1. RGD-based strategies for selective delivery of therapeutics and imaging agents to the tumour vasculature
- Author
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Temming, Kai, Schiffelers, Raymond M., Molema, Grietje, Kok, Robbert J., Sub Drug targeting, Sub Drug delivery, Pharmaceutics, Sub Drug targeting, Sub Drug delivery, and Pharmaceutics
- Subjects
CONDITIONALLY REPLICATIVE ADENOVIRUSES ,Vascular Endothelial Growth Factor A ,Cancer Research ,Polymers ,Endothelial cells ,Therapeutic proteins ,Cilengitide ,protein binding ,Pharmacology ,gene targeting ,Polyethylene Glycols ,chemistry.chemical_compound ,paclitaxel ,cytarabine ,drug binding ,rgd10 peptide ,Neoplasms ,Arg-Gly-Asp ,drug delivery system ,Pharmacology (medical) ,Gene delivery ,VITRONECTIN RECEPTOR ANTAGONIST ,POTENT ANTITUMOR-ACTIVITY ,RNA, Small Interfering ,Internalization ,virus replication ,media_common ,Cancer ,Clinical Trials as Topic ,Drug Carriers ,RGD ,Antivascular therapies ,clinical trial ,Small molecule ,Recombinant Proteins ,unclassified drug ,Infectious Diseases ,Oncology ,priority journal ,Drug delivery ,Oligopeptides ,media_common.quotation_subject ,ligand binding ,Genetic Vectors ,review ,Antineoplastic Agents ,Computational biology ,Biology ,Transfection ,doxorubicin ,Peptides, Cyclic ,Adenoviridae ,POSITRON-EMISSION-TOMOGRAPHY ,tumor vascularization ,VIRUS-LIKE PARTICLES ,In vivo ,SNAKE-VENOM DISINTEGRINS ,Animals ,Humans ,human ,drug accumulation ,arginylglycylaspartic acid ,Radiotracer ,Tumor Necrosis Factor-alpha ,NECROSIS-FACTOR-ALPHA ,Endothelial Cells ,drug targeting ,Genetic Therapy ,Integrin alphaVbeta3 ,heterozygote ,amino acid sequence ,drug structure ,chemistry ,Targeted drug delivery ,cilengitide ,Doxorubicin ,Mutation ,drug synthesis ,Cytostatic drugs ,Angiogenesis ,CANCER ALPHA(V)-INTEGRIN EXPRESSION ,ALPHA(V)BETA(3) INTEGRIN ANTAGONISTS ,Arginylglycylaspartic acid - Abstract
During the past decade, RGD-peptides have become a popular tool for the targeting of drugs and imaging agents to a(v)beta(3)-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 alpha(v)beta(3)-integrin, which demonstrates the feasibility of this approach. This review will summarize the structural requirements for RGD-peptides and RGD-mimetics as ligands for alpha(v)beta(3). 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. (C) 2005 Elsevier Ltd. All rights reserved.
- Published
- 2005