1023970-50-4Relevant academic research and scientific papers
"clickable" Albumin Binders for Modulating the Tumor Uptake of Targeted Radiopharmaceuticals
Bachmann, Michael,Brandt, Florian,Kopka, Klaus,Laube, Markus,Pietzsch, Jens,Ullrich, Martin,Wodtke, Robert,L?ser, Reik,Pietzsch, Hans-Jürgen,Van Den Hoff, J?rg
supporting information, p. 710 - 733 (2022/01/11)
The intentional binding of radioligands to albumin gains increasing attention in the context of radiopharmaceutical cancer therapy as it can lead to an enhanced radioactivity uptake into the tumor lesions and, thus, to a potentially improved therapeutic outcome. However, the influence of the radioligand's albumin-binding affinity on the time profile of tumor uptake has been only partly addressed so far. Based on the previously identified N?-4-(4-iodophenyl)butanoyl-lysine scaffold, we designed "clickable"lysine-derived albumin binders (cLABs) and determined their dissociation constants toward albumin by novel assay methods. Structure-activity relationships were derived, and selected cLABs were applied for the modification of the somatostatin receptor subtype 2 ligand (Tyr3)octreotate. These novel conjugates were radiolabeled with copper-64 and subjected to a detailed in vitro and in vivo radiopharmacological characterization. Overall, the results of this study provide an incentive for further investigations of albumin binders for applications in endoradionuclide therapies.
A portable albumin binder from a DNA-encoded chemical library
Dumelin, Christoph E.,Truessel, Sabrina,Buller, Fabian,Trachsel, Eveline,Bootz, Frank,Zhang, Yixin,Mannocci, Luca,Beck, Susanne C.,Drumea-Mirancea, Mihaela,Seeliger, Mathias W.,Baltes, Christof,Mueggler, Thomas,Kranz, Felicitas,Rudin, Markus,Melkko, Samu,Scheuermann, Joerg,Neri, Dario
supporting information; experimental part, p. 3196 - 3201 (2009/02/08)
(Figure Presented) Seeing eye to eye: Plasma-protein binding is effective in improving the pharmacokinetic properties of otherwise short-lived molecules. One compound in a class of small portable albumin binders can be used to improve the in vivo circulatory half-life of two widely used contrast agents. It improves the imaging performance of fluorescein in angiographic analysis of the retina of mice (see picture).
