1246457-10-2Relevant articles and documents
Iodinated Choline Transport-Targeted Tracers
?vec, Pavel,Novy, Zbyněk,Ku?ka, Jan,Pet?ík, Milo?,Sedlá?ek, Ond?ej,Kucha?, Martin,Li?ková, Barbora,Medvedíková, Martina,Kolouchová, Kristyna,Groborz, Ond?ej,Loukotová, Lenka,Konefa?, Rafa? ?.,Hajdúch, Marián,Hruby, Martin
, p. 15960 - 15978 (2020/12/23)
We present a novel series of radioiodinated tracers and potential theranostics for diseases accompanied by pathological function of proteins involved in choline transport. Unlike choline analogues labeled with 11C or 18F that are currently used in the clinic, the iodinated compounds described herein are applicable in positron emission tomography, single-photon emission computed tomography, and potentially in therapy, depending on the iodine isotope selection. Moreover, favorable half-lives of iodine isotopes result in much less challenging synthesis by isotope exchange reaction. Six of the described compounds were nanomolar ligands, and the best compound possessed an affinity 100-fold greater than that of choline. Biodistribution data of 125I-labeled ligands in human prostate carcinoma bearing (PC-3) mice revealed two compounds with a biodistribution profile superior to that of [18F]fluorocholine.
COMPOUND TARGETING NOREPINEPHRINE TRANSPORTER
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, (2020/07/31)
The invention concerns a compound according to following formula, wherein R1 is an F or an I residue.
Iodination of verapamil for a stronger induction of death, through GSH efflux, of cancer cells overexpressing MRP1
Barattin, Régis,Perrotton, Thomas,Trompier, Doriane,Lorendeau, Doriane,Pietro, Attilio Di,D'Hardemare, Amaury Du Moulinet,Baubichon-Cortay, Hélne
experimental part, p. 6265 - 6274 (2010/10/19)
The multidrug resistance protein 1 (MRP1), involved in multidrug resistance (MDR) of cancer cells, was found to be modulated by verapamil, through stimulation of GSH transport, leading to apoptosis of MRP1-overexpressing cells. In this study, various iodi
