Rational design of RGD-albumin conjugates for targeted delivery of the VEGF-R kinase inhibitor PTK787 to angiogenic endothelium

Kai Temming, Marie Lacombe, Roel Q.J. Schaapveld, László Orfi, Gyorgy Kéri, Klaas Poelstra, Grietje Molema, Robbert J. Kok

Research output: Contribution to journalArticle

28 Citations (Scopus)

Abstract

Linking the unlinkable: Many new chemical entities lack reactive groups for use in the formation of reversible bonds, for example, to conjugate them for targeted drug delivery purposes. We succeeded with the noncovalent coupling of a potent signal transduction inhibitor to a protein backbone by applying the platinum-based universal linkage system. The resulting drug-targeting conjugates offer new potential for cancer treatment with minimal side effects.

Original languageEnglish
Pages (from-to)1200-1203
Number of pages4
JournalChemMedChem
Volume1
Issue number11
DOIs
Publication statusPublished - Nov 1 2006

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Keywords

  • Platinum
  • Prodrugs
  • Protein modifications
  • Signal transduction
  • Targeting

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Drug Discovery
  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Organic Chemistry

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