PDBsum entry 2j4a

Receptor

PDB id

2j4a

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Contents

			Protein chain

					251 a.a. *

			Ligands

					OEF

			Waters ×107

* Residue conservation analysis

PDB id:

2j4a

Links

Name:

Receptor

Title:

Human thyroid hormone receptor beta ligand binding domain in complex with kb131084

Structure:

Thyroid hormone receptor beta-1. Chain: a. Fragment: ligand binding domain, residues 209-461. Synonym: thyroid hormone receptor beta lbd. Engineered: yes. Mutation: yes

Source:

Homo sapiens. Human. Organism_taxid: 9606. Expressed in: escherichia coli. Expression_system_taxid: 562

Resolution:

2.20Å

R-factor:

0.230

R-free:

0.273

Authors:

M.Farnegardh

Key ref:

K.Koehler et al. (2006). Thyroid receptor ligands. 6. A high affinity "direct antagonist" selective for the thyroid hormone receptor. J Med Chem, 49, 6635-6637. PubMed id: 17154490

Date:

28-Aug-06

Release date:

25-Sep-07

PROCHECK

	Headers

	References

Protein chain

P10828 (THB_HUMAN) - Thyroid hormone receptor beta from Homo sapiens

Seq: Struc:					461 a.a. 251 a.a.*

Key:

PfamA domain

Secondary structure

CATH domain

* PDB and UniProt seqs differ at 1 residue position (black cross)



		Enzyme reactions

Enzyme class:

E.C.?

[IntEnz] [ExPASy] [KEGG] [BRENDA]

	J Med Chem 49:6635-6637 (2006)
PubMed id: 17154490

Thyroid receptor ligands. 6. A high affinity "direct antagonist" selective for the thyroid hormone receptor.
K.Koehler, S.Gordon, P.Brandt, B.Carlsson, A.Bäcksbro-Saeidi, T.Apelqvist, P.Agback, G.J.Grover, W.Nelson, M.Grynfarb, M.Färnegårdh, S.Rehnmark, J.Malm.

ABSTRACT

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.

Literature references that cite this PDB file's key reference

PubMed id

Reference

19111515

M.Jeyakumar, and J.A.Katzenellenbogen (2009).
A dual-acceptor time-resolved Föster resonance energy transfer assay for simultaneous determination of thyroid hormone regulation of corepressor and coactivator binding to the thyroid hormone receptor: Mimicking the cellular context of thyroid hormone action.

Anal Biochem, 386, 73-78.

The most recent references are shown first. Citation data come partly from CiteXplore and partly from an automated harvesting procedure. Note that this is likely to be only a partial list as not all journals are covered by either method. However, we are continually building up the citation data so more and more references will be included with time.