ArticleScientific reports2017
Structures of PPARγ complexed with lobeglitazone and pioglitazone reveal key determinants for the recognition of antidiabetic drugs.
Article in Scientific reports, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 45 papers.
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Who cites it
45 citing papers in PubMed, 102 citations in OpenAlex.
- Deciphering the relational dynamics of AF-2 domain of PAN PPAR through drug repurposing and comparative simulations.PloS one · 2023Trial
- A double-blind, Randomized controlled trial on glucose-lowering EFfects and safety of adding 0.25 or 0.5 mg lobeglitazone in type 2 diabetes patients with INadequate control on metformin and dipeptidyl peptidase-4 inhibitor therapy: REFIND study.Diabetes, obesity & metabolism · 2022 · on this mapTrial
- PPARγ Signaling in the Central Nervous System: A Review of the Implications in Synaptic Plasticity, Neuroinflammatory and Neoplastic Processes.Neurochemical research · 2026Review
- Exploring Disulfide Bridge as a Tool to Improve Pioglitazone's Neuroprotective Potential: Toward the Development of Prolonged-Acting MAO-B/PPARγ Modulators.ChemMedChem · 2026Article
- Primary cardiovascular preventive effect of thiazolidinedione in adults with type 2 diabetes: A nationwide cohort study in Korea.Journal of diabetes investigation · 2026Article
- Microalgae Oil Attenuates Liver Fat Deposition in NAFLD via Modulation of Anti-Lipogenic Genes and Insulin Signaling Pathways in HFD Mice.Food science & nutrition · 2026Article
- Computational Repurposing of Asparagus racemosus and Withania somnifera for Postpartum Depression: Insights into MAO-A and Inflammatory Signaling Modulation.Cell biochemistry and biophysics · 2026Article
- Network pharmacology refined with non-ubiquity and decoy-controlled molecular docking reveals insights intoFrontiers in bioinformatics · 2026Article
- Structural determinants of non-covalent PPARγ inverse agonism and their therapeutic implications.Nature communications · 2025Article
- Genomics-informed drug-repurposing strategy identifies two therapeutic targets for preventing liver disease associated with metabolic dysfunction.American journal of human genetics · 2025Article
- Sustainable Photocatalytic Synthesis of Glitazones via Riboflavin Tetraacetate.The Journal of organic chemistry · 2025Article
- Design and synthesis of a novel quinoline thiazolidinedione hybrid as a potential antidiabetic PPARγ modulator.Scientific reports · 2025Article
- Application of microbial pigments in the pharmaceutical industry: current status and opportunities.Archives of microbiology · 2025Review
- 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.Frontiers in chemistry · 2025Article
- The role of PPARγ in cancer cachexia: friend or foe?Frontiers in endocrinology · 2025Review
- Article
- Novel PPAR-γ agonists as potential neuroprotective agents against Alzheimer's disease: rational design, synthesisRSC advances · 2024Article
- Exploring the Antidiabetic Potential ofPlants (Basel, Switzerland) · 2024Article
- Article
- Structural Studies on the Binding Mode of Bisphenols to PPARγ.Biomolecules · 2024Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Peroxisome proliferator-activator receptor (PPAR) γ is a nuclear hormone receptor that regulates glucose homeostasis, lipid metabolism, and adipocyte function. PPARγ is a target for thiazolidinedione (TZD) class of drugs which are widely used for the treatment of type 2 diabetes. Recently, lobeglitazone was developed as a highly effective TZD with reduced side effects by Chong Kun Dang Pharmaceuticals. To identify the structural determinants for the high potency of lobeglitazone as a PPARγ agonist, we determined the crystal structures of the PPARγ ligand binding domain (LBD) in complex with lobeglitazone and pioglitazone at 1.7 and 1.8 Å resolutions, respectively. Comparison of ligand-bound PPARγ structures revealed that the binding modes of TZDs are well conserved. The TZD head group forms hydrogen bonds with the polar residues in the AF-2 pocket and helix 12, stabilizing the active conformation of the LBD. The unique p-methoxyphenoxy group of lobeglitazone makes additional hydrophobic contacts with the Ω-pocket. Docking analysis using the structures of TZD-bound PPARγ suggested that lobeglitazone displays 12 times higher affinity to PPARγ compared to rosiglitazone and pioglitazone. This structural difference correlates with the enhanced affinity and the low effective dose of lobeglitazone compared to the other TZDs.
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