1uk0
From Proteopedia
(New page: 200px<br /> <applet load="1uk0" size="450" color="white" frame="true" align="right" spinBox="true" caption="1uk0, resolution 3.Å" /> '''Crystal structure of ...) |
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caption="1uk0, resolution 3.Å" /> | caption="1uk0, resolution 3.Å" /> | ||
'''Crystal structure of catalytic domain of human poly(ADP-ribose) polymerase with a novel inhibitor'''<br /> | '''Crystal structure of catalytic domain of human poly(ADP-ribose) polymerase with a novel inhibitor'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1UK0 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with FRM as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [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] Full crystallographic information is available from [http:// | + | 1UK0 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=FRM:'>FRM</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [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] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1UK0 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: protein-inhibitor complex]] | [[Category: protein-inhibitor complex]] | ||
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Revision as of 15:02, 15 February 2008
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Crystal structure of catalytic domain of human poly(ADP-ribose) polymerase with a novel inhibitor
Contents |
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.
Disease
Known diseases associated with this structure: Xeroderma pigmentosum (1) OMIM:[173870]
About this Structure
1UK0 is a Single protein structure of sequence from Homo sapiens with as ligand. Active as NAD(+) ADP-ribosyltransferase, with EC number 2.4.2.30 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
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