Document Detail


Binding of f-PIP, a pyrrole- and imidazole-containing triamide, to the inverted CCAAT box-2 of the topoisomerase IIalpha promoter and modulation of gene expression in cells.
MedLine Citation:
PMID:  17011187     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
An N-formamido pyrrole- and imidazole-containing triamide (f-PIP) has been shown by DNase I footprinting, SPR, and CD studies to bind as a stacked dimer to its cognate sequences: 5'-TACGAT-3' (5'-flank of the inverted CCAAT box-2 of the human topoisomerase IIalpha promoter) and 5'-ATCGAT-3'. A gel shift experiment provided evidence for f-PIP to inhibit protein-DNA interaction at the ICB2 site. Western blot studies showed that expression of the topoisomerase IIalpha gene in confluent NIH 3T3 cells was induced by treatment with f-PIP. The results suggested that the triamide was able to enter the nucleus, interacted with the target site within ICB2, inhibited NF-Y binding, and activated gene expression.
Authors:
N Minh Le; Alan M Sielaff; Amanda J Cooper; Hilary Mackay; Toni Brown; Minal Kotecha; Caroline O'Hare; Daniel Hochhauser; Moses Lee; John A Hartley
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.     Date:  2006-09-29
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  16     ISSN:  0960-894X     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2006 Dec 
Date Detail:
Created Date:  2006-11-19     Completed Date:  2007-02-16     Revised Date:  2014-02-19    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  6161-4     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
3T3 Cells
Animals
Base Sequence
Circular Dichroism
DNA Footprinting
DNA Topoisomerases, Type II / genetics*
Deoxyribonuclease I
Distamycins / pharmacokinetics*
Gene Expression Regulation, Neoplastic*
Imidazoles / pharmacokinetics*
Mice
Promoter Regions, Genetic*
Pyrroles / pharmacokinetics*
Grant Support
ID/Acronym/Agency:
G0000168//Medical Research Council
Chemical
Reg. No./Substance:
0/Distamycins; 0/Imidazoles; 0/N-(2-(diethylamino)ethyl)-1-methyl-4-(1-methyl-4-(4-formamido-1-methylimidazole-2-carboxamido)pyrrole-2-carboxamido)imidazole-2-carboxamide; 0/Pyrroles; EC 3.1.21.1/Deoxyribonuclease I; EC 5.99.1.3/DNA Topoisomerases, Type II

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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