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1vzk

From Proteopedia

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[[Image:1vzk.gif|left|200px]]
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{{Seed}}
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[[Image:1vzk.png|left|200px]]
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{{STRUCTURE_1vzk| PDB=1vzk | SCENE= }}
{{STRUCTURE_1vzk| PDB=1vzk | SCENE= }}
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'''A THIOPHENE BASED DIAMIDINE FORMS A "SUPER" AT BINDING MINOR GROOVE AGENT'''
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===A THIOPHENE BASED DIAMIDINE FORMS A "SUPER" AT BINDING MINOR GROOVE AGENT===
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==Overview==
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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 increase in affinity. X-ray results indicate a small bond angle difference between the C-S-C angle of thiophene and the C-O-C angle of furan that, when amplified out to the terminal amidines of the benzimidazole compounds, yields a very significant difference in the positions of the amidines and their DNA interaction strength.
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The line below this paragraph, {{ABSTRACT_PUBMED_15493923}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 15493923 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15493923}}
==About this Structure==
==About this Structure==
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[[Category: Minor groove binder]]
[[Category: Minor groove binder]]
[[Category: Nucleic acid]]
[[Category: Nucleic acid]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 12:57:24 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 15:36:00 2008''

Revision as of 12:36, 28 July 2008

Image:1vzk.png

Template:STRUCTURE 1vzk

A THIOPHENE BASED DIAMIDINE FORMS A "SUPER" AT BINDING MINOR GROOVE AGENT

Template:ABSTRACT PUBMED 15493923

About this Structure

1VZK is a Single protein structure. 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

Page seeded by OCA on Mon Jul 28 15:36:00 2008

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