high tumor uptake
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2021 ◽  
Vol 12 (10) ◽  
pp. 1589-1595
Author(s):  
Lixue Chen ◽  
Shengnan Li ◽  
Yanfang Ding ◽  
Changyuan Wang ◽  
Sitong Zhang ◽  
...  


Molecules ◽  
2020 ◽  
Vol 25 (23) ◽  
pp. 5548
Author(s):  
Di Xiao ◽  
Xiaojiang Duan ◽  
Qianqian Gan ◽  
Xuran Zhang ◽  
Junbo Zhang

Prostate-specific membrane antigen (PSMA) is a well-established biological target that is overexpressed on the surface of prostate cancer lesions. Radionuclide-labeled small-molecule PSMA inhibitors have been shown to be promising PSMA-specific agents for the diagnosis and therapy of prostate cancer. In this study, a glutamate-urea-based PSMA-targeted ligand containing an isonitrile (CNGU) was synthesized and labeled with 99mTc to prepare [99mTc]Tc-CNGU with a high radiochemical purity (RCP). The CNGU ligand showed a high affinity toward PSMA (Ki value is 8.79 nM) in LNCaP cells. The [99mTc]Tc-CNGU exhibited a good stability in vitro and hydrophilicity (log P = −1.97 ± 0.03). In biodistribution studies, BALB/c nude mice bearing LNCaP xenografts showed that the complex had a high tumor uptake with 4.86 ± 1.19% ID/g, which decreased to 1.74 ± 0.90% ID/g after a pre-injection of the selective PSMA inhibitor ZJ-43, suggesting that it was a PSMA-specific agent. Micro-SPECT imaging demonstrated that the [99mTc]Tc-CNGU had a tumor uptake and that the uptake was reduced in the image after blocking with ZJ-43, further confirming its PSMA specificity. All of the results in this work indicated that [99mTc]Tc-CNGU is a promising PSMA-specific tracer for the imaging of prostate cancer.



2020 ◽  
pp. jnumed.120.250738 ◽  
Author(s):  
Hsiou-Ting Kuo ◽  
Kuo-Shyan Lin ◽  
Zhengxing Zhang ◽  
Carlos F Uribe ◽  
Helen Merkens ◽  
...  


2019 ◽  
Vol 58 (42) ◽  
pp. 14991-14994 ◽  
Author(s):  
Nicholas A. Zia ◽  
Carleen Cullinane ◽  
Jessica K. Van Zuylekom ◽  
Kelly Waldeck ◽  
Lachlan E. McInnes ◽  
...  


2019 ◽  
Vol 131 (42) ◽  
pp. 15133-15136
Author(s):  
Nicholas A. Zia ◽  
Carleen Cullinane ◽  
Jessica K. Van Zuylekom ◽  
Kelly Waldeck ◽  
Lachlan E. McInnes ◽  
...  


Pharmaceutics ◽  
2019 ◽  
Vol 11 (7) ◽  
pp. 348 ◽  
Author(s):  
Kevin J. H. Allen ◽  
Rubin Jiao ◽  
Mackenzie E. Malo ◽  
Connor Frank ◽  
Darrell R. Fisher ◽  
...  

Melanoma is a cancer with increasing incidence and there is a need for alternatives to immunotherapy within effective approaches to treatment of metastatic melanoma. We performed comparative radioimmunotherapy (RIT) of experimental B16-F10 melanoma with novel humanized IgG to melanin h8C3 labeled with a beta emitter, 177Lu, and an alpha-emitter, 213Bi, as well as biodistribution, microSPECT/CT imaging, and mouse and human dosimetry calculations. microSPECT/CT imaging showed that a humanized antibody that targets “free” melanin in the tumor microenvironment had high tumor uptake in B16F10 murine melanoma in C57Bl/6 mice, with little to no uptake in naturally melanized tissues. Extrapolation of the mouse dosimetry data to an adult human demonstrated that doses delivered to major organs and the whole body by 177Lu-h8C3 would be approximately two times higher than those delivered by 213Bi-h8C3, while the doses to the tumor would be almost similar. RIT results indicated that 213Bi-h8C3 was more effective in slowing down the tumor growth than 177Lu-h8C3, while both radiolabeled antibodies did not produce significant hematologic or systemic side effects. We concluded that h8C3 antibody labeled with 213Bi is a promising reagent for translation into a clinical trial in patients with metastatic melanoma.



Molecules ◽  
2019 ◽  
Vol 24 (8) ◽  
pp. 1612 ◽  
Author(s):  
Alejandro Amor-Coarasa ◽  
James M. Kelly ◽  
Pradeep K. Singh ◽  
Shashikanth Ponnala ◽  
Anastasia Nikolopoulou ◽  
...  

Determining chemokine receptor CXCR4 expression is significant in multiple diseases due to its role in promoting inflammation, cell migration and tumorigenesis. [68Ga]Pentixafor is a promising ligand for imaging CXCR4 expression in multiple tumor types, but its utility is limited by the physical properties of 68Ga. We screened a library of >200 fluorine-containing structural derivatives of AMD-3465 to identify promising candidates for in vivo imaging of CXCR4 expression by positron emission tomography (PET). Compounds containing fluoroethyltriazoles consistently achieved higher docking scores. Six of these higher scoring compounds were radiolabeled by click chemistry and evaluated in PC3-CXCR4 cells and BALB/c mice bearing bilateral PC3-WT and PC3-CXCR4 xenograft tumors. The apparent CXCR4 affinity of the ligands was relatively low, but tumor uptake was CXCR4-specific. The tumor uptake of [18F]RPS-534 (7.2 ± 0.3 %ID/g) and [18F]RPS-547 (3.1 ± 0.5 %ID/g) at 1 h p.i. was highest, leading to high tumor-to-blood, tumor-to-muscle, and tumor-to-lung ratios. Total cell-associated activity better predicted in vivo tumor uptake than did the docking score or apparent CXCR4 affinity. By this metric, and on the basis of their high yielding radiosynthesis, high tumor uptake, and good contrast to background, [18F]RPS-547, and especially [18F]RPS-534, are promising 18F-labeled candidates for imaging CXCR4 expression.



2019 ◽  
Vol 10 (29) ◽  
pp. 7023-7028 ◽  
Author(s):  
Feng Ding ◽  
Zhao Chen ◽  
Won Young Kim ◽  
Amit Sharma ◽  
Chonglu Li ◽  
...  

A novel NIR-II theranostic nanoprobe, PSY (∼110 nm), was concisely developed, which demonstrated excellent photostability, high tumor uptake, superior S/N ratios and more efficient cancer treatment with minimal side effects than cisplatin.



ACS Nano ◽  
2017 ◽  
Vol 11 (9) ◽  
pp. 8838-8848 ◽  
Author(s):  
Fuwu Zhang ◽  
Guizhi Zhu ◽  
Orit Jacobson ◽  
Yi Liu ◽  
Kai Chen ◽  
...  


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