Document Detail


In vivo screening of S100B inhibitors for melanoma therapy.
MedLine Citation:
PMID:  23296618     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Danna B Zimmer; Rena G Lapidus; David J Weber
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Methods in molecular biology (Clifton, N.J.)     Volume:  963     ISSN:  1940-6029     ISO Abbreviation:  Methods Mol. Biol.     Publication Date:  2013  
Date Detail:
Created Date:  2013-01-08     Completed Date:  2013-06-11     Revised Date:  2013-07-25    
Medline Journal Info:
Nlm Unique ID:  9214969     Medline TA:  Methods Mol Biol     Country:  United States    
Other Details:
Languages:  eng     Pagination:  303-17     Citation Subset:  IM    
Affiliation:
Department of Biochemistry and Molecular Biology, Center for Biomolecular Therapeutics, The University of Maryland School of Medicine, Baltimore, MD, USA. dzimmer@som.umaryland.edu
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MeSH Terms
Descriptor/Qualifier:
Animals
Antineoplastic Agents / adverse effects,  pharmacokinetics,  pharmacology*,  therapeutic use
Drug Screening Assays, Antitumor / methods*
Male
Maximum Tolerated Dose
Melanoma / drug therapy*
Mice
Nerve Growth Factors / antagonists & inhibitors*
S100 Proteins / antagonists & inhibitors*
Grant Support
ID/Acronym/Agency:
CA107331/CA/NCI NIH HHS; R01 CA107331/CA/NCI NIH HHS; R01 GM058888/GM/NIGMS NIH HHS; S10 RR016812/RR/NCRR NIH HHS; S10 RR023447/RR/NCRR NIH HHS; S10 RR029601/RR/NCRR NIH HHS; S10 RR031729/RR/NCRR NIH HHS
Chemical
Reg. No./Substance:
0/Antineoplastic Agents; 0/Nerve Growth Factors; 0/S-100 calcium-binding protein beta subunit; 0/S100 Proteins
Comments/Corrections

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