1uou

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[[Image:1uou.gif|left|200px]]
[[Image:1uou.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1uou |SIZE=350|CAPTION= <scene name='initialview01'>1uou</scene>, resolution 2.11&Aring;
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The line below this paragraph, containing "STRUCTURE_1uou", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:Cmu+Binding+Site+For+Chain+A'>AC1</scene>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=CMU:5-CHLORO-6-(1-(2-IMINOPYRROLIDINYL)+METHYL)+URACIL'>CMU</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Thymidine_phosphorylase Thymidine phosphorylase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.4.2.4 2.4.2.4] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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-->
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|DOMAIN=
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{{STRUCTURE_1uou| PDB=1uou | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1uou FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1uou OCA], [http://www.ebi.ac.uk/pdbsum/1uou PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1uou RCSB]</span>
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}}
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'''CRYSTAL STRUCTURE OF HUMAN THYMIDINE PHOSPHORYLASE IN COMPLEX WITH A SMALL MOLECULE INHIBITOR'''
'''CRYSTAL STRUCTURE OF HUMAN THYMIDINE PHOSPHORYLASE IN COMPLEX WITH A SMALL MOLECULE INHIBITOR'''
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[[Category: Timms, D.]]
[[Category: Timms, D.]]
[[Category: Tucker, J A.]]
[[Category: Tucker, J A.]]
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[[Category: angiogenesis]]
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[[Category: Angiogenesis]]
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[[Category: chemotaxis]]
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[[Category: Chemotaxis]]
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[[Category: glycosyltransferase]]
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[[Category: Glycosyltransferase]]
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[[Category: phosphorylase]]
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[[Category: Phosphorylase]]
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[[Category: transferase]]
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[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 11:30:46 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 00:13:14 2008''
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Revision as of 08:30, 3 May 2008

Image:1uou.gif

Template:STRUCTURE 1uou

CRYSTAL STRUCTURE OF HUMAN THYMIDINE PHOSPHORYLASE IN COMPLEX WITH A SMALL MOLECULE INHIBITOR


Overview

Human thymidine phosphorylase (HTP), also known as platelet-derived endothelial cell growth factor (PD-ECGF), is overexpressed in certain solid tumors where it is linked to poor prognosis. HTP expression is utilized for certain chemotherapeutic strategies and is also thought to play a role in tumor angiogenesis. We determined the structure of HTP bound to the small molecule inhibitor 5-chloro-6-[1-(2-iminopyrrolidinyl) methyl] uracil hydrochloride (TPI). The inhibitor appears to mimic the substrate transition state, which may help explain the potency of this inhibitor and the catalytic mechanism of pyrimidine nucleotide phosphorylases (PYNPs). Further, we have confirmed the validity of the HTP structure as a template for structure-based drug design by predicting binding affinities for TPI and other known HTP inhibitors using in silico docking techniques. This work provides the first structural insight into the binding mode of any inhibitor to this important drug target and forms the basis for designing novel inhibitors for use in anticancer therapy.

About this Structure

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

Reference

Crystal structure of human thymidine phosphorylase in complex with a small molecule inhibitor., Norman RA, Barry ST, Bate M, Breed J, Colls JG, Ernill RJ, Luke RW, Minshull CA, McAlister MS, McCall EJ, McMiken HH, Paterson DS, Timms D, Tucker JA, Pauptit RA, Structure. 2004 Jan;12(1):75-84. PMID:14725767 Page seeded by OCA on Sat May 3 11:30:46 2008

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