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Structure-Activity Relationship of F-18-Labeled Phosphoramidate Peptidomimetic Prostate-Specific Membrane Antigen (PSMA)-Targeted Inhibitor Analogues for PET Imaging of Prostate Cancer
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SYSNO ASEP 0469119 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název Structure-Activity Relationship of F-18-Labeled Phosphoramidate Peptidomimetic Prostate-Specific Membrane Antigen (PSMA)-Targeted Inhibitor Analogues for PET Imaging of Prostate Cancer Tvůrce(i) Dannoon, S. (US)
Ganguly, T. (US)
Cahaya, H. (US)
Geruntho, J. J. (US)
Galliher, M. S. (US)
Beyer, S. K. (US)
Choy, C.J. (US)
Hopkins, M.R. (US)
Regan, M. (US)
Blecha, J.E. (US)
Škultétyová, Ĺubica (BTO-N) RID
Drake, Ch.R. (US)
Jivan, S. (US)
Bařinka, Cyril (BTO-N) RID, ORCID
Jones, E. F. (US)
Berkman, C.E. (US)
VanBrocklin, H.F. (US)Zdroj.dok. Journal of Medicinal Chemistry. - : American Chemical Society - ISSN 0022-2623
Roč. 59, č. 12 (2016), s. 5684-5694Poč.str. 11 s. Jazyk dok. eng - angličtina Země vyd. US - Spojené státy americké Klíč. slova GLUTAMATE CARBOXYPEPTIDASE-II ; REACTION-MECHANISM ; FOLATE-HYDROLASE Vědní obor RIV FD - Onkologie a hematologie CEP GAP301/12/1513 GA ČR - Grantová agentura ČR ED1.1.00/02.0109 GA MŠMT - Ministerstvo školství, mládeže a tělovýchovy Institucionální podpora BTO-N - RVO:86652036 UT WOS 000378662900007 DOI 10.1021/acs.jmedchem.5b01850 Anotace A series of phosphoramidate-based prostate specific membrane antigen (PSMA) inhibitors of increasing lipophilicity were synthesized (4, 5, and 6), and their fluorine-18 analogs were evaluated for use as positron emission tomography (PET) imaging agents for prostate cancer. To gain insight into their modes of binding, they were also cocrystallized with the extracellular domain of PSMA. All analogs exhibited irreversible binding to PSMA with IC50 values ranging from 0.4 to 1.3 nM. In vitro assays showed binding and rapid internalization (80-95%, 2 h) of the radiolabeled ligands in PSMA(+) cells. In vivo distribution demonstrated significant uptake in CWR22Rv1 (PSMA(+)) tumor, with tumor to blood ratios of 25.6:1, 63.6:1, and 69.6:1 for [F-18]4, [F-18]. 5, and [18F]6, respectively, at 2 h postinjection. Installation of aminohexanoic acid (AH) linkers in the phosphoramidate scaffold improved their PSMA binding and inhibition and was critical for achieving suitable in vivo imaging properties, positioning [F-18]5 and [F-18]6 as favorable candidates for future prostate cancer imaging clinical trials. Pracoviště Biotechnologický ústav Kontakt Monika Kopřivová, Monika.Koprivova@ibt.cas.cz, Tel.: 325 873 700 Rok sběru 2017
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