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1uk0

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1uk0, resolution 3.00Å ()
Ligands:
Activity: NAD(+) ADP-ribosyltransferase, with EC number 2.4.2.30
Domains: parp_like
Related: 1uk1
Resources: FirstGlance, OCA, PDBsum, RCSB
Coordinates: save as pdb, mmCIF, xml



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

Publication Abstract from PubMed

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.

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

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

About this Structure

1UK0 is a 2 chains structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.

Reference

  • Kinoshita T, Nakanishi I, Warizaya M, Iwashita A, Kido Y, Hattori K, Fujii T. Inhibitor-induced structural change of the active site of human poly(ADP-ribose) polymerase. FEBS Lett. 2004 Jan 2;556(1-3):43-6. PMID:14706823

Page seeded by OCA on Wed Feb 18 08:26:46 2009

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