1dvy

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[[Image:1dvy.gif|left|200px]]
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{{STRUCTURE_1dvy| PDB=1dvy | SCENE= }}
{{STRUCTURE_1dvy| PDB=1dvy | SCENE= }}
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'''CRYSTAL STRUCTURE OF TRANSTHYRETIN IN COMPLEX WITH N-(M-TRIFLUOROMETHYLPHENYL) PHENOXAZINE-4,6-DICARBOXYLIC ACID'''
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===CRYSTAL STRUCTURE OF TRANSTHYRETIN IN COMPLEX WITH N-(M-TRIFLUOROMETHYLPHENYL) PHENOXAZINE-4,6-DICARBOXYLIC ACID===
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==Overview==
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The human amyloid disorders, familial amyloid polyneuropathy, familial amyloid cardiomyopathy and senile systemic amyloidosis, are caused by insoluble transthyretin (TTR) fibrils, which deposit in the peripheral nerves and heart tissue. Several nonsteroidal anti-inflammatory drugs and structurally similar compounds have been found to strongly inhibit the formation of TTR amyloid fibrils in vitro. These include flufenamic acid, diclofenac, flurbiprofen, and resveratrol. Crystal structures of the protein-drug complexes have been determined to allow detailed analyses of the protein-drug interactions that stabilize the native tetrameric conformation of TTR and inhibit the formation of amyloidogenic TTR. Using a structure-based drug design approach ortho-trifluormethylphenyl anthranilic acid and N-(meta-trifluoromethylphenyl) phenoxazine 4, 6-dicarboxylic acid have been discovered to be very potent and specific TTR fibril formation inhibitors. This research provides a rationale for a chemotherapeutic approach for the treatment of TTR-associated amyloid diseases.
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(as it appears on PubMed at http://www.pubmed.gov), where 10742177 is the PubMed ID number.
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{{ABSTRACT_PUBMED_10742177}}
==About this Structure==
==About this Structure==
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[[Category: Signaling protein]]
[[Category: Signaling protein]]
[[Category: Thyroxine transport]]
[[Category: Thyroxine transport]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 14:20:48 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jun 30 23:42:03 2008''

Revision as of 20:42, 30 June 2008

Image:1dvy.png

Template:STRUCTURE 1dvy

CRYSTAL STRUCTURE OF TRANSTHYRETIN IN COMPLEX WITH N-(M-TRIFLUOROMETHYLPHENYL) PHENOXAZINE-4,6-DICARBOXYLIC ACID

Template:ABSTRACT PUBMED 10742177

About this Structure

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

Reference

Rational design of potent human transthyretin amyloid disease inhibitors., Klabunde T, Petrassi HM, Oza VB, Raman P, Kelly JW, Sacchettini JC, Nat Struct Biol. 2000 Apr;7(4):312-21. PMID:10742177

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