1uk0
From Proteopedia
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| - | [[Image:1uk0.gif|left|200px]] | + | [[Image:1uk0.gif|left|200px]] |
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| - | '''Crystal structure of catalytic domain of human poly(ADP-ribose) polymerase with a novel inhibitor''' | + | {{Structure |
| + | |PDB= 1uk0 |SIZE=350|CAPTION= <scene name='initialview01'>1uk0</scene>, resolution 3.Å | ||
| + | |SITE= | ||
| + | |LIGAND= <scene name='pdbligand=FRM:2-{3-[4-(4-FLUOROPHENYL)-3,6-DIHYDRO-1(2H)-PYRIDINYL]PROPYL}-8-METHYL-4(3H)-QUINAZOLINONE'>FRM</scene> | ||
| + | |ACTIVITY= [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] | ||
| + | |GENE= | ||
| + | }} | ||
| + | |||
| + | '''Crystal structure of catalytic domain of human poly(ADP-ribose) polymerase with a novel inhibitor''' | ||
| + | |||
==Overview== | ==Overview== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1UK0 is a [ | + | 1UK0 is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1UK0 OCA]. |
==Reference== | ==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:[http:// | + | 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]] | ||
[[Category: NAD(+) ADP-ribosyltransferase]] | [[Category: NAD(+) ADP-ribosyltransferase]] | ||
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[[Category: protein-inhibitor complex]] | [[Category: protein-inhibitor complex]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 14:32:57 2008'' |
Revision as of 12:32, 20 March 2008
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| , resolution 3.Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | |||||||
| Activity: | NAD(+) ADP-ribosyltransferase, with EC number 2.4.2.30 | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
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. 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 Thu Mar 20 14:32:57 2008
