Design of Inhibitors for S100B
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: computer-aided drug design; cyclin-dependent kinase inhibitor; epitope mapping; fluorescence spectroscopy; melanoma; p53 tumor suppressor protein; std-nmr
Document Type: Review Article
Affiliations: Dept. of Biochemistry and Molecular Biology, University of Maryland School of Medicine, 108 N. Greene St., Baltimore, MD 21201.
Publication date: 01 October 2005
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