RGD-based strategies for selective delivery of therapeutics and imaging agents to the tumour vasculature

Kai Temming, Raymond M. Schiffelers, Grietje Molema, Robbert J. Kok

Research output: Contribution to journalReview articlepeer-review

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 languageEnglish
Pages (from-to)381-402
Number of pages22
JournalDrug Resistance Updates
Volume8
Issue number6
DOIs
Publication statusPublished - 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

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