A Cyclen-Based Tetraphosphinate Chelator for the Preparation of Radiolabeled Tetrameric Bioconjugates

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11310%2F13%3A10139598" target="_blank" >RIV/00216208:11310/13:10139598 - isvavai.cz</a>
Result on the web
<a href="http://dx.doi.org/10.1002/chem.201300338" target="_blank" >http://dx.doi.org/10.1002/chem.201300338</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1002/chem.201300338" target="_blank" >10.1002/chem.201300338</a>

Result language
angličtina
Original language name
A Cyclen-Based Tetraphosphinate Chelator for the Preparation of Radiolabeled Tetrameric Bioconjugates
Original language description
The cyclen-based tetraphosphinate chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrakis[methylene(2-carboxyethyl)phosphinic acid] (DOTPI) comprises four additional carboxylic acid moieties for bioconjugation. The thermodynamic stability constants (logKML) of metal complexes, as determined by potentiometry, were 23.11 for CuII, 20.0 for LuIII, 19.6 for YIII, and 21.0 for GdIII. DOTPI was functionalized with four cyclo(Arg-Gly-Asp-D-Phe-Lys) (RGD) peptides through polyethylene glycol (PEG4) linkers. The resulting tetrameric conjugate DOTPI(RGD)4 was radiolabeled with 177Lu and 64Cu and showed improved labeling efficiency compared with 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA). The labeled compounds were fully stable in transchelation challenges against trisodium diethylenetriaminepentaacetate (DTPA) and disodium ethylenediaminetetraacetic acid (ETDA), in phosphate buffered saline (PBS), and human plasma. Integrin v3 affinities of the non-radioactive LuIII and Cu
Czech name
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Czech description
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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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Project
<a href="/en/project/GA13-08336S" target="_blank" >GA13-08336S: Hybrid materials based on macrocyclic ligands for medical applications</a><br>
Continuities
Z - Vyzkumny zamer (s odkazem do CEZ)<br>I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year
2013
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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