Design of Inhibitors for S100B.

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TitleDesign of Inhibitors for S100B.
Publication TypeJournal Article
Year of Publication2005
AuthorsMarkowitz, J, Mackerell, AD, Carrier, F, Charpentier, TH, Weber, DJ
JournalCurr Top Med Chem
Volume5
Issue12
Pagination1093-108
Date Published2005
ISSN1568-0266
KeywordsBiomarkers, Tumor, Calcium, Computer-Aided Design, Drug Design, Female, Humans, Magnetic Resonance Spectroscopy, Male, Molecular Structure, Nerve Growth Factors, S100 Calcium Binding Protein beta Subunit, S100 Proteins, Solubility, Spectrometry, Fluorescence, Tumor Suppressor Protein p53
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.

Alternate JournalCurr Top Med Chem
PubMed ID16248785
Grant ListS10 RR016812 / RR / NCRR NIH HHS / United States
GM58888 / GM / NIGMS NIH HHS / United States
F30-NS043916 / NS / NINDS NIH HHS / United States
S10 RR015741 / RR / NCRR NIH HHS / United States
R01 GM058888 / GM / NIGMS NIH HHS / United States