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| [[Image:2qge.jpg|left|200px]] | | {{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'''
| | ===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.
| | The line below this paragraph, {{ABSTRACT_PUBMED_18095641}}, adds the Publication Abstract to the page |
| | (as it appears on PubMed at http://www.pubmed.gov), where 18095641 is the PubMed ID number. |
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| | {{ABSTRACT_PUBMED_18095641}} |
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| ==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 14:54:48 2008'' | | |
| | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 06:07:00 2008'' |
