Search Results - "Alvarez, Lautaro D"
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Structure and dynamics of neurosteroid binding to the α1β2γ2 GABAA receptor
Published in The Journal of steroid biochemistry and molecular biology (01-09-2018)“…[Display omitted] •The GABAAR-α1β2γ2 heteropentamer have four different neurosteroid binding sites.•All the sites are able to properly bind pregnanolone; two…”
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2
Live cell imaging unveils multiple domain requirements for in vivo dimerization of the glucocorticoid receptor
Published in PLoS biology (01-03-2014)“…Glucocorticoids are essential for life, but are also implicated in disease pathogenesis and may produce unwanted effects when given in high doses…”
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3
Exploring the molecular basis of action of ring D aromatic steroidal antiestrogens
Published in Proteins, structure, function, and bioinformatics (01-07-2015)“…ABSTRACT Salpichrolides are natural plant steroids that contain an unusual six‐membered aromatic ring D. We recently reported that some of these compounds, and…”
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4
Synthesis and activity evaluation of a series of cholanamides as modulators of the liver X receptors
Published in Bioorganic & medicinal chemistry (01-03-2018)“…[Display omitted] •A series of cholanamides with modified A/B rings were synthesized.•6β,19-Epoxycholanamide 4 was an LXRα selective…”
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Insights on glucocorticoid receptor activity modulation through the binding of rigid steroids
Published in PloS one (11-10-2010)“…The glucocorticoid receptor (GR) is a transcription factor that regulates gene expression in a ligand-dependent fashion. This modular protein is one of the…”
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6
Synthetic DAF-12 modulators with potential use in controlling the nematode life cycle
Published in Biochemical journal (01-01-2015)“…Dafachronic acids (DAs) are 3-keto cholestenoic acids bearing a carboxylic acid moiety at the end of the steroid side chain. These compounds interact with the…”
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7
Synthesis and biological evaluation of salpichrolide analogs as antiestrogenic agents
Published in European journal of medicinal chemistry (23-07-2014)“…The antiestrogenic activity of three natural salpichrolides A, G and B (1, 3 and 4) and of five synthetic analogs containing an aromatic D ring and a…”
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8
Structural Basis for Molecular Recognition of Cannabinoids by Inhibitory Cys-Loop Channels
Published in Journal of medicinal chemistry (14-03-2024)“…Cannabis sativa has a long history of medicinal use, dating back to ancient times. This plant produces cannabinoids, which are now known to interact with…”
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Mapping the neurosteroid binding sites on glycine receptors
Published in The Journal of steroid biochemistry and molecular biology (01-09-2019)“…[Display omitted] •Glycine receptors have five neurosteroid binding cavities.•Both overall flat and overall bent steroids are able to bind glycine…”
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10
In Search of GABA A Receptor's Neurosteroid Binding Sites
Published in Journal of medicinal chemistry (13-06-2019)“…Neurosteroids (NS) are the main modulators of γ-aminobutyric acid type A receptors (GABA Rs), which are the ligand-gated channels target of the major…”
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Structure of the Glucocorticoid Receptor, a Flexible Protein That Can Adapt to Different Ligands
Published in ChemMedChem (03-05-2010)“…Crystal structures of the glucocorticoid receptor (GR) ligand binding domain in complex with various agonists and antagonists give us an insight on how ligands…”
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In Search of GABAA Receptor's Neurosteroid Binding Sites
Published in Journal of medicinal chemistry (13-06-2019)Get full text
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13
Molecular determinants of tetrahydrocannabinol binding to the glycine receptor
Published in Proteins, structure, function, and bioinformatics (01-03-2023)“…The recognition of Cannabis as a source of new compounds suitable for medical use has attracted strong interest from the scientific community in its research,…”
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14
Structural Insights into the Ligand Binding Domain of the Glucocorticoid Receptor: A Molecular Dynamics Study
Published in Journal of chemical information and modeling (24-02-2020)“…The glucocorticoid receptor (GR) is a ligand-binding dependent transcription factor that ultimately regulates vital biological processes and inflammation…”
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Hemisuccinate of 21-Hydroxy-6,19-Epoxyprogesterone: A Tissue-Specific Modulator of the Glucocorticoid Receptor
Published in ChemMedChem (15-12-2008)“…The introduction of a hemisuccinate group at the 21‐position of the passive antiglucocorticoid 21OH‐6,19OP leads to a compound (21HS‐6,19OP) with a notable…”
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Insights into estrogen receptor alpha modulation by cholestenoic acids
Published in The Journal of steroid biochemistry and molecular biology (01-03-2022)“…[Display omitted] •The cholesterol metabolite cholestenoic acid is an ERα agonist.•Cholestenoic acid analogues with an unsaturated the side chain are also ERα…”
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Exploring the molecular basis of neurosteroid binding to the β3 homopentameric GABAA receptor
Published in The Journal of steroid biochemistry and molecular biology (01-11-2015)“…•A neurosteroid binding site was identified in the β3 Homopentameric GABAA receptor.•The site is able to bind both overall torsioned and flat steroids.•Its…”
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Expanding the Repertoire of ceDAF‐12 Ligands for Modulation of the Steroid Endocrine System in C. Elegans
Published in Chembiochem : a European journal of chemical biology (04-11-2024)“…Steroid hormones are essential for the biological processes of eukaryotic organisms. The steroid endocrine system of C. elegans, which includes dafachronic…”
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Cholestenoic acid analogues as inverse agonists of the liver X receptors
Published in The Journal of steroid biochemistry and molecular biology (01-05-2020)“…[Display omitted] •Five new analogues of cholestenoic acid were synthesized•Δ24 analogues with E configuration were inverse agonists of LXRs•Δ24 analogues with…”
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Fluorinated oxysterol analogues: Synthesis, molecular modelling and LXRβ activity
Published in The Journal of steroid biochemistry and molecular biology (01-01-2017)“…[Display omitted] •Difluoro-oxysterols were prepared by Reformatsky reaction with ultrasound irradiation.•25,25-Difluoro-27-norcholestenoic acid was an inverse…”
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