1vzk

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(New page: 200px<br /> <applet load="1vzk" size="450" color="white" frame="true" align="right" spinBox="true" caption="1vzk, resolution 1.77&Aring;" /> '''A THIOPHENE BASED D...)
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==About this Structure==
==About this Structure==
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1VZK is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/ ]] with MG and D1B as [[http://en.wikipedia.org/wiki/ligands ligands]]. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1VZK OCA]].
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1VZK is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/ ]] with MG and D1B as [[http://en.wikipedia.org/wiki/ligands ligands]]. Structure known Active Site: AC1. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1VZK OCA]].
==Reference==
==Reference==
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[[Category: nucleic acids]]
[[Category: nucleic acids]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Oct 29 21:44:49 2007''
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 14:14:34 2007''

Revision as of 12:09, 30 October 2007


1vzk, resolution 1.77Å

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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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