Evaluation of the H2)dedpa scaffold and its cRGDyK conjugates for labeling with 64Cu

Inorganic Chemistry
Eszter BorosChris Orvig

Abstract

Studies of the acyclic ligand scaffold H(2)dedpa and its derivatives with the peptide cRGDyK for application in copper radiopharmaceuticals are described. Previously shown to be a superb ligand for (67/68)Ga, the chelate is now shown to coordinate (64)Cu in its derivatized and nonderivatized forms rapidly under mild reaction conditions (10 min, RT, pH 5.5 10 mM sodium acetate buffered solution). The hexadentate, distorted octahedral coordination of H(2)dedpa is confirmed in the corresponding solid state X-ray crystal structure of [Cu(dedpa)]. Cyclic voltammetry determined the reduction potential of [Cu(dedpa)] to be below values found for common bioreductants. Reduction and reoxidation were irreversible but reproducible, indicating a potential change of coordination mode upon reduction of Cu(II) to Cu(I). The thermodynamic stability constant log K(CuL) was determined to be 19.16(5), comparable to other frequently used (64)Cu chelates. Serum stability of the (64)Cu labeled chelate revealed only 3% transchelation/association to serum proteins after 2 h, while the conjugates reveal 10% ([Cu(RGD1)]) and 6% ([Cu(RGD2)]) transchelation at the same time point.

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Mar 3, 2012·Nuclear Medicine and Biology·Eszter BorosChris Orvig

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Citations

Oct 31, 2012·Inorganic Chemistry·Gwendolyn A BaileyChris Orvig
Sep 24, 2015·Inorganic Chemistry·Attila ForgácsCarlos Platas-Iglesias
Feb 13, 2016·Dalton Transactions : an International Journal of Inorganic Chemistry·Thomas W PriceGraeme J Stasiuk
Oct 27, 2017·Dalton Transactions : an International Journal of Inorganic Chemistry·Laura Caneda-MartínezCarlos Platas-Iglesias
May 11, 2016·Dalton Transactions : an International Journal of Inorganic Chemistry·Caterina F RamogidaChris Orvig
Dec 2, 2014·Dalton Transactions : an International Journal of Inorganic Chemistry·David Brasse, Aline Nonat
Feb 11, 2015·Dalton Transactions : an International Journal of Inorganic Chemistry·Aurora Rodríguez-RodríguezCarlos Platas-Iglesias
Dec 14, 2018·Dalton Transactions : an International Journal of Inorganic Chemistry·Rosa Pujales-ParadelaDavid Esteban-Gómez
Nov 1, 2013·Chemical Society Reviews·Eric W Price, Chris Orvig
Mar 29, 2014·Dalton Transactions : an International Journal of Inorganic Chemistry·Eric W PriceChris Orvig
Oct 10, 2012·Dalton Transactions : an International Journal of Inorganic Chemistry·Jakub SimečekJohannes Notni
Aug 31, 2017·Dalton Transactions : an International Journal of Inorganic Chemistry·María de Guadalupe Jaraquemada-PeláezChris Orvig
Jul 27, 2021·Inorganic Chemistry·Lily SouthcottChris Orvig
Dec 4, 2013·Molecular Pharmaceutics·Eszter BorosPeter Caravan
Aug 2, 2013·Journal of the American Chemical Society·Eric W PriceChris Orvig
Sep 16, 2017·Inorganic Chemistry·Raphaël GilletLoïc J Charbonnière
Dec 19, 2016·Inorganic Chemistry·Peter CombaHubert Wadepohl
Mar 24, 2020·Chemical Reviews·Weijun WeiWeibo Cai
Aug 22, 2017·Journal of the American Chemical Society·Nilantha BandaraLiviu M Mirica
Feb 19, 2015·Inorganic Chemistry·Ferenc Krisztián KálmánGyula Tircsó

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