Thyroid receptor ligands. 6. A high affinity "direct antagonist" selective for the thyroid hormone receptor

  • J Med Chem. 2006 Nov 16;49(23):6635-7. doi: 10.1021/jm060521i.
Konrad Koehler  1 ,  Sandra Gordon ,  Peter Brandt ,  Bo Carlsson ,  Anna Bäcksbro-Saeidi ,  Theresa Apelqvist ,  Peter Agback ,  Gary J Grover ,  William Nelson ,  Marlena Grynfarb ,  Mathias Färnegårdh ,  Stefan Rehnmark ,  Johan Malm
Affiliations
  • 1. Karo Bio AB, Novum, Huddinge SE-141 57, Sweden.
PMID: 17154490 DOI: 10.1021/jm060521i
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.

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