• Something wrong with this record ?

Iodinated Choline Transport-Targeted Tracers

P. Švec, Z. Nový, J. Kučka, M. Petřík, O. Sedláček, M. Kuchař, B. Lišková, M. Medvedíková, K. Kolouchová, O. Groborz, L. Loukotová, RŁ. Konefał, M. Hajdúch, M. Hrubý

. 2020 ; 63 (24) : 15960-15978. [pub] 20201203

Language English Country United States

Document type Journal Article, Research Support, Non-U.S. Gov't

Persistent link   https://www.medvik.cz/link/bmc21011702

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.

References provided by Crossref.org

000      
00000naa a2200000 a 4500
001      
bmc21011702
003      
CZ-PrNML
005      
20211207151954.0
007      
ta
008      
210420s2020 xxu f 000 0|eng||
009      
AR
024    7_
$a 10.1021/acs.jmedchem.0c01710 $2 doi
035    __
$a (PubMed)33271015
040    __
$a ABA008 $b cze $d ABA008 $e AACR2
041    0_
$a eng
044    __
$a xxu
100    1_
$a Švec, Pavel $u Institute of Macromolecular Chemistry, CAS, Heyrovského sq. 2, Prague 6 162 06, Czech Republic $u Department of Physical and Macromolecular Chemistry, Faculty of Science, Charles University, Hlavova 8, Prague 2 128 43, Czech Republic
245    10
$a Iodinated Choline Transport-Targeted Tracers / $c P. Švec, Z. Nový, J. Kučka, M. Petřík, O. Sedláček, M. Kuchař, B. Lišková, M. Medvedíková, K. Kolouchová, O. Groborz, L. Loukotová, RŁ. Konefał, M. Hajdúch, M. Hrubý
520    9_
$a 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.
650    _2
$a zvířata $7 D000818
650    _2
$a apoptóza $7 D017209
650    _2
$a proliferace buněk $7 D049109
650    _2
$a cholin $x analogy a deriváty $x farmakokinetika $7 D002794
650    _2
$a radioizotopy fluoru $x farmakokinetika $7 D005462
650    _2
$a lidé $7 D006801
650    _2
$a radioizotopy jodu $x farmakokinetika $7 D007457
650    _2
$a mužské pohlaví $7 D008297
650    _2
$a myši $7 D051379
650    _2
$a myši SCID $7 D016513
650    _2
$a pozitronová emisní tomografie $7 D049268
650    _2
$a nádory prostaty $x diagnostické zobrazování $x metabolismus $x patologie $7 D011471
650    12
$a radioaktivní indikátory $7 D011849
650    _2
$a radiofarmaka $x farmakokinetika $7 D019275
650    _2
$a tkáňová distribuce $7 D014018
650    _2
$a nádorové buňky kultivované $7 D014407
650    _2
$a xenogenní modely - testy protinádorové aktivity $7 D023041
655    _2
$a časopisecké články $7 D016428
655    _2
$a práce podpořená grantem $7 D013485
700    1_
$a Nový, Zbyněk $u Institute of Molecular and Translational Medicine, Faculty of Medicine and Dentistry, Palacký University Olomouc, Hněvotínská 5, Olomouc 779 00, Czech Republic
700    1_
$a Kučka, Jan $u Institute of Macromolecular Chemistry, CAS, Heyrovského sq. 2, Prague 6 162 06, Czech Republic
700    1_
$a Petřík, Miloš $u Institute of Molecular and Translational Medicine, Faculty of Medicine and Dentistry, Palacký University Olomouc, Hněvotínská 5, Olomouc 779 00, Czech Republic
700    1_
$a Sedláček, Ondřej $u Institute of Macromolecular Chemistry, CAS, Heyrovského sq. 2, Prague 6 162 06, Czech Republic
700    1_
$a Kuchař, Martin $u Forensic Laboratory of Biologically Active Substances, University of Chemistry and Technology, Technická 1905/5, Prague 160 00, Czech Republic
700    1_
$a Lišková, Barbora $u Institute of Molecular and Translational Medicine, Faculty of Medicine and Dentistry, Palacký University Olomouc, Hněvotínská 5, Olomouc 779 00, Czech Republic $7 xx0267204
700    1_
$a Medvedíková, Martina $u Institute of Molecular and Translational Medicine, Faculty of Medicine and Dentistry, Palacký University Olomouc, Hněvotínská 5, Olomouc 779 00, Czech Republic
700    1_
$a Kolouchová, Kristýna $u Institute of Macromolecular Chemistry, CAS, Heyrovského sq. 2, Prague 6 162 06, Czech Republic
700    1_
$a Groborz, Ondřej $u Institute of Macromolecular Chemistry, CAS, Heyrovského sq. 2, Prague 6 162 06, Czech Republic
700    1_
$a Loukotová, Lenka $u Institute of Macromolecular Chemistry, CAS, Heyrovského sq. 2, Prague 6 162 06, Czech Republic
700    1_
$a Konefał, Rafał Ł $u Institute of Macromolecular Chemistry, CAS, Heyrovského sq. 2, Prague 6 162 06, Czech Republic
700    1_
$a Hajdúch, Marián $u Institute of Molecular and Translational Medicine, Faculty of Medicine and Dentistry, Palacký University Olomouc, Hněvotínská 5, Olomouc 779 00, Czech Republic
700    1_
$a Hrubý, Martin $u Institute of Macromolecular Chemistry, CAS, Heyrovského sq. 2, Prague 6 162 06, Czech Republic
773    0_
$w MED00010049 $t Journal of medicinal chemistry $x 1520-4804 $g Roč. 63, č. 24 (2020), s. 15960-15978
856    41
$u https://pubmed.ncbi.nlm.nih.gov/33271015 $y Pubmed
910    __
$a ABA008 $b sig $c sign $y p $z 0
990    __
$a 20210420 $b ABA008
991    __
$a 20211207151952 $b ABA008
999    __
$a ok $b bmc $g 1650159 $s 1132081
BAS    __
$a 3
BAS    __
$a PreBMC
BMC    __
$a 2020 $b 63 $c 24 $d 15960-15978 $e 20201203 $i 1520-4804 $m Journal of medicinal chemistry $n J Med Chem $x MED00010049
LZP    __
$a Pubmed-20210420

Find record

Citation metrics

Archiving options