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

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

Affiliation

  • 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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