Iodinated Choline Transport-Targeted Tracers

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60461373%3A22330%2F20%3A43923099" target="_blank" >RIV/60461373:22330/20:43923099 - isvavai.cz</a>

Alternative codes found

RIV/61389013:_____/20:00536679 RIV/00216208:11310/20:10422520 RIV/61989592:15110/20:73602636

Result on the web

<a href="https://pubs.acs.org/doi/10.1021/acs.jmedchem.0c01710" target="_blank" >https://pubs.acs.org/doi/10.1021/acs.jmedchem.0c01710</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1021/acs.jmedchem.0c01710" target="_blank" >10.1021/acs.jmedchem.0c01710</a>

Result language

angličtina

Original language name

Iodinated Choline Transport-Targeted Tracers

Original language description

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. © 2020 American Chemical Society. All rights reserved.

Czech name

—

Czech description

—

Type

J_imp - Article in a specialist periodical, which is included in the Web of Science database

CEP classification

—

OECD FORD branch

10404 - Polymer science

Project

<a href="/en/project/TE01020028" target="_blank" >TE01020028: Center for Development of Original Drugs</a><br>

Continuities

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Publication year

2020

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

Journal of Medicinal Chemistry

ISSN

0022-2623

e-ISSN

—

Volume of the periodical

63

Issue of the periodical within the volume

24

Country of publishing house

US - UNITED STATES

Number of pages

19

Pages from-to

15960-15978

UT code for WoS article

000603401900045

EID of the result in the Scopus database

2-s2.0-85097899954