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Cell Co-culture Patterning Using Aqueous Two-phase Systems
Published on: March 26, 2013
Template assembled cyclopeptides as multimeric system for integrin targeting and endocytosis.
Didier Boturyn1, Jean-Luc Coll, Elisabeth Garanger
1LEDSS, UMR CNRS 5616 and ICMG, FR-2607, Université Joseph Fourier, BP 53, 38041 Grenoble Cedex 9, France.
Journal of the American Chemical Society
|May 6, 2004
Summary
Researchers developed multimeric cyclopeptides targeting alpha(V)beta(3) integrin for cancer research. These novel molecules show promising binding and uptake properties for potential therapeutic and diagnostic applications in angiogenesis.
Area of Science:
- Biochemistry
- Molecular Biology
- Drug Discovery
Background:
- The alpha(V)beta(3) integrin receptor is crucial in human metastasis and tumor-induced angiogenesis.
- Selective alpha(V)beta(3) integrin ligands, like c[-RGDfV-] peptide, are vital tools in neoangiogenesis research, therapy, and diagnosis.
Purpose of the Study:
- To synthesize and biologically characterize template-assembled multimeric cyclopeptides for targeting alpha(V)beta(3) integrin-expressing cells.
- To evaluate the potential of these multivalent systems for targeted cellular uptake and applications in angiogenesis.
Main Methods:
- Modular synthesis of c[-RGDfK-] within a cyclodecapeptide template using chemoselective oxime bond formation.
- Creation of multivalent systems labeled with different reporter groups.
- Assessment of binding affinity to the alpha(V)beta(3) receptor and cellular uptake properties.
Main Results:
- Successfully assembled multivalent c[-RGDfK-] cyclopeptides on a template.
- Demonstrated significant binding propensity to the alpha(V)beta(3) receptor.
- Exhibited good cellular uptake properties, indicating effective targeting and endocytosis.
Conclusions:
- Template-assembled multimeric cyclopeptides are effective systems for targeting alpha(V)beta(3) integrin.
- These novel RAFT molecules offer unique properties for designing advanced multimeric systems.
- The findings provide a new perspective for utilizing integrins in angiogenesis regulation and developing sophisticated molecular conjugate vectors.
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