Iodinated Choline Transport-Targeted Tracers.

xlomafota13 shared this article with you from Inoreader Iodinated Choline Transport-Targeted Tracers. Via radioactive iodine Related Articles Iodinated Choline Transport-Targeted Tracers. J Med Chem. 2020 12 24;63(24):15960-15978 Authors: Švec P, Nový Z, Kučka J, Petřík M, Sedláček O, Kuchař M, Lišková B, Medvedíková M, Kolouchová K, Groborz O, Loukotová L, Konefał RŁ, Hajdúch M, Hrubý M Abstract 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. PMID: 33271015 [PubMed - indexed for MEDLINE] View on the web Inoreader. Take back control of your news feed. Follow us on Twitter and Facebook.