13
views
0
recommends
+1 Recommend
0 collections
    0
    shares
      • Record: found
      • Abstract: found
      • Article: not found

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

      Drug resistance updates : reviews and commentaries in antimicrobial and anticancer chemotherapy
      Animals, Antineoplastic Agents, metabolism, therapeutic use, Clinical Trials as Topic, Doxorubicin, analogs & derivatives, Drug Carriers, chemistry, Endothelial Cells, Genetic Therapy, Genetic Vectors, genetics, Humans, Integrin alphaVbeta3, analysis, Mutation, Neoplasms, diagnosis, drug therapy, Oligopeptides, Peptides, Cyclic, Polyethylene Glycols, RNA, Small Interfering, Recombinant Proteins, Transfection, Tumor Necrosis Factor-alpha, Vascular Endothelial Growth Factor A

      Read this article at

      ScienceOpenPublisherPubMed
      Bookmark
          There is no author summary for this article yet. Authors can add summaries to their articles on ScienceOpen to make them more accessible to a non-specialist audience.

          Abstract

          During the past decade, RGD-peptides have become a popular tool for the targeting of drugs and imaging agents to alphavbeta3-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 alphavbeta3-integrin, which demonstrates the feasibility of this approach. This review will summarize the structural requirements for RGD-peptides and RGD-mimetics as ligands for alphavbeta3. 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.

          Related collections

          Author and article information

          Comments

          Comment on this article