Generic placeholder image

Current Topics in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Design of Inhibitors for S100B

Author(s): Joseph Markowitz, Alexander D. MacKerell Jr., France Carrier, Thomas H. Charpentier and David J. Weber

Volume 5, Issue 12, 2005

Page: [1093 - 1108] Pages: 16

DOI: 10.2174/156802605774370865

Price: $65

Abstract

S100B interacts with the p53 protein in a calcium-dependent manner and down-regulates its function as a tumor suppressor. Therefore, inhibiting the S100B-p53 interaction represents a new approach for restoring functional wild-type p53 in cancers with elevated S100B such as found in malignant melanoma. A discussion of the biological rational for targeting S100B and a description of methodologies relevant to the discovery of compounds that inhibit S100B-p53 binding, including computational techniques, structural biology techniques, and cellular assays, is presented.

Keywords: melanoma, p53 tumor suppressor protein, cyclin-dependent kinase inhibitor, epitope mapping, computer-aided drug design, fluorescence spectroscopy, std-nmr


Rights & Permissions Print Cite
© 2024 Bentham Science Publishers | Privacy Policy