Design of Inhibitors for S100B

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

Journal Name: Current Topics in Medicinal Chemistry

Volume 5 , Issue 12 , 2005

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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

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Article Details

VOLUME: 5
ISSUE: 12
Year: 2005
Page: [1093 - 1108]
Pages: 16
DOI: 10.2174/156802605774370865
Price: $58

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