kb-2115 and Disease-Models--Animal

kb-2115 has been researched along with Disease-Models--Animal* in 1 studies

Other Studies

1 other study(ies) available for kb-2115 and Disease-Models--Animal

Article	Year
Discovery of novel indane derivatives as liver-selective thyroid hormone receptor β (TRβ) agonists for the treatment of dyslipidemia. Bioorganic & medicinal chemistry, 2012, Jun-01, Volume: 20, Issue:11 Thyromimetics that specifically target TRβ have been shown to reduce plasma cholesterol levels and avoid atherosclerosis through the promotion of reverse cholesterol transport in an animal model. We designed novel thyromimetics with high receptor (TRβ) and organ (liver) selectivity based on the structure of eprotirome (3) and molecular modeling. We found that indane derivatives are potent and dual-selective thyromimetics expected to avoid hypothyroidism in some tissues as well as heart toxicity. KTA-439 (29), a representative indane derivative, showed the same high human TRβ selectivity in a binding assay as 3 and higher liver selectivity than 3 in a cholesterol-fed rat model. Topics: Animals; Arginine; Cholesterol; Disease Models, Animal; Drug Design; Drug Evaluation, Preclinical; Dyslipidemias; Humans; Indans; Ligands; Liver; Male; Malonates; Models, Molecular; Molecular Mimicry; Molecular Structure; Rats; Rats, Wistar; Small Molecule Libraries; Structure-Activity Relationship; Thyroid Hormone Receptors beta	2012

Article

Year

Discovery of novel indane derivatives as liver-selective thyroid hormone receptor β (TRβ) agonists for the treatment of dyslipidemia.

Bioorganic & medicinal chemistry, 2012, Jun-01, Volume: 20, Issue:11

Thyromimetics that specifically target TRβ have been shown to reduce plasma cholesterol levels and avoid atherosclerosis through the promotion of reverse cholesterol transport in an animal model. We designed novel thyromimetics with high receptor (TRβ) and organ (liver) selectivity based on the structure of eprotirome (3) and molecular modeling. We found that indane derivatives are potent and dual-selective thyromimetics expected to avoid hypothyroidism in some tissues as well as heart toxicity. KTA-439 (29), a representative indane derivative, showed the same high human TRβ selectivity in a binding assay as 3 and higher liver selectivity than 3 in a cholesterol-fed rat model.

Topics: Animals; Arginine; Cholesterol; Disease Models, Animal; Drug Design; Drug Evaluation, Preclinical; Dyslipidemias; Humans; Indans; Ligands; Liver; Male; Malonates; Models, Molecular; Molecular Mimicry; Molecular Structure; Rats; Rats, Wistar; Small Molecule Libraries; Structure-Activity Relationship; Thyroid Hormone Receptors beta

2012