Radiolabeled 111In-FGF-2 Is Suitable for In Vitro/Ex Vivo Evaluations and In Vivo Imaging
| Autor: | Manuel Hilbert, Tessa Lühmann, Alessandra Moscaroli, Eliane Fischer, Gabriel Jones, Stephanie Wälti, Martin Béhé, Alain Blanc, Lorenz Meinel, Roger Schibli |
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| Rok vydání: | 2017 |
| Předmět: |
0301 basic medicine
Pathology medicine.medical_specialty Cell growth Chemistry Pharmaceutical Science Isothermal titration calorimetry Heparin Heparan sulfate Pharmacology Fibroblast growth factor In vitro 03 medical and health sciences chemistry.chemical_compound 030104 developmental biology 0302 clinical medicine 030220 oncology & carcinogenesis Drug Discovery medicine Molecular Medicine Ex vivo Preclinical imaging medicine.drug |
| Zdroj: | Molecular Pharmaceutics. 14:639-648 |
| ISSN: | 1543-8392 1543-8384 |
| DOI: | 10.1021/acs.molpharmaceut.6b00913 |
| Popis: | Fibroblast growth factor-2 (FGF-2) is a potent modulator of cell growth and regulation, with improper FGF-2 signaling being involved in impaired responses to injury or even cancer. Therefore, the exploitation of FGF-2 as a therapeutic drives the prerequisite for effective insight into drug disposition kinetics. In this article, we present an 111In-radiolabeled FGF-2 derivative for noninvasive imaging in small animals deploying single photon emission tomography (SPECT). 111In-FGF-2 is equally well suitable for in vitro and ex vivo investigations as 125I-FGF-2. Furthermore, 111In-FGF-2 permits the performance of in vivo imaging, for example for the analysis of FGF-2 containing pharmaceutical formulations in developmental or preclinical stages. 111In-FGF-2 had affinity for the low-molecular-weight heparin enoxaparin identical to that of unlabeled FGF-2 (Kd: 0.6 ± 0.07 μM and 0.33 ± 0.03 μM, respectively) as assessed by isothermal titration calorimetry. The binding of 111In-FGF-2 to heparan sulfate proteoglyc... |
| Databáze: | OpenAIRE |
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