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Structure and specificity of nuclear receptor-coactivator interactions.
TLDR
Biochemical and crystallographic analyses revealed that hormone binding leads to the formation of a hydrophobic groove within the ligand binding domain of the thyroid hormone receptor that interacts with an LxxLL motif-containing alpha-helix from GRIP1, a coactivator, suggesting that these common structural elements impart flexibility to combinatorial regulation, whereas side chains at the interface impart specificity.
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A structural role for hormone in the thyroid hormone receptor
TLDR
A structural role for ligand is suggested, in establishing the active conformation of the receptor, that is likely to underlie hormonal regulation of gene expression for the nuclear receptors.
View on Nature
A surface on the androgen receptor that allosterically regulates coactivator binding
TLDR
It is proposed that BF-3 is a previously unrecognized allosteric regulatory site needed for AR activity in vivo and a possible pharmaceutical target.
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A method for isolation of intact, translationally active ribonucleic acid.
TLDR
A method for isolation of large, translationally active RNA species is presented and yields large mRNA precursors up to 10 kb and mRNA species which translate very well, however, small RNA species are recovered with a poor yield.
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A high-affinity subtype-selective agonist ligand for the thyroid hormone receptor.
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Hormone-dependent coactivator binding to a hydrophobic cleft on nuclear receptors.
TLDR
Scanning surface mutagenesis on the human thyroid hormone receptor was performed to define the site that binds the coactivators, glucocorticoid receptor-interacting protein 1 (GRIP1) and steroid receptor coactivator 1 (SRC-1).
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Regulation of Thyroid Hormone Receptor Isoforms in Physiological and Pathological Cardiac Hypertrophy
TLDR
It is concluded that TR isoforms have distinct regulation and function in rat cardiac myocytes, and changes in myocyte TR levels can explain in part the characteristic molecular phenotypes in physiological and pathological cardiac hypertrophy.
View on Wolters Kluwer
Selective thyroid hormone receptor-β activation: A strategy for reduction of weight, cholesterol, and lipoprotein (a) with reduced cardiovascular liability
TLDR
TRβ-selective agonists may constitute a previously uncharacterized class of drugs to treat obesity, hypercholesterolemia, and elevated lipoprotein in mice, rats, and monkeys.
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Selective thyroid receptor modulation by GC-1 reduces serum lipids and stimulates steps of reverse cholesterol transport in euthyroid mice.
TLDR
Use of TRbeta and uptake selective agonists such as GC-1 should be further explored as a strategy to improve lipid metabolism in dyslipoproteinemia to stimulate important steps in reverse cholesterol transport.
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The thyroid hormone mimetic compound KB2115 lowers plasma LDL cholesterol and stimulates bile acid synthesis without cardiac effects in humans
TLDR
In moderately overweight and hypercholesterolemic subjects KB2115 was found to be safe and well tolerated and elicited up to a 40% lowering of total and LDL cholesterol after 14 days of treatment, suggesting that the pharmacological selectivity observed in animal models translates to humans.
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