Abstract
During the past decade, RGD-peptides have become a popular tool for the targeting of drugs and imaging agents to αvβ3- integrin expressing tumour vasculature. RGD-peptides have been introduced by recombinant means into therapeutic proteins and viruses. Chemical means have been applied to couple RGD-peptides and RGD-mimetics to liposomes, polymers, peptides, small molecule drugs and radiotracers. Some of these products show impressive results in preclinical animal models and a RGD targeted radiotracer has already successfully been tested in humans for the visualization of αvβ3-integrin, which demonstrates the feasibility of this approach. This review will summarize the structural requirements for RGD-peptides and RGD-mimetics as ligands for αvβ3. We will show how they have been introduced in the various types of constructs by chemical and recombinant techniques. The importance of multivalent RGD-constructs for high affinity binding and internalization will be highlighted. Furthermore the in vitro and in vivo efficacy of RGD-targeted therapeutics and diagnostics reported in recent years will be reviewed. © 2005 Elsevier Ltd. All rights reserved.
Original language | English |
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Pages (from-to) | 381-402 |
Number of pages | 22 |
Journal | Drug Resistance Updates |
Volume | 8 |
Issue number | 6 |
DOIs | |
Publication status | Published - 1 Dec 2005 |
Keywords
- Angiogenesis
- Antivascular therapies
- Arg-Gly-Asp
- Cancer
- Cytostatic drugs
- Drug delivery
- Endothelial cells
- Gene delivery
- Polymers
- Radiotracer
- RGD
- Therapeutic proteins
- arginylglycylaspartic acid
- cilengitide
- cytarabine
- doxorubicin
- paclitaxel
- rgd10 peptide
- unclassified drug
- Adenoviridae
- amino acid sequence
- clinical trial
- drug accumulation
- drug binding
- drug delivery system
- drug structure
- drug synthesis
- drug targeting
- gene targeting
- heterozygote
- human
- ligand binding
- priority journal
- protein binding
- review
- tumor vascularization
- virus replication