Ligand binding and co-activator assembly of the peroxisome proliferator-activated receptor-γ

No abstract is available for this paper.

• Publication year

  1998

• Venue

  Nature

• Publication date

  1998-09-10

• Fields of study

  Biology, Medicine, Chemistry

• Identifiers
  DOI 10.1038/25931PMID 9744270
• 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.

• Nuclear receptor coactivators.

  2000cited by this paper
• The peroxisome proliferator-activated receptor-gamma is a negative regulator of macrophage activation.

  1998cited by this paper
• The coactivator TIF2 contains three nuclear receptor‐binding motifs and mediates transactivation through CBP binding‐dependent and ‐independent pathways

  1998cited by this paper
• Interactions controlling the assembly of nuclear-receptor heterodimers and co-activators

  1998cited by this paper
• The peroxisome proliferator-activated receptor-γ is a negative regulator of macrophage activation

  1998cited by this paper
• PPARγ Promotes Monocyte/Macrophage Differentiation and Uptake of Oxidized LDL

  1998cited by this paper
• PPARgamma promotes monocyte/macrophage differentiation and uptake of oxidized LDL.

  1998cited by this paper
• Nuclear receptor coactivator ACTR is a novel histone acetyltransferase and forms a multimeric activation complex with P/CAF and CBP/p300.

  1997cited by this paper
• A signature motif in transcriptional co-activators mediates binding to nuclear receptors

  1997cited by this paper
• GRIP1, a transcriptional coactivator for the AF-2 transactivation domain of steroid, thyroid, retinoid, and vitamin D receptors

  1997cited by this paper
• PHASES-95: a program package for processing and analyzing diffraction data from macromolecules.

  1997cited by this paper
• Molecular basis of agonism and antagonism in the oestrogen receptor

  1997cited by this paper
• AIB1, a steroid receptor coactivator amplified in breast and ovarian cancer.

  1997cited by this paper
• AF-2 activity and recruitment of steroid receptor coactivator 1 to the estrogen receptor depend on a lysine residue conserved in nuclear receptors

  1997cited by this paper
• Fatty acids and eicosanoids regulate gene expression through direct interactions with peroxisome proliferator-activated receptors alpha and gamma.

  1997cited by this paper
• Suprabasal expression of a dominant-negative RXR alpha mutant in transgenic mouse epidermis impairs regulation of gene transcription and basal keratinocyte proliferation by RAR-selective retinoids.

  1997cited by this paper
• Hypolipidemic drugs, polyunsaturated fatty acids, and eicosanoids are ligands for peroxisome proliferator-activated receptors alpha and delta.

  1997cited by this paper
• Fatty acids and eicosanoids regulate gene expression through direct interactions with peroxisome proliferator-activated receptors α and γ

  1997cited by this paper
• Nuclear receptor coactivators.

  1997cited by this paper
• Hypolipidemic drugs, polyunsaturated fatty acids, and eicosanoids are ligands for peroxisome proliferator-activated receptors α and δ

  1997cited by this paper
• The transcriptional co-activator p/CIP binds CBP and mediates nuclear-receptor function

  1997cited by this paper
• Induction of peroxisome proliferator-activated receptor gamma during the conversion of 3T3 fibroblasts into adipocytes is mediated by C/EBPbeta, C/EBPdelta, and glucocorticoids

  1996cited by this paper
• Nuclear receptor coactivators and corepressors.

  1996cited by this paper
• A CBP integrator complex mediates transcriptional activation and AP-1 inhibition by nuclear receptors.

  1996cited by this paper
• TIF2, a 160 kDa transcriptional mediator for the ligand‐dependent activation function AF‐2 of nuclear receptors.

  1996cited by this paper
• The structure - Activity relationship between peroxisome proliferator-activated receptor γ agonism and the antihyperglycemic activity of thiazolidinediones

  1996cited by this paper
• Differential activation of adipogenesis by multiple PPAR isoforms.

  1996cited by this paper
• Cloning and identification of mouse steroid receptor coactivator-1 (mSRC-1), as a coactivator of peroxisome proliferator-activated receptor gamma.

  1996cited by this paper
• Non thiazolidinedione antihyperglycaemic agents. 2: α-Carbon substituted β-phenylpropanoic acids1

  1996cited by this paper
• The Glitazone Family of Antidiabetic Agents

  1996cited by this paper
• The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones.

  1996cited by this paper
• Crystal structure of the ligand-binding domain of the human nuclear receptor RXR-α

  1995cited by this paper
• Crystal structure of the RAR-gamma ligand-binding domain bound to all-trans retinoic acid.

  1995cited by this paper
• An Antidiabetic Thiazolidinedione Is a High Affinity Ligand for Peroxisome Proliferator-activated Receptor γ (PPARγ) (*)

  1995cited by this paper
• An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor gamma (PPAR gamma).

  1995cited by this paper
• Crystal structure of the RAR-γ ligand-binding domain bound to all-trans retinoic acid

  1995cited by this paper
• A structural role for hormone in the thyroid hormone receptor

  1995cited by this paper
• Unique response pathways are established by allosteric interactions among nuclear hormone receptors.

  1995cited by this paper
• The nuclear receptor superfamily: the second decade.

  1995cited by this paper
• Functional analysis of a transactivation domain in the thyroid hormone beta receptor.

  1994cited by this paper
• Activation function 2 (AF‐2) of retinoic acid receptor and 9‐cis retinoic acid receptor: presence of a conserved autonomous constitutive activating domain and influence of the nature of the response element on AF‐2 activity.

  1994cited by this paper
• mPPAR gamma 2: tissue-specific regulator of an adipocyte enhancer.

  1994cited by this paper
• Characterization of the ligand‐dependent transactivation domain of thyroid hormone receptor.

  1994cited by this paper
• Peroxisome proliferator-activated receptor (PPAR) gamma: adipose-predominant expression and induction early in adipocyte differentiation.

  1994cited by this paper
• The CCP4 suite: programs for protein crystallography.

  1994cited by this paper
• Stimulation of adipogenesis in fibroblasts by PPAR gamma 2, a lipid-activated transcription factor.

  1994cited by this paper
• Insulin resistance and the prevention of diabetes mellitus.

  1994cited by this paper
• Differential expression and activation of a family of murine peroxisome proliferator-activated receptors.

  1994cited by this paper
• Regulation of retinoid signalling by receptor polarity and allosteric control of ligand binding

  1994cited by this paper
• Identification of a conserved region required for hormone dependent transcriptional activation by steroid hormone receptors.

  1992cited by this paper
• Improved methods for building protein models in electron density maps and the location of errors in these models.

  1991cited by this paper
• The steroid and thyroid hormone receptor superfamily.

  1988cited by this paper

• The novel SPPARM YR3-16 ameliorates metabolic disorders in vivo and attenuates adipocyte inflammation in vitro via PPARγ-dependent ERK suppression.

  2026cites this paper
• Discovery of PPARγ Partial Agonists for Treatment of Type 2 Diabetes Based on an Integrated Virtual Screening Strategy that Combines Fragment Molecular Orbital Calculations, Machine Learning, Molecular Docking, Interaction Fingerprint Filtering, and Molecular Dynamics Simulations.

  2026cites this paper
• Mapping the Allosteric Landscape of PPARγ: a Markov State Modeling and Energetic Analysis Approach.

  2026cites this paper
• Identification of antidiabetic leads using in-silico screening, molecular dynamics simulation, and biological evaluation using cell viability, anti-adipogenesis, glucose uptake, and peroxisome proliferator activated receptor-γ in-vitro assay

  2026cites this paper
• C(3)-H alkenylation of quinoxalin-2(1H)-ones with Hantzsch esters and in silico studies.

  2026cites this paper
• Unveiling the Novel Multitarget Antidepressant Mechanisms of Ligustilide in Postpartum Depression: An Integrative Network Pharmacology and Molecular Simulation Study

  2026cites this paper
• Shifting the PPARγ conformational ensemble toward a transcriptionally repressive state improves covalent inhibitor efficacy

  2026cites this paper
• A Tunable Pulmonary Organoid Model Demonstrates Compositionally Driven Epithelial Plasticity and Immune Polarization

  2025cites this paper
• Secoiridoid-enriched extra virgin olive oil extracts enhance mitochondrial activity and antioxidant response in colorectal cancer cells: The role of Oleacein and Oleocanthal in PPARγ interaction.

  2025cites this paper
• Potential PPARγ Partial Agonists from Ascidian-Associated Bacillus subtilis J08J-1-B’-4 Enhance Glucose Uptake without Adipogenesis

  2025influential citation
• Structural determinants of non-covalent PPARγ inverse agonism and their therapeutic implications

  2025cites this paper
• PPGBioPred: a webserver for predicting the bioactivity of compounds against PPARγ involved in the negative regulation of the Wnt/β-catenin signaling pathway.

  2025cites this paper
• Cyclopropane xenolipids resemble monounsaturated fatty acids and modulate peroxisome proliferator-activated receptors

  2025cites this paper
• An integrated investigation on taro vegetable (Colocasia gigantea Hook.f.) to ascertain its ethnomedicinal importance: insights into prospective phytochemicals regulating analgesic, antidiabetic, and cytotoxic actions

  2025cites this paper
• Recent advances in the design, development and therapeutic applications of PPARγ agonists.

  2025cites this paper
• Hsp90-dependent triage of the glucocorticoid receptor via the CHIP E3 ubiquitin ligase

  2025cites this paper
• A New Era for PPARγ: Covalent Ligands and Therapeutic Applications.

  2025cites this paper
• In Silico and In Vivo Evaluation of Novel 2-Aminobenzothiazole Derivative Compounds as Antidiabetic Agents

  2025cites this paper
• Thiamine as a putative natural modulator of PPARγ: exploring a nutrient-based approach for type 2 diabetes

  2025cites this paper
• Genomic Crosstalk Between Nuclear Receptors in Hormone-dependent Cancers

  2025cites this paper
• Targeting YAP/TAZ-TEAD and their protein-protein interaction for precision cancer therapy.

  2025cites this paper
• Novel Glitazones Protect Rotenone-induced Parkinsonism in Mouse Models by Targeting PGC1α.

  2025cites this paper
• A farnesoid X receptor T296I variant disrupts ligand-induced FXR activation and thus bile acid transport in progressive familial intrahepatic cholestasis

  2025cites this paper
• Photochemical fate of carbamazepine-10,11-epoxide mediated by triplet-state dissolved organic matter in sunlit natural waters.

  2025cites this paper
• Design, synthesis, bioassay, and in silico studies of thiazolidinedione–morpholine hybrid ionic liquids as new antidiabetic agents

  2025cites this paper
• Predicting peroxisome proliferator-activated receptor gamma potency of small molecules: a synergistic consensus model and deep learning binding affinity approach powered by Enalos Cloud Platform.

  2025cites this paper
• Structural insights into retinoic acid receptor activation and selective modulators

  2025cites this paper
• Imaging Ligand-Driven PPAR Activities Using Single-Chain Bioluminescent Probes

  2025cites this paper
• Nuclear receptor coregulator interactions: beyond the switch

  2025cites this paper
• Small molecule inhibitor of PPARγ acetylation promotes insulin sensitization and browning of white adipose tissue with improved safety

  2025cites this paper
• Potentials of peroxisome proliferator-activated receptor (PPAR) α, β/δ, and γ: An in-depth and comprehensive review of their molecular mechanisms, cellular Signalling, immune responses and therapeutic implications in multiple diseases.

  2025cites this paper
• Impaired transitioning of the FXR ligand binding domain to an active state underlies an FXR-associated PFIC phenotype

  2025cites this paper
• Identification of PTGR2 inhibitors as a new therapeutic strategy for diabetes and obesity

  2025cites this paper
• Molecular interactions between piperine and peroxisome proliferator-activated receptor gamma ligand-binding domain revealed using co-crystallization studies.

  2025cites this paper
• Shifting the PPARγ conformational ensemble towards a transcriptionally repressive state improves covalent inhibitor efficacy

  2025cites this paper
• Impact of the Ketogenic Diet on Neurological Diseases: A Review

  2025influential citation
• UHPLC-QTOF-MS/MS profiling, molecular networking, and molecular docking analysis of Gliricidia sepium (Jacq.) Kunth. ex. Walp. stem ethanolic extract and its gastroprotective effect on gastritis in rats

  2025cites this paper
• The Furan Fatty Acids 11M5 and 11D5 Can Act as Activators of Human Peroxisome Proliferator‐Activated Receptor Gamma

  2025cites this paper
• Discovery of a novel binding pocket in PPARγ for partial agonists: structure-based virtual screening identifies ginsenoside Rg5 as a partial agonist promoting beige adipogenesis

  2025cites this paper
• Structure-Based Design and Optimization Lead to the Identification of a Novel Potent sEH Inhibitor with PPARγ Partial Agonist Activity against Inflammatory and Metabolic-Related Diseases.

  2025cites this paper
• Therapeutic potential of Baicalin against experimental obsessive compulsive disorder: Evidence from CSF, blood plasma, and brain analysis.

  2025cites this paper
• Exposure to novel brominated flame retardants (NBFRs) drives obesity via PPARγ-mediated adipogenesis: A cross-ethnic study in aging agro-pastoral communities

  2025cites this paper
• Evaluation of binding interaction between compounds targeting peroxisome proliferator-activated receptor γ in Nelumbinis folium using receptor chromatography and molecular dynamic simulation.

  2025cites this paper
• Design and synthesis of a novel quinoline thiazolidinedione hybrid as a potential antidiabetic PPARγ modulator

  2025cites this paper
• Structure-based discovery of a novel nuclear receptor PPARγ inhibitor: Implications for obesity and metabolic disease intervention.

  2025cites this paper
• Multimolecular interactions from Chinese medicines activate nuclear receptor conformational changes: a potential strategy for anti-inflammatory therapy

  2025cites this paper
• From Apo to Ligand-Bound: Unraveling PPARγ-LBD Conformational Shifts via Advanced Molecular Dynamics

  2025cites this paper
• Design, synthesis, antidiabetic, and in silico studies of 5-arylidene thiazolidinedione acetic acid 1,2-diol monoesters as new antidiabetic agents

  2025cites this paper
• Unanticipated mechanisms of covalent inhibitor and synthetic ligand cobinding to PPARγ

  2024cites this paper
• Fluoxetine attenuates chlorpyrifos-induced neuronal injury through the PPARγ, SIRT1, NF-κB, and JAK1/STAT3 signals.

  2024cites this paper
• Preclinical Multi-Omic Assessment of Pioglitazone in Skeletal Muscles of Mice Implanted with Human HER2/neu Overexpressing Breast Cancer Xenografts

  2024cites this paper
• Decoration of GW9662 scaffold with a fragment-like hit via copper-catalyzed azide-alkyne cycloaddition reaction into peroxisome proliferator-activated receptor γ agonists

  2024cites this paper
• Discovery of New Dual-Target Agents Against PPAR-γ and α-Glucosidase Enzymes with Molecular Modeling Methods: Molecular Docking, Molecular Dynamic Simulations, and MM/PBSA Analysis

  2024cites this paper
• The first dimeric indole-diterpenoids from a marine-derived Penicillium sp. fungus and their potential for anti-obesity drugs

  2024influential citation
• Novel PPAR-γ agonists as potential neuroprotective agents against Alzheimer's disease: rational design, synthesis, in silico evaluation, PPAR-γ binding assay and transactivation and expression studies

  2024cites this paper
• The N-terminal activation function AF-1 domain of ERα interacts directly with the C-terminal AF-2-holding ligand-binding domain to recruit the coactivator proteins

  2024cites this paper
• Cladosporols and PPARγ: Same Gun, Same Bullet, More Targets

  2024cites this paper
• Structural Studies on the Binding Mode of Bisphenols to PPARγ

  2024influential citation
• HESPERETIN DERIVATIVES AS PPAR γ AGONIST: A PHARMACOPHORE APPROACH

  2024cites this paper
• An autoinhibitory switch of the LSD1 disordered region controls enhancer silencing.

  2024cites this paper
• Enhanced detection of ligand-PPARγ binding based on surface plasmon resonance through complexation with SRC1- or NCOR2-related polypeptide.

  2024cites this paper
• A Combined Molecular Dynamics and Hydropathic INTeraction (HINT) Approach to Investigate Protein Flexibility: The PPARγ Case Study

  2024cites this paper
• Synthesis and In Vitro and Silico Anti-inflammatory Activity of New Thiazolidinedione-quinoline Derivatives.

  2024cites this paper
• Flavokawain B is an effective natural peroxisome proliferator-activated receptor γ-selective agonist with a strong glucose-lowering effect.

  2024cites this paper
• Different Coactivator Recruitment to Human PPARα/δ/γ Ligand-Binding Domains by Eight PPAR Agonists to Treat Nonalcoholic Fatty Liver Disease

  2024cites this paper
• A structural basis for the activation of peroxisome proliferator-activated receptor gamma (PPARγ) by perfluorooctanoic acid (PFOA).

  2024cites this paper
• PPARγ Modulators in Lung Cancer: Molecular Mechanisms, Clinical Prospects, and Challenges

  2024cites this paper
• Simvastatin mitigates diabetic nephropathy by upregulating farnesoid X receptor and Nrf2/HO-1 signaling and attenuating oxidative stress and inflammation in rats.

  2024cites this paper
• How nuclear receptors transition between active and inactive forms: An energetic perspective.

  2024cites this paper
• A pan-PPAR agonist E17241 ameliorates hyperglycemia and diabetic dyslipidemia in KKAy mice via up-regulating ABCA1 in islet, liver, and white adipose tissue.

  2024cites this paper
• In Silico and In Vitro Investigation of Phytoconstituents from Flacourtia Jangomas as a Potential Candidate for the Treatment of Type 2 Diabetes Mellitus

  2024cites this paper
• Investigating the anti-obesity potential of Nelumbo nucifera leaf bioactive compounds through machine learning and computational biology methods

  2024cites this paper
• Recent advances and therapeutic applications of PPARγ-targeted ligands based on the inhibition mechanism of Ser273 phosphorylation.

  2024cites this paper
• Integrative in-silico and in-vitro analysis of taurine and vitamin B12 in modulating PPARγ and Wnt signaling in hyperhomocysteinemia-induced osteoporosis

  2024cites this paper
• Preclinical Multi-Omic Assessment of Pioglitazone in Skeletal Muscles of Mice Implanted with Human HER2/neu Overexpressing Breast Cancer Xenografts

  2024cites this paper
• Benzopyran hydrazones with dual PPARα/γ or PPARα/δ agonism and an anti-inflammatory effect on human THP-1 macrophages.

  2024cites this paper
• Unanticipated mechanisms of covalent inhibitor and synthetic ligand cobinding to PPARγ

  2024cites this paper
• Antioxidant, Alpha‐Amylase Inhibitory and Hypoglycemic Activity of Smallanthus sonchifolius Leaves from Nepal: An Integrated In Vitro, In Vivo, and In Silico Approach

  2024influential citation
• Design, Synthesis and Computational Insight of Isolated and Thiophene fused 2H‐Pyran‐2‐ones as PPAR‐γ Agonist

  2024cites this paper
• Insights into the chirality-dependent recognition of Danshensu Bingpian Zhi stereoisomers with PPARγ.

  2024cites this paper
• Enhanced Neuroprotection in Experiment Multiple Sclerosis through Combined Rosiglitazone and Probiotic-Loaded Solid Lipid Nanoparticles: Modulation of Cellular Signaling Pathways.

  2024cites this paper
• Crosstalk interactions between transcription factors ERRα and PPARα assist PPARα-mediated gene expression

  2024cites this paper
• Molecular Dynamics Simulations Reveal the Importance of Non-Native Interactions in Modulating the Inactive to Active Conformational Transition in Progesterone Receptor

  2024cites this paper
• Advancements of anticancer agents by targeting the Hippo signalling pathway: biological activity, selectivity, docking analysis, and structure–activity relationship

  2024cites this paper
• Exploring the molecular pathways of the activation process in PPARγ recurrent bladder cancer mutants.

  2024cites this paper
• Computational Drug Design Approaches for the Identification of Novel Antidiabetic Compounds from Natural Resources through Molecular Docking, ADMET, and Toxicological Studies

  2024influential citation
• Expression of Peroxisome Proliferator-Activated Receptor γ in Human Colorectal Carcinoma and Its Correlation with Clinicopathological Characteristics

  2024cites this paper
• Dietary regulation of peroxisome proliferator-activated receptors in metabolic syndrome.

  2023cites this paper
• PPARγ Corepression Involves Alternate Ligand Conformation and Inflation of H12 Ensembles.

  2023cites this paper
• Selenium Organic Content Prediction in Jengkol (Archidendron pauciflorum) and Its Molecular Interaction with Cardioprotection Receptors PPAR-γ, NF-κB, and PI3K

  2023influential citation
• Discriminating functional and non-functional nuclear-receptor ligands with a conformational selection-inspired machine learning algorithm

  2023cites this paper
• Want of Wnt in Parkinson's disease: Could sFRP disrupt interplay between Nurr1 and Wnt signaling?

  2023cites this paper
• Insight into the binding model of per- and polyfluoroalkyl substances to proteins and membranes.

  2023cites this paper
• FXR agonists for colorectal and liver cancers, as a stand-alone or in combination therapy.

  2023cites this paper
• Biological Screening and Crystallographic Studies of Hydroxy γ-Lactone Derivatives to Investigate PPARγ Phosphorylation Inhibition

  2023cites this paper
• Mechanistic insights into chloramphenicol-mediated inactivation of cytochrome P450 enzymes and their active site mutants

  2023cites this paper
• Discovery of FXR/PPARγ dual partial agonist.

  2023cites this paper
• Structural basis of the activation of PPARγ by the plasticizer metabolites MEHP and MINCH.

  2023cites this paper
• Appraisal of the Possible Role of PPARγ Upregulation by CLA of Probiotic Pediococcus pentosaceus GS4 in Colon Cancer Mitigation

  2023cites this paper
• Computational studies, synthesis, in-vitro binding and transcription analysis of novel imidazolidine-2,4-dione and 2-thioxo thiazolidine-4-one based glitazones for central PPAR-γ agonism

  2023cites this paper