4pax

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[[Image:4pax.gif|left|200px]]
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{{Seed}}
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{{STRUCTURE_4pax| PDB=4pax | SCENE= }}
{{STRUCTURE_4pax| PDB=4pax | SCENE= }}
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'''THE CATALYTIC FRAGMENT OF POLY(ADP-RIBOSE) POLYMERASE COMPLEXED WITH 8-HYDROXY-2-METHYL-3-HYDRO-QUINAZOLIN-4-ONE'''
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===THE CATALYTIC FRAGMENT OF POLY(ADP-RIBOSE) POLYMERASE COMPLEXED WITH 8-HYDROXY-2-METHYL-3-HYDRO-QUINAZOLIN-4-ONE===
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==Overview==
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Inhibitors of poly(ADP-ribose) polymerase (PARP, EC 2.4.2.30) are of clinical interest because they have potential for improving radiation therapy and chemotherapy of cancer. The refined binding structures of four such inhibitors are reported together with the refined structure of the unligated catalytic fragment of the enzyme. Following their design, all inhibitors bind at the position of the nicotinamide moiety of the substrate NAD+. The observed binding mode suggests inhibitor improvements that avoid other NAD(+)-binding enzymes. Because the binding pocket of NAD+ has been strongly conserved during evolution, the homology with ADP-ribosylating bacterial toxins could be used to extend the bound nicotinamide, which is marked by the inhibitors, to the full NAD+ molecule.
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(as it appears on PubMed at http://www.pubmed.gov), where 9521710 is the PubMed ID number.
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{{ABSTRACT_PUBMED_9521710}}
==About this Structure==
==About this Structure==
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[[Category: Glycosyltransferase]]
[[Category: Glycosyltransferase]]
[[Category: Transferase]]
[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 22:27:46 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Jul 3 13:46:27 2008''

Revision as of 10:46, 3 July 2008

Image:4pax.png

Template:STRUCTURE 4pax

THE CATALYTIC FRAGMENT OF POLY(ADP-RIBOSE) POLYMERASE COMPLEXED WITH 8-HYDROXY-2-METHYL-3-HYDRO-QUINAZOLIN-4-ONE

Template:ABSTRACT PUBMED 9521710

About this Structure

4PAX is a Single protein structure of sequence from Gallus gallus. Full crystallographic information is available from OCA.

Reference

Inhibitor and NAD+ binding to poly(ADP-ribose) polymerase as derived from crystal structures and homology modeling., Ruf A, de Murcia G, Schulz GE, Biochemistry. 1998 Mar 17;37(11):3893-900. PMID:9521710

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