95539-58-5Relevant academic research and scientific papers
Effect of chelators on the pharmacokinetics of 99mTc-labeled imaging agents for the prostate-specific membrane antigen (PSMA)
Ray Banerjee, Sangeeta,Pullambhatla, Mrudula,Foss, Catherine A.,Falk, Alexander,Byun, Youngjoo,Nimmagadda, Sridhar,Mease, Ronnie C.,Pomper, Martin G.
, p. 6108 - 6121 (2013)
Technetium-99m, the most commonly used radionuclide in nuclear medicine, can be attached to biologically important molecules through a variety of chelating agents, the choice of which depends upon the imaging application. The prostate-specific membrane antigen (PSMA) is increasingly recognized as an important target for imaging and therapy of prostate cancer (PCa). Three different 99mTc-labeling methods were employed to investigate the effect of the chelator on the biodistribution and PCa tumor uptake profiles of 12 new urea-based PSMA-targeted radiotracers. This series includes hydrophilic ligands for radiolabeling with the [99mTc(CO)3] + core (L8-L10), traditional NxSy-based chelating agents with varying charge and polarity for the 99mTc-oxo core (L11-L18), and a 99mTc-organohydrazine-labeled radioligand (L19). 99mTc(I)-Tricarbonyl-labeled [99mTc]L8 produced the highest PSMA+ PC3 PIP to PSMA- PC3 flu tumor ratios and demonstrated the lowest retention in normal tissues including kidney after 2 h. These results suggest that choice of chelator is an important pharmacokinetic consideration in the development of 99mTc-labeled radiopharmaceuticals targeting PSMA.
Targeted biocompatible nanoparticles for the delivery of (-)-epigallocatechin 3-gallate to prostate cancer cells
Sanna, Vanna,Pintus, Gianfranco,Roggio, Anna Maria,Punzoni, Stefania,Posadino, Anna Maria,Arca, Alessandro,Marceddu, Salvatore,Bandiera, Pasquale,Uzzau, Sergio,Sechi, Mario
experimental part, p. 1321 - 1332 (2011/04/24)
Molecular targeted cancer therapy mediated by nanoparticles (NPs) is a promising strategy to overcome the lack of specificity of conventional chemotherapeutic agents. In this context, the prostate-specific membrane antigen (PSMA) has demonstrated a powerf
Synthesis and evaluation of technetium-99m- and rhenium-labeled inhibitors of the prostate-specific membrane antigen (PSMA)
Banerjee, Sangeeta R.,Foss, Catherine A.,Castanares, Mark,Mease, Ronnie C.,Byun, Youngjoo,Fox, James J.,Hilton, John,Lupold, Shawn E.,Kozikowski, Alan P.,Pomper, Martin G.
experimental part, p. 4504 - 4517 (2009/06/06)
The prostate-specific membrane antigen (PSMA) is increasingly recognized as a viable target for imaging and therapy of cancer. We prepared seven 99mTc/Re-labeled compounds by attaching known Tc/Re chelating agents to an amino-functionalized PSMA inhibitor (lys-NHCONH-glu) with or without a variable length linker moiety. Ki values ranged from 0.17 to 199 nM. Ex vivo biodistribution and in vivo imaging demonstrated the degree of specific binding to engineered PSMA+ PC3 PIP tumors. PC3-PIP cells are derived from PC3 that have been transduced with the gene for PSMA. Despite demonstrating nearly the lowest PSMA inhibitory potency of this series, [99mTc(CO) 3(L1)]+ (L1 = (2-pyridylmethyl)2N(CH 2)4CH(CO2H)-NHCO-(CH2) 6CO-NH-lys-NHCONH-glu) showed the highest, most selective PIP tumor uptake, at 7.9 ± 4.0% injected dose per gram of tissue at 30 min postinjection. Radioactivity cleared from nontarget tissues to produce a PIP to flu (PSMA-PC3) ratio of 44:1 at 120 min postinjection. PSMA can accommodate the steric requirements of 99mTc/Re complexes within PSMA inhibitors, the best results achieved with a linker moiety between the ε amine of the urea lysine and the chelator.
