Iodinated choline transport-targeted tracers

0536679 - ÚMCH 2021 RIV US eng J - Journal Article
Švec, Pavel - Nový, Z. - Kučka, Jan - Petřík, M. - Sedláček, Ondřej - Kuchař, M. - Lišková, B. - Medvedíková, M. - Kolouchová, Kristýna - Groborz, Ondřej - Loukotová, Lenka - Konefal, Rafal - Hajdúch, M. - Hrubý, Martin
Iodinated choline transport-targeted tracers.
Journal of Medicinal Chemistry. Roč. 63, č. 24 (2020), s. 15960-15978. ISSN 0022-2623. E-ISSN 1520-4804
R&D Projects: GA ČR(CZ) GA19-01602S; GA MZd(CZ) NV16-30544A; GA MŠMT(CZ) LM2015064
Institutional support: RVO:61389013
Keywords : choline transport * radioiodination * fluorocholine
OECD category: Polymer science
Impact factor: 7.446, year: 2020
Method of publishing: Limited access
https://pubs.acs.org/doi/10.1021/acs.jmedchem.0c01710

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.
Permanent Link: http://hdl.handle.net/11104/0315705