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A dimeric bicyclic RGD ligand displays enhanced integrin binding affinity and strong biological effects on U-373 MG glioblastoma cells.
- Source :
-
Organic & biomolecular chemistry [Org Biomol Chem] 2019 Oct 21; Vol. 17 (39), pp. 8913-8917. Date of Electronic Publication: 2019 Sep 26. - Publication Year :
- 2019
-
Abstract
- A C <subscript>2</subscript> -symmetric bicyclic peptide bearing two RGD motifs was developed as a dimeric ligand, and it displayed enhanced inhibition of ECM protein binding to purified integrin receptors as compared to monomeric RGD analogues. Moreover, the dimeric bicyclic ligand induced cell detachment and inhibited FAK phosphorylation in U-373 MG glioblastoma cells.
- Subjects :
- Binding Sites drug effects
Cell Adhesion drug effects
Cell Line, Tumor
Dimerization
Extracellular Matrix Proteins chemistry
Focal Adhesion Kinase 1 antagonists & inhibitors
Focal Adhesion Kinase 1 metabolism
Glioblastoma metabolism
Glioblastoma pathology
Humans
Ligands
Peptides, Cyclic chemical synthesis
Peptides, Cyclic chemistry
Phosphorylation drug effects
Extracellular Matrix Proteins antagonists & inhibitors
Glioblastoma drug therapy
Integrins chemistry
Oligopeptides chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1477-0539
- Volume :
- 17
- Issue :
- 39
- Database :
- MEDLINE
- Journal :
- Organic & biomolecular chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 31556442
- Full Text :
- https://doi.org/10.1039/c9ob01811e