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1uk1

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[[Image:1uk1.gif|left|200px]]
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{{STRUCTURE_1uk1| PDB=1uk1 | SCENE= }}
{{STRUCTURE_1uk1| PDB=1uk1 | SCENE= }}
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'''Crystal structure of human poly(ADP-ribose) polymerase complexed with a potent inhibitor'''
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===Crystal structure of human poly(ADP-ribose) polymerase complexed with a potent inhibitor===
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==Overview==
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A novel class of quinazolinone derivatives as potent poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors has been discovered. Key to success was application of a rational discovery strategy involving structure-based design, combinatorial chemistry, and classical SAR for improvement of potency and bioavailability. The new inhibitors were shown to bind to the nicotinamide-ribose binding site (NI site) and the adenosine-ribose binding site (AD site) of NAD+.
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(as it appears on PubMed at http://www.pubmed.gov), where 15293985 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15293985}}
==About this Structure==
==About this Structure==
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[[Category: Kinoshita, T.]]
[[Category: Kinoshita, T.]]
[[Category: Protein-inhibitor complex]]
[[Category: Protein-inhibitor complex]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 11:20:01 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 22:14:41 2008''

Revision as of 19:14, 28 July 2008

Image:1uk1.png

Template:STRUCTURE 1uk1

Crystal structure of human poly(ADP-ribose) polymerase complexed with a potent inhibitor

Template:ABSTRACT PUBMED 15293985

About this Structure

1UK1 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Rational approaches to discovery of orally active and brain-penetrable quinazolinone inhibitors of poly(ADP-ribose)polymerase., Hattori K, Kido Y, Yamamoto H, Ishida J, Kamijo K, Murano K, Ohkubo M, Kinoshita T, Iwashita A, Mihara K, Yamazaki S, Matsuoka N, Teramura Y, Miyake H, J Med Chem. 2004 Aug 12;47(17):4151-4. PMID:15293985

Page seeded by OCA on Mon Jul 28 22:14:41 2008

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