2j4a

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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==
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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==
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[[Category: zinc-finger]]
[[Category: zinc-finger]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 5 18:52:34 2007''
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 22:51:38 2007''

Revision as of 20:45, 12 November 2007


2j4a, resolution 2.2Å

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

Contents

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.

Disease

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

About this Structure

2J4A is a Single protein structure of sequence from Homo sapiens with OEF as ligand. Structure known Active Site: AC1. 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

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