Synthesis and Crystal Structure of a Phosphorylated Estrogen Receptor Ligand Binding Domain

No abstract is available for this paper.

• Publication year

  2010

• Venue

  ChemBioChem

• Publication date

  2010-11-02

• Fields of study

  Biology, Medicine, Chemistry

• Identifiers
  DOI 10.1002/cbic.201000532PMID 20922740
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Normal and cancer-related functions of the p160 steroid receptor co-activator (SRC) family

  2009cited by this paper
• NFkappaB selectivity of estrogen receptor ligands revealed by comparative crystallographic analyses.

  2008cited by this paper
• An integrated-molecule-format multicolor probe for monitoring multiple activities of a bioactive small molecule.

  2008cited by this paper
• Sex-steroid hormones and EGF signalling in breast and prostate cancer cells: targeting the association of Src with steroid receptors.

  2008cited by this paper
• Inhibition of Estradiol Receptor/Src Association and Cell Growth by an Estradiol Receptor α Tyrosine-Phosphorylated Peptide

  2007cited by this paper
• Panning for SNuRMs: using cofactor profiling for the rational discovery of selective nuclear receptor modulators.

  2007cited by this paper
• Design of selective nuclear receptor modulators: RAR and RXR as a case study

  2007cited by this paper
• Post-translational modifications of steroid receptors.

  2006cited by this paper
• Protein ligation: an enabling technology for the biophysical analysis of proteins

  2006cited by this paper
• Protein semisynthesis and expressed protein ligation: chasing a protein's tail.

  2005cited by this paper
• Mechanism of the nuclear receptor molecular switch.

  2004cited by this paper
• Structure-based design of estrogen receptor-beta selective ligands.

  2004cited by this paper
• Characterization of the interactions of estrogen receptor and MNAR in the activation of cSrc.

  2004cited by this paper
• Nuclear receptors: integration of multiple signalling pathways through phosphorylation.

  2003cited by this paper
• Mutations of tyrosine 537 in the human estrogen receptor-alpha selectively alter the receptor's affinity for estradiol and the kinetics of the interaction.

  2002cited by this paper
• Crystal structure of a phosphorylated Smad2. Recognition of phosphoserine by the MH2 domain and insights on Smad function in TGF-beta signaling.

  2001cited by this paper
• Steroid‐induced androgen receptor–oestradiol receptor β–Src complex triggers prostate cancer cell proliferation

  2000cited by this paper
• Nuclear receptor ligand-binding domains: three-dimensional structures, molecular interactions and pharmacological implications.

  2000cited by this paper
• Function of estrogen receptor tyrosine 537 in hormone binding, DNA binding, and transactivation.

  1999cited by this paper
• Structure of the ligand‐binding domain of oestrogen receptor beta in the presence of a partial agonist and a full antagonist

  1999cited by this paper
• Ligand-independent Activation of the Estrogen Receptors α and β by Mutations of a Conserved Tyrosine Can Be Abolished by Antiestrogens

  1998cited by this paper
• The structural basis of estrogen receptor/coactivator recognition and the antagonism of this interaction by tamoxifen.

  1998cited by this paper
• Ligand-independent activation of the estrogen receptors alpha and beta by mutations of a conserved tyrosine can be abolished by antiestrogens.

  1998cited by this paper
• Cooperativity and Dimerization of Recombinant Human Estrogen Receptor Hormone-binding Domain*

  1997cited by this paper
• Ligand‐independent activation of the oestrogen receptor by mutation of a conserved tyrosine

  1997cited by this paper
• A canonical structure for the ligand-binding domain of nuclear receptors

  1996cited by this paper
• Constitutively active human estrogen receptors containing amino acid substitutions for tyrosine 537 in the receptor protein.

  1996cited by this paper
• Phosphorylation of the human estrogen receptor on tyrosine 537 in vivo and by src family tyrosine kinases in vitro.

  1995cited by this paper

• Anatomical characteristics and bioactivities of Vitis vinifera L. (Cv. Atasarisi) leaves

  2026cites this paper
• Multicomplex Pharmacophore Modeling of Estrogen Receptors Suggests the Probable Repurposing of Procaterol as an Antiproliferative Agent Against Breast Cancer Cells

  2026cites this paper
• Flaxseed Extracts Impact the Cellular Structure of a Keratinocyte Model for Oral Lichen Planus—A Preliminary Study

  2025cites this paper
• Di(2-ethylhexyl) Phthalate Alters Primordial Germ Cell Distribution and the Reproductive Neuroendocrine Regulatory Axis in Zebrafish Embryos

  2025cites this paper
• Green Synthesis of Gold Nanoparticles and Their Cytotoxic Effect in Breast Cancer: An Experimental and Theoretical Study

  2025cites this paper
• An integrated network pharmacological approach unveils the therapeutic mechanism of bonducellin, a homoisoflavonoid from Caesalpinia bonducella, against polycystic ovary syndrome

  2025cites this paper
• Advances in the chemical synthesis of human proteoforms

  2025cites this paper
• Identification of pharmacophore synergism for optimization of estrogen receptor beta binders for hormone dependent forms of breast cancer

  2025cites this paper
• Unveiling geniposide from Paederia foetida as a potential antihypertensive treatment: an integrated approach involving in vivo and computational methods

  2024cites this paper
• Detection of isoflavones and phytoestrogen-rich plant extracts binding to estrogen receptor β using a yeast-based fluorescent assay.

  2024cites this paper
• Potential of covalently linked tamoxifen hybrids for cancer treatment: recent update.

  2024cites this paper
• Raloxifene's in vitro anticancer effects against MCF-7 cells were facilitated by cholesterol-PEG functionalized mesoporous silica nanoparticles

  2023cites this paper
• Development of subtype-selective estrogen receptor modulators using the bis(4-hydroxyphenyl)silanol core as a stable isostere of bis(4-hydroxyphenyl)methanol

  2023cites this paper
• In silico simulations and molecular descriptors to predict in vitro transactivation potencies of Baikal seal estrogen receptors by environmental contaminants.

  2023cites this paper
• The G Protein-Coupled Estrogen Receptor (GPER): A Critical Therapeutic Target for Cancer

  2023cites this paper
• In vivo and in silico assessments of estrogenic potencies of bisphenol A and its analogs in zebrafish (Danio rerio): Validity of in silico approaches to predict in vivo effects.

  2023cites this paper
• Phytoecdysteroids and Anabolic Effect of Atriplex dimorphostegia: UPLC-PDA-MS/MS Profiling, In Silico and In Vivo Models

  2023cites this paper
• The marionette mechanism of domain–domain communication in the antagonist, agonist, and coactivator responses of the estrogen receptor

  2023cites this paper
• Discriminating functional and non-functional nuclear-receptor ligands with a conformational selection-inspired machine learning algorithm

  2023cites this paper
• Breast cancer therapies reduce risk of Alzheimer’s disease and promote estrogenic pathways and action in brain

  2023cites this paper
• Determination of Molecule Category of Ligands Targeting the Ligand-Binding Pocket of Nuclear Receptors with Structural Elucidation and Machine Learning

  2022cites this paper
• Effects of Organochlorine Pesticide Residues in Maternal Body on Infants

  2022influential citation
• Comprehensive assessment of estrogenic activities of parabens by in silico approach and in vitro assays.

  2022cites this paper
• Relevance of the viral Spike protein/cellular Estrogen Receptor-α interaction for endothelial-based coagulopathy induced by SARS-CoV-2

  2022cites this paper
• Optimization, spectral characterization, QSAR, and molecular docking analyses of newly designed boron compounds

  2022cites this paper
• The SARS-CoV-2 spike protein binds and modulates estrogen receptors

  2022cites this paper
• IN VITRO ANTI-NEUROINFLAMMATORY EFFECT OF GENISTEIN (4',5,7-TRIHYDROXYISOFLAVONE) ON MICROGLIA HMC3 CELL LINE, AND IN SILICO EVALUATION OF ITS INTERACTION WITH ESTROGEN RECEPTOR-β

  2021cites this paper
• Small Molecules Inhibit Extranuclear Signaling by Estrogen: A Promising Strategy to Halt Breast Cancer Progression and Metastasis

  2020cites this paper
• GLL398, an oral selective estrogen receptor degrader (SERD), blocks tumor growth in xenograft breast cancer models

  2020cites this paper
• Development of bivalent triarylalkene- and cyclofenil-derived dual estrogen receptor antagonists and downregulators.

  2020cites this paper
• Understanding the interaction of estrogenic ligands with estrogen receptors: a survey of the functional and binding kinetic studies.

  2020cites this paper
• In vivo and in silico analyses of estrogenic potential of equine estrogens in medaka (Oryzias latipes).

  2020cites this paper
• Metabolite Profiling of 96% Ethanol Extract from Marsilea crenata Presl. Leaves Using UPLC-QToF-MS/MS and Anti-Neuroinflammatory Predicition Activity with Molecular Docking

  2019cites this paper
• Size, site, and signaling: Three attributes of estrogen receptors

  2019cites this paper
• Hybrid in silico/in vitro target fishing to assign function to "orphan" compounds of food origin - The case of the fungal metabolite atromentin.

  2019cites this paper
• Estrogen receptor-mediated transcriptional activities of spent coffee grounds and spent coffee grounds compost, and their phenolic acid constituents.

  2019cites this paper
• Bone protective effects of purified extract from Ruscus aculeatus on ovariectomy-induced osteoporosis in rats.

  2019cites this paper
• Target of rapamycin FATC domain as a general membrane anchor: The FKBP‐12 like domain of FKBP38 as a case study

  2018cites this paper
• Activation of steroid hormone receptors: Shed light on the in silico evaluation of endocrine disrupting chemicals.

  2018cites this paper
• Identification of D‐seco modified steroid derivatives with affinity for estrogen receptor &agr; and &bgr; isoforms using a non‐transcriptional fluorescent cell assay in yeast

  2018cites this paper
• ZB716, a steroidal selective estrogen receptor degrader (SERD), is orally efficacious in blocking tumor growth in mouse xenograft models

  2018cites this paper
• An alternative conformation of ERβ bound to estradiol reveals H12 in a stable antagonist position

  2017cites this paper
• Biallelic and monoallelic ESR2 variants associated with 46,XY disorders of sex development

  2017cites this paper
• Phytoestrogenic Activity of Blackcurrant Anthocyanins Is Partially Mediated through Estrogen Receptor Beta

  2017influential citation
• The promiscuous estrogen receptor: evolution of physiological estrogens and response to phytochemicals and endocrine disruptors

  2017influential citation
• A second estrogen receptor from Japanese lamprey (Lethenteron japonicum) does not have activities for estrogen binding and transcription.

  2016cites this paper
• Insight into the structural stability of coumestrol with human estrogen receptor α and β subtypes: a combined approach involving docking and molecular dynamics simulation studies

  2015cites this paper
• Subtype-specific modulation of estrogen receptor-coactivator interaction by phosphorylation.

  2015cites this paper
• The Application of Ligand-Mapping Molecular Dynamics Simulations to the Rational Design of Peptidic Modulators of Protein-Protein Interactions.

  2015cites this paper
• Survey of phosphorylation near drug binding sites in the Protein Data Bank (PDB) and their effects

  2015cites this paper
• Docking-based classification models for exploratory toxicology studies on high-quality estrogenic experimental data.

  2015cites this paper
• Estrogen Receptor Folding Modulates cSrc Kinase SH2 Interaction via a Helical Binding Mode.

  2015cites this paper
• Phenytoin Is an Estrogen Receptor α-Selective Modulator That Interacts With Helix 12

  2015cites this paper
• Investigating the in Vitro Thermal Stability and Conformational Flexibility of Estrogen Receptors as Potential Key Factors of Their in Vivo Activity.

  2015cites this paper
• Estrogen Physiology from an Evolutionary Perspective

  2014cites this paper
• A structural perspective on nuclear receptors as targets of environmental compounds

  2014cites this paper
• Ecdysteroids: A novel class of anabolic agents?

  2014cites this paper
• Biological and Biomedical Aspects of Metal Phenolates

  2014cites this paper
• 3D models of human ERα and ERβ complexed with coumestrol.

  2014cites this paper
• Versatility or Promiscuity: The Estrogen Receptors, Control of Ligand Selectivity and an Update on Subtype Selective Ligands

  2014cites this paper
• Expanding the structural footprint of xenoestrogens

  2014cites this paper
• Structural Characterization of the Binding Interactions of Various Endogenous Estrogen Metabolites with Human Estrogen Receptor α and β Subtypes: A Molecular Modeling Study

  2013cites this paper
• Protein Structural Statistics with PSS

  2013cites this paper
• Beyond the Ligand‐Binding Pocket: Targeting Alternate Sites in Nuclear Receptors

  2013cites this paper
• Phosphorylation of the Retinoic Acid Receptor Alpha Induces a Mechanical Allosteric Regulation and Changes in Internal Dynamics

  2013cites this paper
• Diosgenin relieves goiter via the inhibition of thyrocyte proliferation in a mouse model of Graves' disease

  2013cites this paper
• 3D Models of MBP, a Biologically Active Metabolite of Bisphenol A, in Human Estrogen Receptor α and Estrogen Receptor β

  2012cites this paper
• Insilico studies of daidzein and genistein with human estrogen receptor α

  2012cites this paper
• Influence of chlorine or fluorine substitution on the estrogenic properties of 1-alkyl-2,3,5-tris(4-hydroxyphenyl)-1H-pyrroles.

  2012cites this paper
• 3D models of human ERα and ERβ complexed with 5-androsten-3β,17β-diol.

  2012cites this paper
• Estrogen receptor α/β-cofactor motif interactions; interplay of tyrosine 537/488 phosphorylation and LXXLL motifs.

  2012cites this paper
• Functional Residues in Proteins

  2011cites this paper
• The Dynamic Structure of the Estrogen Receptor

  2011cites this paper
• Recent advances in the molecular modeling of estrogen receptor-mediated toxicity.

  2011cites this paper
• Design and evaluation of fragment-like estrogen receptor tetrahydroisoquinoline ligands from a scaffold-detection approach.

  2011cites this paper
• Sulfonamides as selective oestrogen receptor β agonists.

  2011cites this paper