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 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

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phosphorylation
Phosphorylation
tyrosine
Platelet-Derived Growth Factor
platelets
Libraries
Tyrosine
Tumors
tumors
Platelet-Derived Growth Factor Receptors
Neoplasms
Alkylation
Growth
Starvation
Scaffolds
Head
angiogenesis
alkylation
calix(4)arene
rims

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Chemistry(all)

Cite this

Structure-activity studies on a library of potent calix[4]arene-based PDGF antagonists that inhibit PDGF-stimulated PDGFR tyrosine phosphorylation. / Zhou, Huchen; Wang, De An; Baldini, Laura; Ennis, Eileen; Jain, Rishi; Carie, Adam; Sebti, Saïd M.; Hamilton, Andrew.

In: Organic and Biomolecular Chemistry, Vol. 4, No. 12, 2006, p. 2376-2386.

Research output: Contribution to journalArticle

Zhou, Huchen ; Wang, De An ; Baldini, Laura ; Ennis, Eileen ; Jain, Rishi ; Carie, Adam ; Sebti, Saïd M. ; Hamilton, Andrew. / Structure-activity studies on a library of potent calix[4]arene-based PDGF antagonists that inhibit PDGF-stimulated PDGFR tyrosine phosphorylation. In: Organic and Biomolecular Chemistry. 2006 ; Vol. 4, No. 12. pp. 2376-2386.
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