RGD-mediated delivery of small-molecule drugs

Sotirios Katsamakas; Theodora Chatzisideri; Savvas Thysiadis; Vasiliki Sarli

doi:10.4155/fmc-2017-0008

RGD-mediated delivery of small-molecule drugs

Future Med Chem. 2017 Apr;9(6):579-604. doi: 10.4155/fmc-2017-0008. Epub 2017 Apr 10.

Authors

Sotirios Katsamakas¹, Theodora Chatzisideri², Savvas Thysiadis², Vasiliki Sarli²

Affiliations

¹ Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotle University of Thessaloniki, University Campus, 54124, Thessaloniki, Greece.
² Department of Chemistry, Aristotle University of Thessaloniki, University Campus, 54124, Thessaloniki, Greece.

PMID: 28394627
DOI: 10.4155/fmc-2017-0008

Abstract

Conjugates of cytotoxic agents with RGD peptides (Arg-Gly-Asp) addressed to α_νβ₃, α₅β₁ and α_νβ₆ integrin receptors overexpressed by cancer cells, have recently gained attention as potential selective anticancer chemotherapeutics. In this review, the design and the development of RGD conjugates coupled to different small molecules including known cytotoxic drugs and natural products will be discussed.

Keywords: RGD conjugates; RGD peptide; angiogenesis; integrin avβ3; targeted drug delivery; tumor therapy.

Publication types

Review
Research Support, Non-U.S. Gov't

MeSH terms

Animals
Antineoplastic Agents / administration & dosage*
Antineoplastic Agents / chemistry*
Biological Products / administration & dosage
Biological Products / chemistry*
Cell Proliferation / drug effects
Drug Delivery Systems*
Humans
Integrins / metabolism
Molecular Structure
Oligopeptides / metabolism*
Small Molecule Libraries / administration & dosage*
Small Molecule Libraries / chemistry*

Substances

Antineoplastic Agents
Biological Products
Integrins
Oligopeptides
Small Molecule Libraries
arginyl-glycyl-aspartic acid