2j4a
From Proteopedia
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- | [[Image:2j4a.jpg|left|200px]]<br /><applet load="2j4a" size=" | + | [[Image:2j4a.jpg|left|200px]]<br /><applet load="2j4a" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="2j4a, resolution 2.2Å" /> | caption="2j4a, resolution 2.2Å" /> | ||
'''HUMAN THYROID HORMONE RECEPTOR BETA LIGAND BINDING DOMAIN IN COMPLEX WITH KB131084'''<br /> | '''HUMAN THYROID HORMONE RECEPTOR BETA LIGAND BINDING DOMAIN IN COMPLEX WITH KB131084'''<br /> | ||
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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. | ||
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- | ==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 OEF 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:// | + | 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:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 13:26:28 2008'' |
Revision as of 11:26, 23 January 2008
|
HUMAN THYROID HORMONE RECEPTOR BETA LIGAND BINDING DOMAIN IN COMPLEX WITH KB131084
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.
About 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.
Reference
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
Page seeded by OCA on Wed Jan 23 13:26:28 2008