title: Thyroid receptor ligands. 6. A high affinity "direct antagonist" selective for the thyroid hormone receptor.
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.
authors.affiliation: Karo Bio AB, Novum, Huddinge SE-141 57, Sweden.
authors.forename: Konrad
authors.initials: K
authors.lastname: Koehler
authors.forename: Sandra
authors.initials: S
authors.lastname: Gordon
authors.forename: Peter
authors.initials: P
authors.lastname: Brandt
authors.forename: Bo
authors.initials: B
authors.lastname: Carlsson
authors.forename: Anna
authors.initials: A
authors.lastname: Bäcksbro-Saeidi
authors.forename: Theresa
authors.initials: T
authors.lastname: Apelqvist
authors.forename: Peter
authors.initials: P
authors.lastname: Agback
authors.forename: Gary J
authors.initials: GJ
authors.lastname: Grover
authors.forename: William
authors.initials: W
authors.lastname: Nelson
authors.forename: Marlena
authors.initials: M
authors.lastname: Grynfarb
authors.forename: Mathias
authors.initials: M
authors.lastname: Färnegårdh
authors.forename: Stefan
authors.initials: S
authors.lastname: Rehnmark
authors.forename: Johan
authors.initials: J
authors.lastname: Malm
mesh_terms: D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D006801:Humans; D008024:Ligands; D008958:Models, Molecular; D010666:Phenylpropionates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D011988:Receptors, Thyroid Hormone / Q000037:antagonists & inhibitors*; D037021:Thyroid Hormone Receptors alpha / Q000037:antagonists & inhibitors; D037042:Thyroid Hormone Receptors beta / Q000037:antagonists & inhibitors / Q000737:chemistry; D015533:Transcriptional Activation / Q000187:drug effects
chemical_list: C516213:3-(3,5-dibromo-4-(4-hydroxy-3-isopropyl-5-(2-pyridin-4-ylvinyl)phenoxy)phenyl)propionic acid; D008024:Ligands; D010666:Phenylpropionates; D011725:Pyridines; D011988:Receptors, Thyroid Hormone; D037021:Thyroid Hormone Receptors alpha; D037042:Thyroid Hormone Receptors beta