2j4a: Difference between revisions

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==Overview==
==Overview==
A new high-affinity thyroid hormone antagonist 6 with druglike properties, was designed and synthesized. The compound behaved as an antagonist in a, cell transactivation assay, and in a first in vivo experiment in rats.
A new high-affinity thyroid hormone antagonist 6 with druglike properties, was designed and synthesized. The compound behaved as an antagonist in a, cell transactivation assay, and in a first in vivo experiment in rats.
==Disease==
Known diseases associated with this structure: Thyroid hormone resistance OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=190160 190160]], Thyroid hormone resistance, autosomal recessive OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=190160 190160]]


==About this Structure==
==About this Structure==
2J4A is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=OEF:'>OEF</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Known structural/functional Site: <scene name='pdbsite=AC1:Oef Binding Site For Chain A'>AC1</scene>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2J4A OCA].  
2J4A is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=OEF:'>OEF</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Known structural/functional Site: <scene name='pdbsite=AC1:Oef+Binding+Site+For+Chain+A'>AC1</scene>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2J4A OCA].  


==Reference==
==Reference==
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[[Category: zinc-finger]]
[[Category: zinc-finger]]


''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 13:26:28 2008''
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Feb  3 10:41:23 2008''

Revision as of 11:41, 3 February 2008

File:2j4a.jpg


2j4a, resolution 2.2Å

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HUMAN THYROID HORMONE RECEPTOR BETA LIGAND BINDING DOMAIN IN COMPLEX WITH KB131084

OverviewOverview

A new high-affinity thyroid hormone antagonist 6 with druglike properties, was designed and synthesized. The compound behaved as an antagonist in a, cell transactivation assay, and in a first in vivo experiment in rats.

DiseaseDisease

Known diseases associated with this structure: Thyroid hormone resistance OMIM:[190160], Thyroid hormone resistance, autosomal recessive OMIM:[190160]

About this StructureAbout this Structure

2J4A is a Single protein structure of sequence from Homo sapiens with as ligand. Known structural/functional Site: . Full crystallographic information is available from OCA.

ReferenceReference

Thyroid receptor ligands. 6. A high affinity "direct antagonist" selective for the thyroid hormone receptor., Koehler K, Gordon S, Brandt P, Carlsson B, Backsbro-Saeidi A, Apelqvist T, Agback P, Grover GJ, Nelson W, Grynfarb M, Farnegardh M, Rehnmark S, Malm J, J Med Chem. 2006 Nov 16;49(23):6635-7. PMID:17154490

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