Tailored Gallium(III) Chelator NOPO: Synthesis, Characterization, Bioconjugation, and Application in Preclinical Ga-68-PET Imaging
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11310%2F14%3A10286119" target="_blank" >RIV/00216208:11310/14:10286119 - isvavai.cz</a>
Result on the web
<a href="http://dx.doi.org/10.1021/mp400642s" target="_blank" >http://dx.doi.org/10.1021/mp400642s</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1021/mp400642s" target="_blank" >10.1021/mp400642s</a>
Alternative languages
Result language
angličtina
Original language name
Tailored Gallium(III) Chelator NOPO: Synthesis, Characterization, Bioconjugation, and Application in Preclinical Ga-68-PET Imaging
Original language description
The bifunctional chelator NOPO (1,4,7-triazacyclononane-1,4-bis[methylene(hydroxymethyl)phosphinic acid]-7-[methylene(2-carboxyethyl)phosphinic acid]) shows remarkably high Ga(III) complexation efficiency and comprises one carboxylic acid moiety which isnot involved into metal ion coordination. An improved synthetic protocol affords NOPO with 45% overall yield. Stepwise protonation constants (log Ka), determined by potentiometry, are 11.96, 5.22, 3.77, and 1.54; the stability constant of the Ga(III) complex is log K-GaL = 25.0. Within 5 min, Ga-68(III) incorporation by NOPO is virtually quantitative at room temperature between pH 3 and 4, and at 95 degrees C at pH ranging from 0.5 to 7, at NOPO concentrations of 30 mu M and 10 mu M, respectively. During amide bond formation at the distant carboxylate using the HATU coupling reagent, an intramolecular phosphinic acid ester (phosphilactone) is formed, which is cleaved during Ga-68 complexation or in acidic media, such as trifluoroacetic
Czech name
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Czech description
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Classification
Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
CA - Inorganic chemistry
OECD FORD branch
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Result continuities
Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
S - Specificky vyzkum na vysokych skolach<br>I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Others
Publication year
2014
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Molecular Pharmaceutics
ISSN
1543-8384
e-ISSN
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Volume of the periodical
11
Issue of the periodical within the volume
11
Country of publishing house
US - UNITED STATES
Number of pages
11
Pages from-to
3893-3903
UT code for WoS article
000344307700013
EID of the result in the Scopus database
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