peptide ◽  
Human Melanoma ◽  
Spect Imaging ◽  
Preclinical Models ◽  
Melanoma Tumor ◽  
Preclinical Evaluation ◽  
Non Invasive

An 111In-labelled Amp-based RGD-DOTA conjugate was synthesized and evaluated in preclinical models of human melanoma as a novel integrin-targeted SPECT imaging tracer.

Non-invasive immunoPET imaging of PD-L1 using anti-PD-L1-B11 in breast cancer and melanoma tumor model

2021 ◽  
Author(s):  
Aditya Bansal ◽  
Mukesh K. Pandey ◽  
Whitney Barham ◽  
Xin Liu ◽  
Susan M. Harrington ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Tumor Model ◽  
Melanoma Tumor ◽  
Non Invasive

scholarly journals Expansion and Characterization of Human Melanoma Tumor-Infiltrating Lymphocytes (TILs)

PLoS ONE ◽  
2010 ◽  
Vol 5 (11) ◽  
pp. e13940 ◽  
Author(s):  
Linh T. Nguyen ◽  
Pei Hua Yen ◽  
Jessica Nie ◽  
Nicole Liadis ◽  
Danny Ghazarian ◽  
...  
Keyword(s):  
Tumor Infiltrating Lymphocytes ◽  
Human Melanoma ◽  
Melanoma Tumor ◽  
Infiltrating Lymphocytes

scholarly journals [99mTc]Tc-DB15 in GRPR-Targeted Tumor Imaging with SPECT: From Preclinical Evaluation to the First Clinical Outcomes

Cancers ◽  
2021 ◽  
Vol 13 (20) ◽  
pp. 5093
Author(s):  
Berthold A. Nock ◽  
Aikaterini Kaloudi ◽  
Panagiotis Kanellopoulos ◽  
Barbara Janota ◽  
Barbara Bromińska ◽  
...  
Keyword(s):  
Tumor Imaging ◽  
Pharmacokinetic Profile ◽  
Diglycolic Acid ◽  
Preclinical Evaluation ◽  
Peptide Receptor ◽  
Gastrin Releasing Peptide ◽  
Specific Uptake ◽  
Grpr Antagonist

Diagnostic imaging and radionuclide therapy of prostate (PC) and breast cancer (BC) using radiolabeled gastrin-releasing peptide receptor (GRPR)-antagonists represents a promising approach. We herein propose the GRPR-antagonist based radiotracer [99mTc]Tc-DB15 ([99mTc]Tc-N4-AMA-DGA-DPhe6,Sar11,LeuNHEt13]BBN(6-13); N4: 6-carboxy-1,4,8,11-tetraazaundecane, AMA: aminomethyl-aniline, DGA: diglycolic acid) as a new diagnostic tool for GRPR-positive tumors applying SPECT/CT. The uptake of [99mTc]Tc-DB15 was tested in vitro in mammary (T-47D) and prostate cancer (PC-3) cells and in vivo in T-47D or PC-3 xenograft-bearing mice as well as in BC patients. DB15 showed high GRPR-affinity (IC50 = 0.37 ± 0.03 nM) and [99mTc]Tc-DB15 strongly bound to the cell-membrane of T-47D and PC-3 cells, according to a radiolabeled antagonist profile. In mice, the radiotracer showed high and prolonged GRPR-specific uptake in PC-3 (e.g., 25.56 ± 2.78 %IA/g vs. 0.72 ± 0.12 %IA/g in block; 4 h pi) and T-47D (e.g., 15.82 ± 3.20 %IA/g vs. 3.82 ± 0.30 %IA/g in block; 4 h pi) tumors, while rapidly clearing from background. In patients with advanced BC, the tracer could reveal several bone and soft tissue metastases on SPECT/CT. The attractive pharmacokinetic profile of [99mTc]DB15 in mice and its capability to target GRPR-positive BC lesions in patients highlight its prospects for a broader clinical use, an option currently being explored by ongoing clinical studies.

Radioiodination and preclinical evaluation of 4-benzyl-1-(3-[125I]-iodobenzylsulfonyl)piperidine as a breast tumor imaging tracer in mouse

2017 ◽  
Vol 31 (4) ◽  
pp. 335-346
Author(s):  
Masoud Sadeghzadeh ◽  
Behrouz Alirezapour ◽  
Ghorban Ali Charkhlooie ◽  
Maryam Keshavarz Baghery ◽  
Amir Khorouti
Keyword(s):  
Breast Tumor ◽  
Tumor Imaging ◽  
Preclinical Evaluation

Formulation and preclinical evaluation of 99mTc–gemcitabine as a novel radiopharmaceutical for solid tumor imaging

2014 ◽  
Vol 302 (1) ◽  
pp. 179-186 ◽  
Author(s):  
A. B. Ibrahim ◽  
T. M. Sakr ◽  
O. M. A. Khoweysa ◽  
M. A. Motaleb ◽  
A. Abd El-Bary ◽  
...  
Keyword(s):  
Solid Tumor ◽  
Tumor Imaging ◽  
Preclinical Evaluation

Preclinical evaluation of 2-amino-2-[11C]methyl-butanoic acid as a potential tumor-imaging agent in a mouse model

2015 ◽  
Vol 36 (11) ◽  
pp. 1107-1112
Author(s):  
Chie Suzuki ◽  
Atsushi B. Tsuji ◽  
Koichi Kato ◽  
Hitomi Sudo ◽  
Ming-Rong Zhang ◽  
...  
Keyword(s):  
Mouse Model ◽  
Tumor Imaging ◽  
Imaging Agent ◽  
Butanoic Acid ◽  
Preclinical Evaluation ◽  
Tumor Imaging Agent

scholarly journals Apoptosis-Promoting Effects on A375 Human Melanoma Cells Induced by Exposure to 35.2-GHz Millimeter Wave

2020 ◽  
Vol 19 ◽  
pp. 153303382093413
Author(s):  
Ruiting Zhao ◽  
Yonghong Liu ◽  
Sida Liu ◽  
Tong Luo ◽  
Guang Yuan Zhong ◽  
...  
Keyword(s):  
Millimeter Wave ◽  
Caspase 3 ◽  
Malignant Tumors ◽  
Annexin V ◽  
Human Melanoma ◽  
Wave Exposure ◽  
Cell Counting ◽  
Melanoma Tumor ◽  
A375 Cells

Malignant tumors pose a major problem in the medical field. Millimeter wave (MMW) exposure have potential apoptosis-promoting effects on several types of tumors. Considering that the penetration depth of millimeter wave is usually several millimeters, we study the apoptosis-promoting effects of millimeter wave exposure on A375 human melanoma tumor cells in vitro, and this topic has not been explored in the previous literature. In this study, we use the A375 human melanoma cell line as an experimental model exposed to 35.2 GHz millimeter wave in vitro to determine any positive effect and further explore the underlying mechanisms. In this study, 2 groups namely, exposed and sham groups, were set. The exposed groups included 4 exposure time periods of 15, 30, 60, and 90 minutes. The cells in the sham group did not receive millimeter wave exposure. After millimeter wave exposure, the A375 cells in the exposed and sham groups were collected for further experimental procedures. The cell viability after exposure was determined using a cell counting kit, and the apoptosis of A375 cells was assessed by Annexin V/propidium iodide. Changes in the expression of apoptosis-related proteins, including cleaved-caspase-3, and -8, were examined by Western blot. We observed that the millimeter wave exposure could inhibit the viability and induce apoptosis in A375 cells, and the expression of cleaved caspase-3 and -8 were upregulated ( P < .05). The results indicated that the millimeter wave at 35.2 GHz exerted apoptosis-promoting effects on the A375 cells via a pathway by activating of caspase-8 and -3.

scholarly journals Multiplexed non-invasive tumor imaging of glucose metabolism and receptor-ligand engagement using dark quencher FRET acceptor

Theranostics ◽  
2020 ◽  
Vol 10 (22) ◽  
pp. 10309-10325
Author(s):  
Alena Rudkouskaya ◽  
Nattawut Sinsuebphon ◽  
Marien Ochoa ◽  
Sez-Jade Chen ◽  
Joseph E. Mazurkiewicz ◽  
...  
Keyword(s):  
Glucose Metabolism ◽  
Tumor Imaging ◽  
Receptor Ligand ◽  
Invasive Tumor ◽  
Non Invasive
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