2qgc: Difference between revisions

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[[Image:2qgc.jpg|left|200px]]
{{Seed}}
[[Image:2qgc.png|left|200px]]


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{{STRUCTURE_2qgc|  PDB=2qgc  |  SCENE=  }}  
{{STRUCTURE_2qgc|  PDB=2qgc  |  SCENE=  }}  


'''Human transthyretin (TTR) complexed with 2-(3,5-Dimethyl-4-hydroxyphenyl)benzoxazole'''
===Human transthyretin (TTR) complexed with 2-(3,5-Dimethyl-4-hydroxyphenyl)benzoxazole===




==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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{{ABSTRACT_PUBMED_18095641}}


==About this Structure==
==About this Structure==
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[[Category: Tetramer]]
[[Category: Tetramer]]
[[Category: Transthyretin]]
[[Category: Transthyretin]]
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May  4 14:54:39 2008''
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 23:52:41 2008''

Revision as of 20:52, 28 July 2008

File:2qgc.png

Template:STRUCTURE 2qgc

Human transthyretin (TTR) complexed with 2-(3,5-Dimethyl-4-hydroxyphenyl)benzoxazole

Template:ABSTRACT PUBMED 18095641

About this Structure

2QGC 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

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