In vivo screening of S100B inhibitors for melanoma therapy.

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TitleIn vivo screening of S100B inhibitors for melanoma therapy.
Publication TypeJournal Article
Year of Publication2013
AuthorsZimmer, DB, Lapidus, RG, Weber, DJ
JournalMethods Mol Biol
Volume963
Pagination303-17
Date Published07/2013
ISSN1940-6029
KeywordsAnimals, Antineoplastic Agents, Drug Screening Assays, Antitumor, Male, Maximum Tolerated Dose, Melanoma, Mice, Nerve Growth Factors, S100 Proteins
Abstract

S100 proteins are markers for numerous cancers, and in many cases high S100 protein levels are a prognostic indicator for poor survival. One such case is S100B, which is overproduced in a very large percentage of malignant melanoma cases. Elevated S100B protein was more recently validated to have causative effects towards cancer progression via down-regulating the tumor suppressor protein, p53. Towards eliminating this problem in melanoma, targeting S100B with small molecule inhibitors was initiated. This work relies on numerous chemical biology technologies including structural biology, computer-aided drug design, compound screening, and medicinal chemistry approaches. Another important component of drug development is the ability to test compounds and various molecular scaffolds for their efficacy in vivo. This chapter briefly describes the development of S100B inhibitors, termed SBiXs, for melanoma therapy with a focus on the inclusion of in vivo screening at an early stage in the drug discovery process.

DOI10.1007/978-1-62703-230-8_18
Alternate JournalMethods Mol. Biol.
PubMed ID23296618
PubMed Central IDPMC3718549
Grant ListCA107331 / CA / NCI NIH HHS / United States
R01 CA107331 / CA / NCI NIH HHS / United States
R01 GM058888 / GM / NIGMS NIH HHS / United States
S10 RR016812 / RR / NCRR NIH HHS / United States
S10 RR023447 / RR / NCRR NIH HHS / United States
S10 RR029601 / RR / NCRR NIH HHS / United States
S10 RR031729 / RR / NCRR NIH HHS / United States