2j4a

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Image:2j4a.gif

2j4a, resolution 2.2Å

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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 OEF as [ligand]. 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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