99mTc-DTPA-bis-c(RGDfK) a potential alpha(v)beta3 integrin based homobivalent radioligand for imaging neoangiogenesis in malignant glioma and melanoma

RSC Advances ◽  
2015 ◽  
Vol 5 (74) ◽  
pp. 60161-60171 ◽  
Author(s):  
Frédéric Debordeaux ◽  
Jürgen Schulz ◽  
Catherine Savona-Baron ◽  
Puja Panwar Hazari ◽  
Cyril Lervat ◽  
...  

A new99mTc-labeled bivalent DTPA-bis-c(RGDfK) conjugate has been developed and successfully synthesized. Promising results have been obtained for its preclinical evaluation on human glioma and melanoma tumor expressing αvβ3targets.

2004 ◽  
Vol 31 (3) ◽  
pp. 345-355 ◽  
Author(s):  
Abraham Boskovitz ◽  
Gamal H. Akabani ◽  
Charles N. Pegram ◽  
Darrell D. Bigner ◽  
Michael R. Zalutsky

2009 ◽  
Vol 110 (3) ◽  
pp. 572-582 ◽  
Author(s):  
Ian F. Parney ◽  
James S. Waldron ◽  
Andrew T. Parsa

Object To date, glioma immunotherapy has been focused mostly on stimulating antitumor peripheral lymphocyte responses; however, some data suggest that microglia and/or macrophages (not lymphocytes) are the predominant inflammatory cells infiltrating gliomas. To study this hypothesis further, the authors analyzed inflammatory cell infiltrates in fresh human malignant glioma specimens and primary cultures. Methods Single-cell suspensions from fresh operative malignant glioma specimens, obtained by stereotactic localization, were analyzed for CD11b and CD45 by using flow cytometry. A comparison was made with peripheral blood mononuclear cells. In a subset of patients, a more detailed flow cytometry analysis of Class I and II major histocompatibility complex, B7-1, B7-2, CD11c, and CD14 expression was performed. Macrophage-like cells in primary glioma cultures were similarly assessed. Results Operative samples were obtained from 9 newly diagnosed malignant gliomas. The mean percent of CD45+/CD11b− cells (lymphocytes) was 2.48% (range 0.65–5.50%); CD45dim/CD11b+ cells (microglia), 1.65% (range 0.37–3.92%); and CD45bright/CD11b+ (monocytes/macrophages), 6.25% (range 1.56–15.3%). More detailed fluorescence-activated cell sorting suggested that macrophage-like cells expressed Class I and II major histocompatibility complex, B7-2, and CD11c but not CD14 or B7-1. Primary human glioma cultures contained significant numbers of macrophage-like (CD45bright/CD11b+) cells, but these cells were lost with successive passages. These cells maintained the immunomarker profiles of macrophage-like cells from fresh specimens only if they were cultured in serum-free media. Conclusions The CD45+/CD11b+ cells are the predominant inflammatory cell infiltrating human gliomas. Of this type, the CD45bright/CD11b+ cells, a phenotype compatible with circulating macrophages in rodent models, and not microglia, are the most common. Their immunomarker profile is compatible with an immature antigen-presenting cell. They are present in primary glioma cultures but are lost in successive passages. Their role is enigmatic, and they may prove an important target for future glioma immunotherapy studies.


MedChemComm ◽  
2015 ◽  
Vol 6 (12) ◽  
pp. 2175-2183 ◽  
Author(s):  
Andrea Sartori ◽  
Francesca Bianchini ◽  
Silvia Migliari ◽  
Paola Burreddu ◽  
Claudio Curti ◽  
...  

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.


Planta Medica ◽  
2011 ◽  
Vol 77 (12) ◽  
Author(s):  
P Bolfa ◽  
F Sarac ◽  
A Filip ◽  
A Gal ◽  
M Taulescu ◽  
...  

2011 ◽  
Vol 71 (08) ◽  
Author(s):  
KJ Dedes ◽  
P Wilkerson ◽  
D Wetterskog ◽  
MB Lambros ◽  
R Natrajan ◽  
...  

2016 ◽  
Vol 55 (02) ◽  
pp. 51-62 ◽  
Author(s):  
S. Hermann ◽  
M. Schäfers ◽  
C. Höltke ◽  
A. Faust

SummaryOptical imaging has long been considered a method for histological or microscopic investigations. Over the last 15 years, however, this method was applied for preclinical molecular imaging and, just recently, was also able to show its principal potential for clinical applications (e.g. fluorescence-guided surgery). Reviewing the development and preclinical evaluation of new fluorescent dyes and target-specific dye conjugates, these often show characteristic patterns of their routes of excretion and biodistribution, which could also be interesting for the development and optimization of radiopharmaceuticals. Especially ionic charges show a great influence on biodistribution and netcharge and charge-distribution on a conjugate often determines unspecific binding or background signals in liver, kidney or intestine, and other organs.Learning from fluorescent probe behaviour in vivo and translating this knowledge to radio-pharmaceuticals might be useful to further optimize emerging and existing radiopharmaceuticals with respect to their biodistribution and thereby availability for binding to their targets.


2020 ◽  
Author(s):  
M Kirchner ◽  
A Holzgreve ◽  
M Brendel ◽  
V Ruf ◽  
D Pötter ◽  
...  

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