Document Detail

Discovery of novel Myc-Max heterodimer disruptors with a three-dimensional pharmacophore model.
MedLine Citation:
PMID:  19215087     Owner:  NLM     Status:  MEDLINE    
A three-dimensional pharmacophore model was generated utilizing a set of known inhibitors of c-Myc-Max heterodimer formation. The model successfully identified a set of structurally diverse compounds with potential inhibitory activity against c-Myc. Nine compounds were tested in vitro, and four displayed affinities in the micromolar range and growth inhibitory activity against c-Myc-overexpressing cells. These studies demonstrate the applicability of pharmacophore modeling to the identification of novel and potentially more puissant inhibitors of the c-Myc oncoprotein.
Gabriela Mustata; Ariele Viacava Follis; Dalia I Hammoudeh; Steven J Metallo; Huabo Wang; Edward V Prochownik; John S Lazo; Ivet Bahar
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural    
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  52     ISSN:  1520-4804     ISO Abbreviation:  J. Med. Chem.     Publication Date:  2009 Mar 
Date Detail:
Created Date:  2009-10-21     Completed Date:  2010-06-29     Revised Date:  2013-06-02    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  1247-50     Citation Subset:  IM    
Department of Computational Biology, University of Pittsburgh, Pittsburgh, Pennsylvania 15260, USA.
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MeSH Terms
Basic Helix-Loop-Helix Leucine Zipper Transcription Factors / chemistry*,  metabolism
Benzofurans / chemistry,  pharmacology
Cell Line
Cell Proliferation / drug effects
Circular Dichroism
Electrophoretic Mobility Shift Assay
Fibroblasts / cytology,  drug effects,  metabolism
Gene Knockout Techniques
HL-60 Cells
HMGA1b Protein / biosynthesis,  genetics
Models, Molecular*
Protein Binding
Protein Multimerization
Proto-Oncogene Proteins c-myc / chemistry*,  genetics,  metabolism
Pyridines / chemistry,  pharmacology
Pyrrolidines / chemistry,  pharmacology
Thiazoles / chemistry,  pharmacology
Grant Support
1U54MK074411//PHS HHS; U54 MH074411-02/MH/NIMH NIH HHS
Reg. No./Substance:
0/Basic Helix-Loop-Helix Leucine Zipper Transcription Factors; 0/Benzofurans; 0/Proto-Oncogene Proteins c-myc; 0/Pyridines; 0/Pyrrolidines; 0/Thiazoles; 124543-08-4/HMGA1b Protein

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