1uk0

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[[Image:1uk0.gif|left|200px]]
[[Image:1uk0.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1uk0 |SIZE=350|CAPTION= <scene name='initialview01'>1uk0</scene>, resolution 3.&Aring;
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The line below this paragraph, containing "STRUCTURE_1uk0", 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=FRM:2-{3-[4-(4-FLUOROPHENYL)-3,6-DIHYDRO-1(2H)-PYRIDINYL]PROPYL}-8-METHYL-4(3H)-QUINAZOLINONE'>FRM</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= <span class='plainlinks'>[http://en.wikipedia.org/wiki/NAD(+)_ADP-ribosyltransferase NAD(+) ADP-ribosyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.4.2.30 2.4.2.30] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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|DOMAIN=
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{{STRUCTURE_1uk0| PDB=1uk0 | SCENE= }}
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|RELATEDENTRY=[[1uk1|1UK1]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1uk0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1uk0 OCA], [http://www.ebi.ac.uk/pdbsum/1uk0 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1uk0 RCSB]</span>
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}}
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'''Crystal structure of catalytic domain of human poly(ADP-ribose) polymerase with a novel inhibitor'''
'''Crystal structure of catalytic domain of human poly(ADP-ribose) polymerase with a novel inhibitor'''
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Inhibitor-induced structural change of the active site of human poly(ADP-ribose) polymerase., Kinoshita T, Nakanishi I, Warizaya M, Iwashita A, Kido Y, Hattori K, Fujii T, FEBS Lett. 2004 Jan 2;556(1-3):43-6. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/14706823 14706823]
Inhibitor-induced structural change of the active site of human poly(ADP-ribose) polymerase., Kinoshita T, Nakanishi I, Warizaya M, Iwashita A, Kido Y, Hattori K, Fujii T, FEBS Lett. 2004 Jan 2;556(1-3):43-6. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/14706823 14706823]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: NAD(+) ADP-ribosyltransferase]]
 
[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Kinoshita, T.]]
[[Category: Kinoshita, T.]]
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[[Category: protein-inhibitor complex]]
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[[Category: Protein-inhibitor complex]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 11:19:52 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 00:11:16 2008''
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Revision as of 08:19, 3 May 2008

Image:1uk0.gif

Template:STRUCTURE 1uk0

Crystal structure of catalytic domain of human poly(ADP-ribose) polymerase with a novel inhibitor


Overview

The crystal structure of human recombinant poly(ADP-ribose) polymerase (PARP) complexed with a potent inhibitor, FR257517, was solved at 3.0 A resolution. The fluorophenyl part of the inhibitor induces an amazing conformational change in the active site of PARP by motion of the side chain of the amino acid, Arg878, which forms the bottom of the active site. Consequently, a corn-shaped hydrophobic subsite, which consists of the side chains of Leu769, Ile879, Pro881, and the methylene chain of Arg878, newly emerges from the well-known active site.

About this Structure

1UK0 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Inhibitor-induced structural change of the active site of human poly(ADP-ribose) polymerase., Kinoshita T, Nakanishi I, Warizaya M, Iwashita A, Kido Y, Hattori K, Fujii T, FEBS Lett. 2004 Jan 2;556(1-3):43-6. PMID:14706823 Page seeded by OCA on Sat May 3 11:19:52 2008

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