Cyclic RGD Peptides Incorporating Cycloalkanes: Synthesis and Evaluation as PET Radiotracers for Tumor Imaging
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چکیده
منابع مشابه
Radiolabeled cyclic RGD peptides as radiotracers for tumor imaging
The integrin family comprises 24 transmembrane receptors, each a heterodimeric combination of one of 18α and one of 8β subunits. Their main function is to integrate the cell adhesion and interaction with the extracellular microenvironment with the intracellular signaling and cytoskeletal rearrangement through transmitting signals across the cell membrane upon ligand binding. Integrin αvβ3 is a ...
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The integrin family is a group of transmembrane glycoprotein comprised of 19 α- and 8 β-subunits that are expressed in 25 different α/β heterodimeric combinations on the cell surface. Integrins play critical roles in many physiological processes, including cell attachment, proliferation, bone remodeling, and wound healing. Integrins also contribute to pathological events such as thrombosis, ath...
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Inhibition of binding of extracellular matrix (ECM) proteins fibrinogen and vitronectin to the IIbβ3 and vβ3 integrins, respectively, is of great pharmaceutical interest. Both receptors recognize the RGD tripeptide sequence, which is present in these natural ligands. The development of antagonists for these integrins is therefore often based on this tripeptide unit and several cyclic RGD pept...
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This study sought to evaluate FITC-conjugated cyclic RGD peptides (FITC-RGD2, FITC-3P-RGD2, and FITC-Galacto-RGD2) as fluorescent probes for in vitro assays of integrin αvβ3/αvβ5 expression in tumor tissues. FITC-RGD2, FITC-3P-RGD2, and FITC-Galacto-RGD2 were prepared, and their integrin αvβ3/αvβ5 binding affinity was determined using the displacement assay against (125)I-echistatin bound to U8...
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ژورنال
عنوان ژورنال: ACS Medicinal Chemistry Letters
سال: 2014
ISSN: 1948-5875,1948-5875
DOI: 10.1021/ml500135t