NDLI: Binding and Uptake of RGD-Containing Ligands to Cellular α $_{v}$ β $

Content Provider	Springer Nature Link
Author	Cressman, Sonya Sun, Ying Maxwell, E. Jane Fang, Ning Chen, David D. Y. Cullis, Pieter R.
Copyright Year	2008
Abstract	The cyclic peptide, cRGDf[N(me)]V, binds to the α $_{v}$ β $_{3}$ integrin and can disrupt binding of the integrin to its natural ligands in the extracellular matrix. In this work, the ability of a water-soluble, fluorescently labeled variant of the RGD-containing peptide (cRGDfK-488) to bind to integrins on human umbilical vascular endothelial cells (HUVEC) and subsequently undergo endocytosis was characterized. This information was compared to the binding and uptake properties of an α $_{v}$ β $_{3}$ integrin-specific monoclonal antibody, LM609X. The specificity of the RGD-containing peptide is assessed by comparison with control peptide that does not bind to the α $_{v}$ β $_{3}$ integrin, cRADfK-488. Using a high purity construct, it is shown that the RGD ligand exhibits dissociation constants in the micromolar range whereas LM609X exhibits dissociation constants in the nanomolar range. However, the RGD ligand showed greater uptake following incubation at temperatures which permit endocytosis. A 7.4-fold increase in uptake of the RGD peptide was observed following a 1 h incubation with HUVEC at 37°C (an endocytosis permissive temperature), as compared to that at 4°C (an endocytosis prohibitive temperature). In contrast, only a 1.9-fold increase in cell-associated fluorescence was observed for similar incubations with LM609X. Results from fluorescence microscopy supports the notion that the RGD peptide is rapidly endocytosed at 37°C as compared to LM609X. These results are discussed with regard to previous work indicating that RGD ligands enter cells by integrin-independent pathways. These studies provide well-controlled measures of how RGD ligands stimulate endocytosis. This may be of considerable interest for intracellular delivery of ligand-associated drugs in anti-angiogenic applications.
Starting Page	49
Ending Page	59
Page Count	11
File Format	PDF
ISSN	15733149
Journal	International Journal of Peptide Research and Therapeutics
Volume Number	15
Issue Number	1
e-ISSN	15733904
Language	English
Publisher	Springer Netherlands
Publisher Date	2008-12-02
Publisher Place	Dordrecht
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	α $_{v}$ β $_{3}$ integrins RGD Endocytosis Angiogenesis Molecular Medicine Pharmacology/Toxicology Pharmaceutical Sciences/Technology Polymer Sciences Animal Anatomy / Morphology / Histology Biochemistry
Content Type	Text
Resource Type	Article
Subject	Analytical Chemistry Drug Discovery Biochemistry Molecular Medicine Bioengineering

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