Iodinated Choline Transport-Targeted Tracers

Kód výsledku v 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>

Nalezeny alternativní kódy

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

Výsledek na webu

<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>

Jazyk výsledku

angličtina

Název v původním jazyce

Iodinated Choline Transport-Targeted Tracers

Popis výsledku v původním jazyce

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.

Název v anglickém jazyce

Iodinated Choline Transport-Targeted Tracers

Popis výsledku anglicky

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.

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

10404 - Polymer science

Projekt

<a href="/cs/project/TE01020028" target="_blank" >TE01020028: Centrum vývoje originálních léčiv</a><br>

Návaznosti

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

Rok uplatnění

2020

Kód důvěrnosti údajů

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

Název periodika

Journal of Medicinal Chemistry

ISSN

0022-2623

e-ISSN

—

Svazek periodika

63

Číslo periodika v rámci svazku

24

Stát vydavatele periodika

US - Spojené státy americké

Počet stran výsledku

19

Strana od-do

15960-15978

Kód UT WoS článku

000603401900045

EID výsledku v databázi Scopus

2-s2.0-85097899954