Structure-activity studies on a library of potent calix[4]arene-based PDGF antagonists that inhibit PDGF-stimulated PDGFR tyrosine phosphorylation

Huchen Zhou, De An Wang, Laura Baldini, Eileen Ennis, Rishi Jain, Adam Carie, Saïd M. Sebti, Andrew D. Hamilton

Research output: Contribution to journalArticle

Abstract

Platelet-derived growth factor (PDGF) and its receptor PDGFR are required for tumor growth and angiogenesis, so disruption of the PDGF-PDGFR interaction should lead to starvation of tumors and reduction of tumor growth. Potent PDGF antagonists have been discovered through the synthesis of a series of calix[4]arene-based compounds that are designed to bind to the three-loop region of PDGF. The effect of lower-rim alkylation, linker and number of interacting head groups on the calix[4]arene scaffold on PDGF affinity and cellular activity has been investigated.

Original languageEnglish (US)
Pages (from-to)2376-2386
Number of pages11
JournalOrganic and Biomolecular Chemistry
Volume4
Issue number12
DOIs
StatePublished - 2006

ASJC Scopus subject areas

  • Biochemistry
  • Physical and Theoretical Chemistry
  • Organic Chemistry

Fingerprint Dive into the research topics of 'Structure-activity studies on a library of potent calix[4]arene-based PDGF antagonists that inhibit PDGF-stimulated PDGFR tyrosine phosphorylation'. Together they form a unique fingerprint.

  • Cite this