An integrin-targeted photoactivatable Pt(IV) complex as a selective anticancer pro-drug: synthesis and photoactivation studies

Chem Commun (Camb). 2015 Jun 4;51(44):9169-72. doi: 10.1039/c5cc03180j.

Abstract

A new anticancer agent based on the conjugation of a photoactivatable Pt(IV) pro-drug to a cyclic RGD-containing peptide is described. Upon visible light irradiation, phototoxicity was induced preferentially in SK-MEL-28 melanoma cancer cells overexpressing αVβ3 integrin compared to control DU-145 human prostate carcinoma cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents* / chemistry
  • Antineoplastic Agents* / pharmacology
  • Antineoplastic Agents* / radiation effects
  • Cell Line, Tumor
  • Humans
  • Integrin alphaVbeta3 / metabolism*
  • Light
  • Organoplatinum Compounds* / chemistry
  • Organoplatinum Compounds* / pharmacology
  • Organoplatinum Compounds* / radiation effects
  • Peptides, Cyclic* / chemistry
  • Peptides, Cyclic* / pharmacology
  • Peptides, Cyclic* / radiation effects
  • Platinum / metabolism
  • Prodrugs* / chemistry
  • Prodrugs* / pharmacology
  • Prodrugs* / radiation effects
  • Receptors, Vitronectin / metabolism

Substances

  • Antineoplastic Agents
  • Integrin alphaVbeta3
  • Organoplatinum Compounds
  • Peptides, Cyclic
  • Prodrugs
  • Receptors, Vitronectin
  • integrin alphaVbeta5
  • Platinum