Structural Development of Liver X Receptor (LXR) Antagonists Derived from Thalidomide-Related Glucosidase Inhibitors

スポンサーリンク

概要

• 論文の詳細を見る

• Following our previous discovery of LXR antagonistic activity of 2'-substituted phenylphthalimides derived from thalidomide-related glucosidase inhibitors, structure-activity studies and further structural development led to 5-chloro-N-2'-n-pentylphenyl-1, 3-dithiophthalimide (5CPPSS-50), with IC_<50> values of about 10 and 13 μM for LXRα and LXRβ, respectively.

• 公益社団法人日本薬学会の論文
• 2007-12-01

著者

• Aoyama Hiroshi

  東京大学分子細胞生物学研究所

• Aoyama Hiroshi

  Univ. Tokyo Tokyo Jpn

• Aoyama Hiroshi

  Institute Of Molecular & Cellular Biosciences The University Of Tokyo

• MIYACHI Hiroyuki

  Institute of Molecular & Cellular Biosciences, The University of Tokyo

• HASHIMOTO Yuichi

  Institute of Molecular & Cellular Biosciences, The University of Tokyo

• Hashimoto Yuichi

  Univ. Tokyo Tokyo Jpn

• Hashimoto Y

  Univ. Tokyo Tokyo Jpn

• Hashimoto Y

  Graduate School Of Pharmaceutical Sciences Kyushu University

• 中山 太ニ

  岡山大学薬学部薬剤学教室

• Aoyama Atsushi

  Institute of Molecular and Cellular Biosciences, University of Tokyo

• NOGUCHI-YACHIDE Tomomi

  Institute of Molecular & Cellular Biosciences, The University of Tokyo

• MAKISHIMA Makoto

  Department of Biochemistry, Nihon University School of Medicine

• Miyachi Hiroyuki

  Institute Of Molecular & Cellular Biosciences University Of Tokyo

• Hashimoto Yuichi

  Institute Of Molecular & Cellular Biosciences University Of Tokyo

• Hashimoto Yuichi

  Institute Of Molecular And Cellular Biosciences The Universityv Of Tokyo

• Harada Yuichi

  Center For Influenza Virus Research National Institute Of Infectious Diseases

• Noguchi T

  Medicinal Research Laboratories Taisho Pharmaceutical Co. Ltd.

• Miyachi H

  Institute Of Molecular & Cellular Biosciences The University Of Tokyo

• Miyachi Hiroyuki

  Div. Of Pharmaceutical Sciences Graduate School Of Medicine Dentistry And Pharmaceutical Sciences Ok

• Noguchi-yachide Tomomi

  Institute Of Molecular & Cellular Biosciences The University Of Tokyo

• Hashimoto Y

  Institute Of Molecular & Cellular Biosciences The University Of Tokyo

• Makishima Makoto

  Department Of Biochemistry Nihon University School Of Medicine

• Makishima Makoto

  Div. Of Biochemistry Dep. Of Biomedical Sciences School Of Medicine Nihon Univ.

• Hashimoto Yuichi

  Institute of Molecular & Cellular Biosciences, The University of Tokyo

関連論文

• Coordination of Divalent Metal Cation to Amide Group to Form Adduct Ion in FAB Mass Spectrometry: Implication of Zn^ in Enzymatic Hydrolysis of Amide Bond
• Glycosylative Inactivation of Chalcomycin and Tylosin by a Clinically Isolated Nocardia asteroides Strain
• Structures of ADP-Ribosylated Rifampicin and Its Metabolite : Intermediates of Rifampicin-ribosylation by Mycobacterium smegmatis DSM43756
• Thermostability of Doubly Glycosylated Recombinant Lysozyme
• Expression and Characterization of Human Rheumatoid Factor Single-Chain FV
• Construction of the Single-Chain Fv from 196-14 Antibody toward Ovarian Cancer-Associated Antigen CA125
• Influence of Mutations of the N-Cap Residue, Gly4, on Stability and Structure of Hen Lysozyme
• Analysis of the Stabilization of Hen Lysozyme by Helix Macrodipole and Charged Side Chain Interaction
• Stabilization of Lysozyme by Introducing N-Glycosylation Signal Sequence
• A Mutation Study of Catalytic Residue Asp 52 in Hen Egg Lysozyme^1
• Correlation between the Differences in the Free Energy Change and conformational Energy in the Folded State of Hen Lysozymes with Gly-Pro and Pro-Gly Sequences Introduced to the Same Site
• Effect of Salt Concentration on the pK_a of Acidic Residues in Lysozyme
• EFFECT OF CYP2C POLYMORPHISMS ON THE PHARMACOKINETICS OF PHENYTOIN IN JAPANESE PATIENTS WITH EPILEPSY
• Population Pharmacokinetics of Phenytoin in Japanese Patients with Epilepsy : Analysis with a Dose-Dependent Clearance Model
• 1P084 サリドマイド・アナログの抗インフルエンザウイルス活性(蛋白質-機能(反応機構,生物活性など),第48回日本生物物理学会年会)
• Enhancing Effect of Tumor Promoters, Phorbol Esters and Teleocidins on Nuclear Receptor-Mediated Transcription
• Identification of Protein Disulfide Isomerase as a Phorbol Ester-Binding Protein
• Photoaffinity Labeling of Tumor Promoter-Binding Protein (CN-TPBP) and Preparation of Affinity Sorbent Gels
• α-Glucosidase Inhibitors with a 4, 5, 6, 7-Tetrachlorophthalimide Skeleton Pendanted with a Cycloalkyl or Dicarba-closo-dodecaborane Group
• α-Glucosidase Inhibitors with a Phthalimide Skeleton : Stucture-Activity Relationship Study
• Modulators of Tumor Necrosis Factor α Production Bearing Dicarba-closo-dodecaborane as a Hydrophobic Pharmacophore
• Involvement of the CYP1A Subfamily in Stereoselective Metabolism of Carvedilol in β-Naphthoflavone-Treated Caco-2 Cells(Biopharmacy)
• Novel Retinoidal Tropolone Derivatives. Bioisosteric Relationship of Tropolone Ring with Benzoic Acid Moiety in Retinoid Structure
• Retinoidal Pyrimidinecarboxylic Acids. Unexpected Diaza-Substituent Effects in Retinobenzoic Acids
• Retinoid X Receptor-Antagonistic Diazepinylbenzoic Acids
• NOVEL THIAZOLIDINEDIONE DERIVATIVES WITH RETINOID SYNERGISTIC ACTIVITY
• POTENT RETINOID SYNERGISTS WITH A DIPHENYLAMINE SKELETON
• Polyenylidine Thiazolidine Derivatives with Retinoidal Activities
• Photoaffinity Labeling of the Ligand-Interacting Helix of the Retinoic Acid Receptor Alpha
• Evaluation of Differentiation-Inducing Activity of Retinoids on Human Leukemia Cell Lines HL-60 and NB4
• NOVEL AROMATIC UREA DERIVATIVES WITH DNA-BINDING ABILITY
• DEIODOTRIFLUOROMETHYLATION OF ETHYL 3,3', 5-TRIIODOTHYROACETATE. DIVERGENT DERIVATIZATION BASED ON THE COMBINATORIAL CONCEPT
• Design and Synthesis of Phthalimide-Based Fluorescent Liver X Receptor Antagonists
• Structural Development of Benzhydrol-Type 1'-Acetoxychavicol Acetate (ACA) Analogs as Human Leukemia Cell-Growth Inhibitors Based on Quantitative Structure-Activity Relationship (QSAR) Analysis
• Structure-Based Design and Synthesis of Fluorescent PPARα/δ Co-agonist and Its Application as a Probe for Fluorescent Polarization Assay of PPARδ Ligands
• Fusarielin A as an Anti-angiogenic and Anti-proliferative Agent : Basic Biological Characterization
• Structural Development of Liver X Receptor (LXR) Antagonists Derived from Thalidomide-Related Glucosidase Inhibitors
• Development of Tubulin-Polymerization Inhibitors Based on the Thalidomide Skeleton
• Hydrolyzed Metabolites of Thalidomide : Synthesis and TNF-α Production-Inhibitory Activity
• Mono- and Dihydroxylated Metabolites of Thalidomide : Synthesis and TNF-α Production-Inhibitory Activity
• Effects of Immunomodulatory Derivatives of Thalidomide (IMiDs) and Their Analogs on Cell-Differentiation, Cyclooxygenase Activity and Angiogenesis
• Enhancement of All-trans Retinoic Acid-Induced HL-60 Cell Differentiation by Thalidomide and Its Metabolites(Communication to the Editor)
• N-Phenylphthalimide-Type Cyclooxygenase (COX) Inhibitors Derived from Thalidomide : Substituent Effects on Subtype Selectivity
• Thalidomide as a Nitric Oxide Synthase Inhibitor and Its Structural Development
• Conversion of Ca^ Salt of an Organic Compound to Its Li^+ Salt to Simplify the Fast Atom Bombardment Mass Spectrum
• Coordination of Sodium Cation to an Oxygen Function and Olefinic Double Bond to Form Molecular Adduct Ion in Fast Atom Bombardment Mass Spectrometry
• Separation of Phosphatidylinositol 4-Phosphate from a Mixture with Phosphatidylserine and Phosphatidylinositol by Sep-Pak C_ Cartridge
• Potent Homophthalimide-Type Inhibitors of B16F10/L5 Mouse Melanoma Cell Invasion
• OJ-003 Influences of CYP2D6 Genotype on Plasma Concentrations of Carvedilol : a Comparison with Metoprolol and Bisoprolol(Cardiovascular pharmacology, basic/clinical-2 (H) OJ1,Oral Presentation (Japanese),The 70th Anniversary Annual Scientific Meeting of
• Pharmacokinetics of R- and S-Carvedilol in Routinely Treated Japanese Patients with Heart Failure(Biopharmacy)
• Collisionally Activated Dissociation of 13-Membered Peptides, Ustiloxins, and Phomopsins
• Structural Identification of a Major Cytokinin in Coconut Milk as 14-O-{3-O-[β-D-Galactopyranosyl-(1→2)-α-D-galactopyranosyl-(1→3)-α-L-arabinofuranosyl]-4-O-(α-L-arabinofuranosyl)-β-D-galactopyranosyl}trans-zeatin Riboside
• Liver X receptor (LXR) modulators with dibenz〔b,f〕〔1,4〕oxazepin-11-one, (Z)-dibenz〔b,f〕azocin-6-one, and 11,12-dihydrodibenz〔b,f〕azocin-6-one skeletons
• Enhancement of Chemically-Induced HL-60 Cell Differentiation by 3,3′-Diindolylmethane Derivatives
• meso-DNAs with Homopurine Sequences : Analysis of Their Interaction with Natural DNAs
• Characterization of Poly-Leucine Substituted Analogues of the Human Surfactant Protein SP-C
• The Surface Properties of Chemically Synthesized Peptides Analogous to Human Pulmonary Surfactant Protein SP-C
• Synthesis and Anti-tubulin Activity of Ustiloxin D Derivatives
• Isolation and Structure of an Antimitotic Cyclic Peptide, Ustiloxin F: Chemical Interrelation with a Homologous Peptide, Ustiloxin B
• Interaction of Arenastatin A with Porcine Brain Tubulin
• INDUCER-SPECIFIC REGULATORS OF TUMOR NECROSIS FACTOR ALPHA PRODUCTION
• AUGMENTATION BY PHTHALIMIDES OF PHORBOL ESTER-INDUCED EXPRESSION OF TUMOR NECROSIS FACTOR ALPHA MESSAGE
• Location of Two Photoaffinity-Labeled Sites on the Ligand-Binding Domain of Retinoic Acid Receptor α
• Phenylphthalimides with Tumor Necrosis Factor Alpha Production-Enhancing Activity
• Development of Novel Chiral Urea Catalysts for the Hetero-Michael Reaction
• Specific Nonpeptide Inhibitors of Puromycin-Sensitive Aminopeptidase with a 2,4(1H,3H)-Quinazolinedione Skeleton
• Cyclooxygenase Inhibitors Derived from Thalidomide
• Asymmetric Synthesis of a 3-Acyltetronic Acid Derivative, RK-682, and Formation of Its Calcium Salt during Silica Gel Column Chromatography
• Anti-Androgenic Activity of Substituted Azo- and Azoxy-Benzene Derivatives
• Antiangiogenic Activity of Tumor Necrosis Factor-α Production Regulators Derived from Thalidomide
• Tumor Necrosis Factor-Alpha Production Enhancing Activity of Substituted 3'-Methylthalidomide : Influence of Substituents at the Phthaloyl Moiety on the Activity and Stereoselectivity
• Modification by Heme Oxygenase Inhibitor, Tin Protoporphyrin, of Cellular Differentiation of Human Myeloid Leukemia K562 Cell Line
• Nonlinear Mixed Effects Model Analysis of the Pharmacokinetics of Aripiprazole in Healthy Japanese Males(Biopharmacy)
• Membrane Transport Mechanisms of Mizoribine in the Rat Intestine and Human Epithelial LS180 Cells(Biopharmacy)
• The Apical Uptake Transporter of Levofloxacin is Distinct from the Peptide Transporter in Human Intestinal Epithelial Caco-2 Cells
• Directional Transcellular Transport of Bisoprolol in P-glycoprotein-expressed LLC-GA5-COL150 Cells, but not in Renal Epithelial LLC-PK_1 Cells
• Stereoselective Oxidation and Glucuronidation of Carvedilol in Human Liver and Intestinal Microsomes(Biopharmacy)
• Additional Notes on Clinical Repeated-Dose Pharmacokinetic Trials Applying a Peak-and-Trough Sampling Design to Estimate Oral Clearance
• Population Pharmacokinetics and Proton Pump Inhibitory Effects of Intravenous Lansoprazole in Healthy Japanese Males(Analytical Biochemistry)
• Pharmacokinetic Analysis of Transcellular Transport of Levofloxacin across LLC-PK_1 and Caco-2 Cell Monolayers(Biopharmacy)
• Simulation for Clinical Repeated-Dose Pharmacokinetic Trials Applying a Peak-and-Trough Sampling Design to Estimate Oral Clearance(Biopharmacy)
• UGT2B7^*3はR-, S-カルベジロールの体内動態に影響を及ぼさない
• LS180細胞におけるVDRリガンドのCYP3A4発現誘導活性の評価
• Stereoselective Metabolism of Carvedilol by the β-Naphthoflavone-Inducible Enzyme in Human Intestinal Epithelial Caco-2 Cells(Biopharmacy)
• Pharmacokinetics and Hepatic Extraction of Metoprolol in Rats with Glycerol-Induced Acute Renal Failure(Biopharmacy)
• 尿管結紮腎不全モデルラットにおけるビソプロロールの体内動態と薬効の解析
• Endogenous Uremic Substances are not Involved in the Reduced Hepatic Extraction of Metoprolol in Bilateral Ureter-Ligated Rats
• Multiple Regression Analysis of Pharmacogenetic Variability of Carvedilol Disposition in 54 Healthy Japanese Volunteers(Biopharmacy)
• Nucleophilic asymmetric epoxidation catalyzed by cyclic guanidines
• Structure-Activity Relationship of Bis-Galloyl Derivatives Related to (-)-Epigallocatechin Gallate
• Identification of Binding Proteins of Fusarielin A as Actin and Tubulin
• Inhibition of Restriction Enzymes EcoRI, BamHI and HindIII by Phenethylphenylphthalimides Derived from Thalidomide
• Glycogen Phosphorylase a Inhibitors with a Phenethylphenylphthalimide Skeleton Derived from Thalidomide-Related α-Glucosidase Inhibitors and Liver X Receptor Antagonists
• Crystallization of bovine heart mitochondrial cytochrome c oxidase for X-ray diffraction at atomic resolution (2.8A)
• A mechanism of Cytochrome c Oxidase Proposed by the Crystal Structures at Different Oxidation and Ligand Binding States
• Stereoselective Synthesis of Optically Active β-Lactams by the Reaction of Chiral Imines Derived from erythro-2-Amino-1,2-Diphenylethanol with Ester Enolates
• P-415 Target Protein Identification of Batzelladine A and D
• ILVIII-3 STRUCTURAL DEVELOPMENT STUDIES OF NUCLEAR RECEPTOR LIGANDS(Drug Discovery and Developments)
• Thymidine Phosphorylase Inhibitors with a Homophthalimide Skeleton
• Organosilicon Compounds as Adult T-Cell Leukemia Cell Proliferation Inhibitors

もっと見る 閉じる

スポンサーリンク