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2fpt

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{{STRUCTURE_2fpt| PDB=2fpt | SCENE= }}
{{STRUCTURE_2fpt| PDB=2fpt | SCENE= }}
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'''Dual Binding Mode of a Novel Series of DHODH inhibitors'''
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===Dual Binding Mode of a Novel Series of DHODH inhibitors===
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==Overview==
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Human dihydroorotate dehydrogenase (DHODH) represents an important target for the treatment of hyperproliferative and inflammatory diseases. In the cell DHODH catalyzes the rate-limiting step of the de novo pyrimidine biosynthesis. DHODH inhibition results in beneficial immunosuppressant and antiproliferative effects in diseases such as rheumatoid arthritis. Here, we present high-resolution X-ray structures of human DHODH in complex with a novel class of low molecular weight compounds that inhibit the enzyme in the nanomolar range. Some compounds showed an interesting dual binding mode within the same cocrystal strongly depending on the nature of chemical substitution. Measured in vitro activity data correlated with the prevailing mode of binding and explained the observed structure-activity relationship. Additionally, the X-ray data confirmed the competitive nature of the inhibitors toward the putative ubiquinone binding site and will guide structure-based design and synthesis of molecules with higher activity.
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(as it appears on PubMed at http://www.pubmed.gov), where 16480261 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16480261}}
==About this Structure==
==About this Structure==
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[[Category: Walloschek, M.]]
[[Category: Walloschek, M.]]
[[Category: Protein inhibitor complex]]
[[Category: Protein inhibitor complex]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 04:10:51 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 16:30:02 2008''

Revision as of 13:30, 27 July 2008

Image:2fpt.png

Template:STRUCTURE 2fpt

Dual Binding Mode of a Novel Series of DHODH inhibitors

Template:ABSTRACT PUBMED 16480261

About this Structure

2FPT is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Dual binding mode of a novel series of DHODH inhibitors., Baumgartner R, Walloschek M, Kralik M, Gotschlich A, Tasler S, Mies J, Leban J, J Med Chem. 2006 Feb 23;49(4):1239-47. PMID:16480261

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