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In silico and in vitro assessment of androgen receptor antagonists

Computational biology and chemistry, 2021-06, Vol.92, p.107490, Article 107490

2021

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Structural Biology-Based Exploration of Subtype-Selective Agonists for Peroxisome Proliferator-Activated Receptors

International journal of molecular sciences, 2021-08, Vol.22 (17), p.9223

Miyachi, Hiroyuki

2021

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X-Ray Structures of the LXRα LBD in Its Homodimeric Form and Implications for Heterodimer Signaling

Journal of molecular biology, 2010-05, Vol.399 (1), p.120-132

2010

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Ligand Binding Induces Agonistic-Like Conformational Adaptations in Helix 12 of Progesterone Receptor Ligand Binding Domain

Frontiers in chemistry, 2019-05, Vol.7, p.315-315

2019

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Trifluoromethyl group as a pharmacophore: Effect of replacing a CF 3 group on binding and agonist activity of a glucocorticoid receptor ligand

Bioorganic & medicinal chemistry letters, 2005-11, Vol.15 (21), p.4761-4769

2005

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Structural review of PPARγ in complex with ligands: Cartesian‐ and dihedral angle principal component analyses of X‐ray crystallographic data

Proteins, structure, function, and bioinformatics, 2017-09, Vol.85 (9), p.1684-1698

2017

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Atomic modelling and systematic mutagenesis identify residues in multiple drug binding sites that are essential for drug resistance in the major Candida transporter Cdr1

Biochimica et biophysica acta, 2016-11, Vol.1858 (11), p.2858-2870

2016

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Structural and Dynamical Insight into PPARγ Antagonism: In Silico Study of the Ligand-Receptor Interactions of Non-Covalent Antagonists

International journal of molecular sciences, 2015-07, Vol.16 (7), p.15405-15424

2015

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Study of the impact of the T877A mutation on ligand-induced helix-12 positioning of the androgen receptor resulted in design and synthesis of novel antiandrogens

Proteins, structure, function, and bioinformatics, 2010-02, Vol.78 (3), p.623-637

2010

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PPARγ non-covalent antagonists exhibit mutable binding modes with a similar free energy of binding: a case study

Journal of biomolecular structure & dynamics, 2017-02, Vol.35 (3), p.476-485

Fratev, Filip

2017

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Structural insights into Resveratrol's antagonist and partial agonist actions on estrogen receptor alpha

BMC structural biology, 2013-10, Vol.13 (1), p.27-27, Article 27

2013

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CH5137291, an androgen receptor nuclear translocation-inhibiting compound, inhibits the growth of castration-resistant prostate cancer cells

International journal of oncology, 2015-04, Vol.46 (4), p.1560-1572

2015

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An interpretation of positional displacement of the helix12 in nuclear receptors: Preexistent swing-up motion triggered by ligand binding

Biochimica et biophysica acta, 2010-09, Vol.1804 (9), p.1832-1840

2010

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Interaction of β3/β2-Peptides, Consisting of Val-Ala-Leu Segments, with POPC Giant Unilamellar Vesicles (GUVs) and White Blood Cancer Cells (U937) - A New Type of Cell-Penetrating Peptides, and a Surprising Chain-Length Dependence of Their Vesicle- and Cell-Lysing Activity

Chemistry & biodiversity, 2015-05, Vol.12 (5), p.697-732

2015

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Breast cancer-derived M543V mutation in helix 12 of estrogen receptor α inverts response to estrogen and SERMs

Breast cancer research and treatment, 2010-04, Vol.120 (3), p.761-768

2010

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Multiple co-activator complexes support ligand-induced transactivation function of VDR

Archives of biochemistry and biophysics, 2007-04, Vol.460 (2), p.166-171

2007

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β2-amino acids-syntheses, occurrence in natural products, and components of β-peptides1,2

Peptide Science, 2004, Vol.76 (3), p.206-243

2004

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Functional mutations of estrogen receptor protein: assay for detection

Breast cancer research and treatment, 2002-03, Vol.72 (1), p.61-68

2002

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Trehalose induces autophagy via lysosomal-mediated TFEB activation in models of motoneuron degeneration

Autophagy, 2019-04, Vol.15 (4), p.631-651

2019

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Multiple renal cancer susceptibility polymorphisms modulate the HIF pathway

PLoS genetics, 2017-07, Vol.13 (7), p.e1006872-e1006872

2017

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Reciprocal regulation by hypoxia-inducible factor-2α and the NAMPT-NAD+ -SIRT axis in articular chondrocytes is involved in osteoarthritis

Osteoarthritis and cartilage, 2015-12, Vol.23 (12), p.2288-2296

2015

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Functional characterization of the 12p12.1 renal cancer-susceptibility locus implicates BHLHE41

Nature communications, 2016-07, Vol.7 (1), p.12098-12098, Article 12098

2016

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Vitamin B12 and folic acid alleviate symptoms of nutritional deficiency by antagonizing aryl hydrocarbon receptor

Proceedings of the National Academy of Sciences - PNAS, 2020-07, Vol.117 (27), p.15837-15845

2020

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Natural history and cell of origin of TC F3-ZN F384 and PTPN11 mutations in monozygotic twins with concordant BCP-ALL

Blood, 2019-09, Vol.134 (11), p.900-905

2019

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A basic Helix-Loop-Helix (SlARANCIO), identified from a Solanum pennellii introgression line, affects carotenoid accumulation in tomato fruits

Scientific reports, 2019-03, Vol.9 (1), p.3699-3699, Article 3699

2019

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In silico and in vitro assessment of androgen receptor antagonists

Structural Biology-Based Exploration of Subtype-Selective Agonists for Peroxisome Proliferator-Activated Receptors

X-Ray Structures of the LXRα LBD in Its Homodimeric Form and Implications for Heterodimer Signaling

Ligand Binding Induces Agonistic-Like Conformational Adaptations in Helix 12 of Progesterone Receptor Ligand Binding Domain

Trifluoromethyl group as a pharmacophore: Effect of replacing a CF 3 group on binding and agonist activity of a glucocorticoid receptor ligand

Structural review of PPARγ in complex with ligands: Cartesian‐ and dihedral angle principal component analyses of X‐ray crystallographic data

Atomic modelling and systematic mutagenesis identify residues in multiple drug binding sites that are essential for drug resistance in the major Candida transporter Cdr1

Structural and Dynamical Insight into PPARγ Antagonism: In Silico Study of the Ligand-Receptor Interactions of Non-Covalent Antagonists

Study of the impact of the T877A mutation on ligand-induced helix-12 positioning of the androgen receptor resulted in design and synthesis of novel antiandrogens

PPARγ non-covalent antagonists exhibit mutable binding modes with a similar free energy of binding: a case study

Structural insights into Resveratrol's antagonist and partial agonist actions on estrogen receptor alpha

CH5137291, an androgen receptor nuclear translocation-inhibiting compound, inhibits the growth of castration-resistant prostate cancer cells

An interpretation of positional displacement of the helix12 in nuclear receptors: Preexistent swing-up motion triggered by ligand binding

Interaction of β3/β2-Peptides, Consisting of Val-Ala-Leu Segments, with POPC Giant Unilamellar Vesicles (GUVs) and White Blood Cancer Cells (U937) - A New Type of Cell-Penetrating Peptides, and a Surprising Chain-Length Dependence of Their Vesicle- and Cell-Lysing Activity

Breast cancer-derived M543V mutation in helix 12 of estrogen receptor α inverts response to estrogen and SERMs

Multiple co-activator complexes support ligand-induced transactivation function of VDR

β2-amino acids-syntheses, occurrence in natural products, and components of β-peptides1,2

Functional mutations of estrogen receptor protein: assay for detection

Trehalose induces autophagy via lysosomal-mediated TFEB activation in models of motoneuron degeneration

Multiple renal cancer susceptibility polymorphisms modulate the HIF pathway

Reciprocal regulation by hypoxia-inducible factor-2α and the NAMPT-NAD+ -SIRT axis in articular chondrocytes is involved in osteoarthritis

Functional characterization of the 12p12.1 renal cancer-susceptibility locus implicates BHLHE41

Vitamin B12 and folic acid alleviate symptoms of nutritional deficiency by antagonizing aryl hydrocarbon receptor

Natural history and cell of origin of TC F3-ZN F384 and PTPN11 mutations in monozygotic twins with concordant BCP-ALL

A basic Helix-Loop-Helix (SlARANCIO), identified from a Solanum pennellii introgression line, affects carotenoid accumulation in tomato fruits

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