Design of Inhibitors for S100B

Title: Design of Inhibitors for S100B

Volume: 5 Issue: 12

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

Affiliation:

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

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.

Cite this article as:

Markowitz Joseph, MacKerell Jr. D. Alexander, Carrier France, Charpentier H. Thomas and Weber J. David, Design of Inhibitors for S100B, Current Topics in Medicinal Chemistry 2005; 5 (12) . https://dx.doi.org/10.2174/156802605774370865