1vzk
From Proteopedia
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Revision as of 14:15, 30 October 2007
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A THIOPHENE BASED DIAMIDINE FORMS A "SUPER" AT BINDING MINOR GROOVE AGENT
Overview
The DNA minor groove is the interaction site for many enzymes and, transcription control proteins and as a result, development of compounds, that target the minor groove is an active research area. In an effort to, develop biologically active minor groove agents, we are preparing and, exploring the DNA interactions of a systematic set of diamidine, derivatives with a powerful array of methods including DNase I, footprinting, biosensor-SPR methods, and X-ray crystallography., Surprisingly, conversion of the parent phenyl-furan-phenyl diamidine to a, phenyl-thiophene-benzimidazole derivative yields a compound with over, 10-fold-increased affinity for the minor groove at AT sequences. Single, conversion of the furan to a thiophene or a phenyl to benzimidazole does, not cause a similar ... [(full description)]
About this Structure
1VZK is a [Single protein] structure of sequence from [[1]] with MG and D1B as [ligands]. Structure known Active Site: AC1. Full crystallographic information is available from [OCA].
Reference
Thiophene-based diamidine forms a "super" at binding minor groove agent., Mallena S, Lee MP, Bailly C, Neidle S, Kumar A, Boykin DW, Wilson WD, J Am Chem Soc. 2004 Oct 27;126(42):13659-69. PMID:15493923
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