Issue 12, 2006
From the journal:

Organic & Biomolecular Chemistry

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

Huchen Zhou,a   De-an Wang,bc   Laura Baldini,a   Eileen Ennis,a   Rishi Jain,a   Adam Carie,bc   Saïd M. Sebti*bc  and  Andrew D. Hamilton*a  

* Corresponding authors

a Department of Chemistry, Yale University, New Haven, CT 06520, USA
E-mail: Andrew.Hamilton@yale.edu
Fax: +1 203 432 3221
Tel: +1 203 432 5570

b Drug Discovery Program, H. Lee Moffitt Cancer Center & Research Institute, Tampa, FL, USA
E-mail: Sebti@moffitt.usf.edu
Fax: +1 813 979 6748
Tel: +1 813 979 6734

c Departments of Interdisciplinary Oncology and Biochemistry & Molecular Biology, H. Lee Moffitt Cancer Center & Research Institute, Tampa, FL, USA

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.

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

About
Cited by
Related
Download options Please wait...

Article information

DOI
https://doi.org/10.1039/B515483A
Article type
Paper
Submitted
01 Nov 2005
Accepted
21 Mar 2006
First published
10 May 2006

Org. Biomol. Chem., 2006,4, 2376-2386

Permissions

Request permissions

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

H. Zhou, D. Wang, L. Baldini, E. Ennis, R. Jain, A. Carie, S. M. Sebti and A. D. Hamilton, Org. Biomol. Chem., 2006, 4, 2376 DOI: 10.1039/B515483A

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Social activity

Spotlight

Advertisements