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2qge

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[[Image:2qge.jpg|left|200px]]
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{{Seed}}
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{{STRUCTURE_2qge| PDB=2qge | SCENE= }}
{{STRUCTURE_2qge| PDB=2qge | SCENE= }}
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'''Human transthyretin (TTR) complexed with 2-(3,5-Dimethylphenyl)benzoxazole'''
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===Human transthyretin (TTR) complexed with 2-(3,5-Dimethylphenyl)benzoxazole===
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==Overview==
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To develop potent transthyretin (TTR) amyloidogenesis inhibitors that also display high binding selectivity in blood, it proves useful to systematically optimize each of the three substructural elements that comprise a typical inhibitor: the two aryl rings and the linker joining them. In the first study, described herein, structural modifications to one aryl ring were evaluated by screening a library of 2-arylbenzoxazoles bearing thyroid hormone-like aryl substituents on the 2-aryl ring. Several potent and highly selective amyloidogenesis inhibitors were identified that exhibit minimal thyroid hormone nuclear receptor and COX-1 binding. High resolution crystal structures (1.3-1.5 A) of three inhibitors (2f, 4f, and 4d) in complex with TTR were obtained to characterize their binding orientation. Collectively, the results demonstrate that thyroid hormone-like substitution patterns on one aryl ring lead to potent and highly selective TTR amyloidogenesis inhibitors that lack undesirable thyroid hormone receptor or COX-1 binding.
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The line below this paragraph, {{ABSTRACT_PUBMED_18095641}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 18095641 is the PubMed ID number.
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{{ABSTRACT_PUBMED_18095641}}
==About this Structure==
==About this Structure==
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[[Category: Tetramer]]
[[Category: Tetramer]]
[[Category: Transthyretin]]
[[Category: Transthyretin]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 14:54:48 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 06:07:00 2008''

Revision as of 03:07, 28 July 2008

Image:2qge.png

Template:STRUCTURE 2qge

Human transthyretin (TTR) complexed with 2-(3,5-Dimethylphenyl)benzoxazole

Template:ABSTRACT PUBMED 18095641

About this Structure

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

Reference

Biochemical and structural evaluation of highly selective 2-arylbenzoxazole-based transthyretin amyloidogenesis inhibitors., Johnson SM, Connelly S, Wilson IA, Kelly JW, J Med Chem. 2008 Jan 24;51(2):260-70. Epub 2007 Dec 21. PMID:18095641

Page seeded by OCA on Mon Jul 28 06:07:00 2008

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