75 articles for thisTarget
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Design, synthesis and biological evaluation of nonsecosteroidal vitamin D
China Pharmaceutical University
Discovery of phenoxyindazoles and phenylthioindazoles as ROR¿ inverse agonists.
Galderma R & D
2-(3-Methoxyphenyl)quinazoline Derivatives: A New Class of Direct Constitutive Androstane Receptor (CAR) Agonists.
Palacky University In Olomouc
Synthesis and Biological Evaluation of Vitamin D3 Metabolite 20S,23S-Dihydroxyvitamin D3 and Its 23R Epimer.
University of Tennessee Health Science Center
SAR Exploration Guided by LE and Fsp(3): Discovery of a Selective and Orally Efficacious ROR¿ Inhibitor.
Central Pharmaceutical Research Institute
Synthesis and evaluation of vitamin D receptor-mediated activities of cholesterol and vitamin D metabolites.
University of Wisconsin
Synthesis, Biological Activities, and X-ray Crystal Structural Analysis of 25-Hydroxy-25(or 26)-adamantyl-17-[20(22),23-diynyl]-21-norvitamin D Compounds.
Rikkyo University
Effects of alkyl side chains and terminal hydrophilicity on vitamin D receptor (VDR) agonistic activity based on the diphenylpentane skeleton.
National Institute of Health Sciences
Fine tuning of agonistic/antagonistic activity for vitamin D receptor by 22-alkyl chain length of ligands: 22S-Hexyl compound unexpectedly restored agonistic activity.
Showa Pharmaceutical University
Chemical Synthesis and Biological Activities of 20S,24S/R-Dihydroxyvitamin D3 Epimers and Their 1a-Hydroxyl Derivatives.
Veterans Affairs Medical Center
Structural development of stapled short helical peptides as vitamin D receptor (VDR)-coactivator interaction inhibitors.
National Institute of Health Sciences
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORß and ROR¿t.
Phenex Pharmaceuticals
Structural insights into the molecular mechanism of vitamin D receptor activation by lithocholic acid involving a new mode of ligand recognition.
Institute of Genetics and Molecular and Cellular Biology (Igbmc)
Combination of triple bond and adamantane ring on the vitamin D side chain produced partial agonists for vitamin D receptor.
Rikkyo University
A mixed population of antagonist and agonist binding conformers in a single crystal explains partial agonism against vitamin D receptor: active vitamin D analogues with 22R-alkyl group.
Showa Pharmaceutical University
Development of novel Vitamin D Receptor-Coactivator Inhibitors.
University of Wisconsin-Milwaukee
Novel acetamidothiazole derivatives: synthesis and in vitro anticancer evaluation.
University of Mansoura
Novel nonsecosteroidal VDR agonists with phenyl-pyrrolyl pentane skeleton.
China Pharmaceutical University
Synthesis of VS-105: A novel and potent vitamin D receptor agonist with reduced hypercalcemic effects.
Vidasym
Development of stapled short helical peptides capable of inhibiting vitamin D receptor (VDR)-coactivator interactions.
National Institute of Health Sciences
Synthesis of 2?-heteroarylalkyl active vitamin d3 with therapeutic effect on enhancing bone mineral density in vivo.
Teikyo University
Synthesis and evaluation of methylsulfonylnitrobenzamides (MSNBAs) as inhibitors of the thyroid hormone receptor-coactivator interaction.
St. Jude Children'S Research Hospital
Development of silicon-containing bis-phenol derivatives as androgen receptor antagonists: selectivity switching by C/Si exchange.
The University of Tokyo
Structure-activity relationship of benzodiazepine derivatives as LXXLL peptide mimetics that inhibit the interaction of vitamin D receptor with coactivators.
The University of Tokyo
Synthesis and biological evaluation of halogenated curcumin analogs as potential nuclear receptor selective agonists.
Arizona State University
Further synthetic and biological studies on vitamin D hormone antagonists based on C24-alkylation and C2alpha-functionalization of 25-dehydro-1alpha-hydroxyvitamin D(3)-26,23-lactones.
Teikyo University
Practical synthesis and evaluation of the biological activities of 1alpha,25-dihydroxyvitamin D3 antagonists, 1alpha,25-dihydroxyvitamin D3-26,23-lactams. Designed on the basis of the helix 12-folding inhibition hypothesis.
University of Tokyo
Synthesis and biological evaluation of 1a,25-dihydroxyvitamin D3 analogues with a long side chain at C12 and short C17 side chains.
Universidad De Santiago De Compostela
Structural basis for the accommodation of bis- and tris-aromatic derivatives in vitamin D nuclear receptor.
Institute of Genetics and Molecular and Cellular Biology (Igbmc)
Discovery of the first irreversible small molecule inhibitors of the interaction between the vitamin D receptor and coactivators.
University of Wisconsin-Milwaukee
Butyl pocket formation in the vitamin D receptor strongly affects the agonistic or antagonistic behavior of ligands.
Showa Pharmaceutical University
Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.
Mcgill University
2-Methylene 19-nor-25-dehydro-1alpha-hydroxyvitamin D3 26,23-lactones: synthesis, biological activities and molecular basis of passive antagonism.
Tokyo Medical and Dental University
(2S,2'R)-analogue of LG190178 is a major active isomer.
National Institute of Health Sciences
22-Alkyl-20-epi-1alpha,25-dihydroxyvitamin D3 compounds of superagonistic activity: syntheses, biological activities and interaction with the receptor.
Tokyo Medical and Dental University
Design, synthesis and X-ray crystallographic study of new nonsecosteroidal vitamin D receptor ligands.
National Institute of Health Sciences
An o-aminoanilide analogue of 1a,25-dihydroxyvitamin D(3) functions as a strong vitamin D receptor antagonist.
Mcgill University
Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists.
Phenex Pharmaceuticals
LXXLL peptide mimetics as inhibitors of the interaction of vitamin D receptor with coactivators.
The University of Tokyo
Synthesis and anti-inflammatory properties of 1alpha,25-dihydroxy-16-ene-20-cyclopropyl-24-oxo-vitamin D3, a hypocalcemic, stable metabolite of 1alpha,25-dihydroxy-16-ene-20-cyclopropyl-vitamin D3.
Bioxell
Crystal structures of rat vitamin D receptor bound to adamantyl vitamin D analogs: structural basis for vitamin D receptor antagonism and partial agonism.
Tokyo Medical and Dental University
Structure-activity relationship studies on vitamin D lactam derivatives as vitamin D receptor antagonist.
Tokyo University of Agriculture and Technology
Low-calcemic, highly antiproliferative, 23-oxa ether analogs of the natural hormone 1 alpha,25-dihydroxyvitamin D3: design, synthesis, and preliminary biological evaluation.
The Johns Hopkins University
Low-calcemic, highly antiproliferative, 1-difluoromethyl hybrid analogs of the natural hormone 1alpha,25-dihydroxyvitamin D3: design, synthesis, and preliminary biological evaluation.
The University of Texas
Structure-activity relationships of 19-norvitamin D analogs having a fluoroethylidene group at the C-2 position.
Tokyo Medical and Dental University
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
Menoufia University
Vitamin D receptor: ligand recognition and allosteric network.
Tokyo Medical and Dental University
Paradigm shift of "classical" HDAC inhibitors to "hybrid" HDAC inhibitors in therapeutic interventions.
National Institute of Pharmaceutical Education and Research (NIPER)
Design, Synthesis, Biological Activity, and Structural Analysis of Novel Des-C-Ring and Aromatic-D-Ring Analogues of 1?,25-Dihydroxyvitamin D
University of Santiago De Compostela
Crystal structures of the vitamin D nuclear receptor liganded with the vitamin D side chain analogues calcipotriol and seocalcitol, receptor agonists of clinical importance. Insights into a structural basis for the switching of calcipotriol to a receptor antagonist by further side chain modificatio
Institute of Genetics and Molecular and Cellular Biology (Igbmc)
Novel Nonsecosteroidal Vitamin D Receptor Modulator Combined with Gemcitabine Enhances Pancreatic Cancer Therapy through Remodeling of the Tumor Microenvironment.
China Pharmaceutical University
Lithocholic Acid Derivatives as Potent Vitamin D Receptor Agonists.
Ochanomizu University
Discovery of 3?,7?,11?-Trihydroxy-6?-ethyl-5?-cholan-24-oic Acid (TC-100), a Novel Bile Acid as Potent and Highly Selective FXR Agonist for Enterohepatic Disorders.
Tes Pharma
Structural development of non-secosteroidal vitamin D receptor (VDR) ligands without any asymmetric carbon.
National Institute of Health Sciences
Development of novel lithocholic acid derivatives as vitamin D receptor agonists.
Tokyo Medical and Dental University
Novel nonsecosteroidal VDR ligands with phenyl-pyrrolyl pentane skeleton for cancer therapy.
China Pharmaceutical University
Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
China Pharmaceutical University
Synthesis and evaluation of 4-cycloheptylphenols as selective Estrogen receptor-? agonists (SERBAs).
Marquette University
Aromatic-Based Design of Highly Active and Noncalcemic Vitamin D Receptor Agonists.
University of Santiago De Compostela
25 S-Adamantyl-23-yne-26,27-dinor-1?,25-dihydroxyvitamin D
Universidad De Santiago De Compostela
Identification of the Histidine Residue in Vitamin D Receptor That Covalently Binds to Electrophilic Ligands.
Showa Pharmaceutical University
Further Developments of the Phenyl-Pyrrolyl Pentane Series of Nonsteroidal Vitamin D Receptor Modulators as Anticancer Agents.
China Pharmaceutical University
Synthesis and biological evaluation of steroidal derivatives bearing a small ring as vitamin D receptor agonists.
Kyoto University
Structural Basis of Inhibition of ER?-Coactivator Interaction by High-Affinity N-Terminus Isoaspartic Acid Tethered Helical Peptides.
Shenzhen Graduate School of Peking University
Vitamin D Analogues with a p-Hydroxyphenyl Group at the C25 Position: Crystal Structure of Vitamin D Receptor Ligand-Binding Domain Complexed with the Ligand Explains the Mechanism Underlying Full Antagonistic Action.
Showa Pharmaceutical University
Bicyclic hydroxy-1H-pyrrolopyridine-trione containing HIV-1 integrase inhibitors.
National Institutes of Health