2hxm

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[[Image:2hxm.gif|left|200px]]
[[Image:2hxm.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2hxm |SIZE=350|CAPTION= <scene name='initialview01'>2hxm</scene>, resolution 1.30&Aring;
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The line below this paragraph, containing "STRUCTURE_2hxm", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=302:4-[(1E,7E)-8-(2,6-DIOXO-1,2,3,6-TETRAHYDROPYRIMIDIN-4-YL)-3,6-DIOXA-2,7-DIAZAOCTA-1,7-DIEN-1-YL]BENZOIC+ACID'>302</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY=
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or leave the SCENE parameter empty for the default display.
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|GENE= UNG, DGU, UNG15 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_2hxm| PDB=2hxm | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2hxm FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2hxm OCA], [http://www.ebi.ac.uk/pdbsum/2hxm PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2hxm RCSB]</span>
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}}
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'''Complex of UNG2 and a small Molecule synthetic Inhibitor'''
'''Complex of UNG2 and a small Molecule synthetic Inhibitor'''
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[[Category: Seiple, L.]]
[[Category: Seiple, L.]]
[[Category: Stivers,J T.]]
[[Category: Stivers,J T.]]
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[[Category: dna repair]]
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[[Category: Dna repair]]
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[[Category: uracil]]
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[[Category: Uracil]]
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[[Category: uracil dna glycosylase]]
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[[Category: Uracil dna glycosylase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 06:50:16 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:36:53 2008''
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Revision as of 03:50, 4 May 2008

Image:2hxm.gif

Template:STRUCTURE 2hxm

Complex of UNG2 and a small Molecule synthetic Inhibitor


Overview

Human nuclear uracil DNA glycosylase (UNG2) is a cellular DNA repair enzyme that is essential for a number of diverse biological phenomena ranging from antibody diversification to B-cell lymphomas and type-1 human immunodeficiency virus infectivity. During each of these processes, UNG2 recognizes uracilated DNA and excises the uracil base by flipping it into the enzyme active site. We have taken advantage of the extrahelical uracil recognition mechanism to build large small-molecule libraries in which uracil is tethered via flexible alkane linkers to a collection of secondary binding elements. This high-throughput synthesis and screening approach produced two novel uracil-tethered inhibitors of UNG2, the best of which was crystallized with the enzyme. Remarkably, this inhibitor mimics the crucial hydrogen bonding and electrostatic interactions previously observed in UNG2 complexes with damaged uracilated DNA. Thus, the environment of the binding site selects for library ligands that share these DNA features. This is a general approach to rapid discovery of inhibitors of enzymes that recognize extrahelical damaged bases.

About this Structure

2HXM is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Mimicking damaged DNA with a small molecule inhibitor of human UNG2., Krosky DJ, Bianchet MA, Seiple L, Chung S, Amzel LM, Stivers JT, Nucleic Acids Res. 2006;34(20):5872-9. Epub 2006 Oct 24. PMID:17062624 Page seeded by OCA on Sun May 4 06:50:16 2008

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