Iodinated choline transport-targeted tracers

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

doi:https://dx.doi.org/10.1021/acs.jmedchem.0c01710

Number of the records: 1

Iodinated choline transport-targeted tracers

1.

SYSNO ASEP	0536679
Document Type	J - Journal Article
R&D Document Type	Journal Article
Subsidiary J	Článek ve WOS
Title	Iodinated choline transport-targeted tracers
Author(s)	Švec, Pavel (UMCH-V)_{RID, ORCID} Nový, Z. (CZ) Kučka, Jan (UMCH-V)_{RID, ORCID} Petřík, M. (CZ) Sedláček, Ondřej (UMCH-V)_{RID, ORCID} Kuchař, M. (CZ) Lišková, B. (CZ) Medvedíková, M. (CZ) Kolouchová, Kristýna (UMCH-V)_{ORCID, RID} Groborz, Ondřej (UMCH-V)_{ORCID, RID} Loukotová, Lenka (UMCH-V)_{RID, ORCID} Konefal, Rafal (UMCH-V)_{RID, ORCID} Hajdúch, M. (CZ) Hrubý, Martin (UMCH-V)_{RID, ORCID}
Source Title	Journal of Medicinal Chemistry. - : American Chemical Society - ISSN 0022-2623 Roč. 63, č. 24 (2020), s. 15960-15978
Number of pages	19 s.
Language	eng - English
Country	US - United States
Keywords	choline transport ; radioiodination ; fluorocholine
Subject RIV	CD - Macromolecular Chemistry
OECD category	Polymer science
R&D Projects	GA19-01602S GA ČR - Czech Science Foundation (CSF)
	NV16-30544A GA MZd - Ministry of Health (MZ)
	LM2015064 GA MŠMT - Ministry of Education, Youth and Sports (MEYS)
Method of publishing	Limited access
Institutional support	UMCH-V - RVO:61389013
UT WOS	000603401900045
EID SCOPUS	85097899954
DOI	10.1021/acs.jmedchem.0c01710
Annotation	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.
Workplace	Institute of Macromolecular Chemistry
Contact	Eva Čechová, cechova@imc.cas.cz ; Tel.: 296 809 358
Year of Publishing	2021
Electronic address	https://pubs.acs.org/doi/10.1021/acs.jmedchem.0c01710

Number of the records: 1