Design of thyroid hormone receptor antagonists from first principles (Q35089959)

6 August 2017

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title

Design of thyroid hormone receptor antagonists from first principles (English)

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6 August 2017

14

Robert J Fletterick

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6 August 2017

Paul Webb

1

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6 August 2017

Ngoc-Ha Nguyen

2

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6 August 2017

Grazia Chiellini

3

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6 August 2017

Hikari A I Yoshihara

4

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6 August 2017

Suzana T Cunha Lima

5

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6 August 2017

James W Apriletti

6

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6 August 2017

Ralff C J Ribeiro

7

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6 August 2017

Adhirai Marimuthu

8

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6 August 2017

Brian L West

9

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6 August 2017

Patrick Goede

10

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6 August 2017

Karin Mellstrom

11

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6 August 2017

Stefan Nilsson

12

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6 August 2017

Peter J Kushner

13

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6 August 2017

Thomas S Scanlan

15

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6 August 2017

John D Baxter

16

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6 August 2017

language of work or name

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1 December 2002

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The Journal of Steroid Biochemistry and Molecular Biology

6 August 2017

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6 August 2017

83

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6 August 2017

1-5

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6 August 2017

59-73

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The nuclear hormone receptor gene superfamily

6 August 2017

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https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Selective modulation of thyroid hormone receptor action.

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Therapeutic potential of selective estrogen receptor modulators.

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

An issue of tissues: divining the split personalities of selective estrogen receptor modulators

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https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Connections and regulation of the human estrogen receptor

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https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Molecular determinants for the tissue specificity of SERMs

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https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Differential ligand activation of estrogen receptors ERalpha and ERbeta at AP1 sites

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

The estrogen receptor enhances AP-1 activity by two distinct mechanisms with different requirements for receptor transactivation functions

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https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Unique protein determinants of the subtype-selective ligand responses of the estrogen receptors (ERalpha and ERbeta ) at AP-1 sites

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Synthesis and structure-activity relationships of oxamic acid and acetic acid derivatives related to L-thyronine

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Transcriptional Regulation of Rat Hepatic Low-Density Lipoprotein Receptor and Cholesterol 7α Hydroxylase by Thyroid Hormone

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Effects of L-triiodothyronine and the thyromimetic L-94901 on serum lipoprotein levels and hepatic low-density lipoprotein receptor, 3-hydroxy-3-methylglutaryl coenzyme A reductase, and apo A-I gene expression.

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Experimental hyperthyroidism in man: effects on plasma lipoproteins, lipoprotein lipase and hepatic lipase

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https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Thyrotoxicosis and the heart

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https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Biochemical basis of thyroid hormone action in the heart

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https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Cardiac function in thyroid disease: clinical features and management considerations

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Thyroid hormone treatment of depression

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https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Biochemical assessment of bone loss in patients on long-term thyroid hormone treatment.

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Serum triiodothyronine, bone turnover, and bone mass changes in euthyroid pre- and postmenopausal women

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Molecular and structural biology of thyroid hormone receptors.

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https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

A high-affinity subtype-selective agonist ligand for the thyroid hormone receptor

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https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Physiological and molecular basis of thyroid hormone action

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https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

The mechanism of action of thyroid hormones

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https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

The T3R alpha gene encoding a thyroid hormone receptor is essential for post-natal development and thyroid hormone production

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Abnormal heart rate and body temperature in mice lacking thyroid hormone receptor alpha 1

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Functions of thyroid hormone receptors in mice

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https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

The effects of amiodarone on thyroid hormone function: a review of the physiology and clinical manifestations

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Antagonism of thyroid hormone action by amiodarone in rat pituitary tumor cells

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Desethylamiodarone is a noncompetitive inhibitor of the binding of thyroid hormone to the thyroid hormone beta 1-receptor protein

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Desethylamiodarone is a competitive inhibitor of the binding of thyroid hormone to the thyroid hormone alpha 1-receptor protein

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Desethylamiodarone interferes with the binding of co-activator GRIP-1 to the beta 1-thyroid hormone receptor

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Interaction of amiodarone and desethylamiodarone with solubilized nuclear thyroid hormone receptors

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https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Amiodarone-induced liver toxicity

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Identification and measurement of desethylamiodarone in blood plasma specimens from amiodarone-treated patients

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Effect of mutations in the beta1-thyroid hormone receptor on the inhibition of T3 binding by desethylamiodarone

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https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Amiodarone and desethylamiodarone toxicity in isolated hepatocytes in culture.

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Cytotoxic effects of amiodarone and desethylamiodarone on human thyrocytes

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

The molecular biology of thyroid hormone action.

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

The nuclear receptor corepressor (N-CoR) contains three isoleucine motifs (I/LXXII) that serve as receptor interaction domains (IDs).

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

X-ray crystallographic and functional studies of thyroid hormone receptor

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https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Nuclear receptor coactivators

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Temporal formation of distinct thyroid hormone receptor coactivator complexes in HeLa cells

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Unliganded thyroid hormone receptor alpha can target TATA-binding protein for transcriptional repression

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

The TRAP220 component of a thyroid hormone receptor- associated protein (TRAP) coactivator complex interacts directly with nuclear receptors in a ligand-dependent fashion

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Specific structural motifs determine TRAP220 interactions with nuclear hormone receptors

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Identity between TRAP and SMCC complexes indicates novel pathways for the function of nuclear receptors and diverse mammalian activators

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

A structural role for hormone in the thyroid hormone receptor.

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Structure and specificity of nuclear receptor-coactivator interactions

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Nuclear-receptor ligands and ligand-binding domains

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Hormone-dependent coactivator binding to a hydrophobic cleft on nuclear receptors

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Structural basis for antagonist-mediated recruitment of nuclear co-repressors by PPARalpha

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Natural ligands of nuclear receptors have conserved volumes

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Molecular basis of agonism and antagonism in the oestrogen receptor

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

The structural basis of estrogen receptor/coactivator recognition and the antagonism of this interaction by tamoxifen

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Structure of the ligand-binding domain of oestrogen receptor beta in the presence of a partial agonist and a full antagonist

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Structural insights into the mode of action of a pure antiestrogen

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Structure-based design and synthesis of a thyroid hormone receptor (TR) antagonist.

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Synthesis and biological activity of novel thyroid hormone analogues: 5'-aryl substituted GC-1 derivatives

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

A designed antagonist of the thyroid hormone receptor

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Rational design and synthesis of a novel thyroid hormone antagonist that blocks coactivator recruitment

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

A thyroid hormone antagonist that inhibits thyroid hormone action in vivo

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Nuclear receptors, coregulators, ligands, and selective receptor modulators: making sense of the patchwork quilt

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Elucidation of the molecular mechanism of action of selective estrogen receptor modulators

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

The nuclear corepressors NCoR and SMRT are key regulators of both ligand- and 8-bromo-cyclic AMP-dependent transcriptional activity of the human progesterone receptor

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

The partial agonist activity of antagonist-occupied steroid receptors is controlled by a novel hinge domain-binding coactivator L7/SPA and the corepressors N-CoR or SMRT

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Diverse signaling pathways modulate nuclear receptor recruitment of N-CoR and SMRT complexes

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

The tamoxifen-responsive estrogen receptor alpha mutant D351Y shows reduced tamoxifen-dependent interaction with corepressor complexes

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Cofactor dynamics and sufficiency in estrogen receptor-regulated transcription

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Control of the estrogen-like actions of the tamoxifen-estrogen receptor complex by the surface amino acid at position 351.

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

An antiestrogen-responsive estrogen receptor-alpha mutant (D351Y) shows weak AF-2 activity in the presence of tamoxifen

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

An inhibitor of the interaction of thyroid hormone receptor beta and glucocorticoid interacting protein 1.

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Estrogen receptor-cofactor interactions as targets for novel drug discovery.

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

Mice devoid of all known thyroid hormone receptors are viable but exhibit disorders of the pituitary-thyroid axis, growth, and bone maturation

1 reference

https://api.crossref.org/works/10.1016%2FS0960-0760%2802%2900270-4

7 January 2021

10.1016/S0960-0760(02)00270-4

Identifiers

DOI

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6 August 2017

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