ArticleChemMedChem2012
Comparative molecular profiling of the PPARα/γ activator aleglitazar: PPAR selectivity, activity and interaction with cofactors.
Article in ChemMedChem, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
21 citing papers in PubMed, 46 citations in OpenAlex.
- Trial
- GC-MS metabolomic profiling and PPARγ-targetedFrontiers in nutrition · 2026Article
- Novel pyrrolo[2,1-RSC advances · 2025Article
- Identification of PPAR-related differentially expressed genes liver hepatocellular carcinoma and construction of a prognostic model based on data analysis and molecular docking.Journal of cellular and molecular medicine · 2024Article
- Functional and Structural Insights into Human PPARα/δ/γ Subtype Selectivity of Bezafibrate, Fenofibric Acid, and Pemafibrate.International journal of molecular sciences · 2022Article
- Nuclear hormone and peptide hormone therapeutics for NAFLD and NASH.Molecular metabolism · 2021Review
- Nonalcoholic steatohepatitis: the role of peroxisome proliferator-activated receptors.Nature reviews. Gastroenterology & hepatology · 2021Review
- Parsing the Role of PPARs in Macrophage Processes.Frontiers in immunology · 2021Review
- Pemafibrate, a New Selective PPARα Modulator: Drug Concept and Its Clinical Applications for Dyslipidemia and Metabolic Diseases.Current atherosclerosis reports · 2020Review
- Dual PPARα/γ agonist aleglitazar confers stroke protection in a model of mild focal brain ischemia in mice.Journal of molecular medicine (Berlin, Germany) · 2019Article
- Article
- The Opportunities and Challenges of Peroxisome Proliferator-Activated Receptors Ligands in Clinical Drug Discovery and Development.International journal of molecular sciences · 2018Review
- Predicted Biological Activity of Purchasable Chemical Space.Journal of chemical information and modeling · 2018Article
- Effects of peroxisome proliferator activated receptors (PPAR)-γ and -α agonists on cochlear protection from oxidative stress.PloS one · 2017Article
- Discovery and Preclinical Evaluation of BMS-711939, an Oxybenzylglycine Based PPARα Selective Agonist.ACS medicinal chemistry letters · 2016Article
- Observational study of effects of Saroglitazar on glycaemic and lipid parameters on Indian patients with type 2 diabetes.Scientific reports · 2015Observational
- Minireview: Challenges and opportunities in development of PPAR agonists.Molecular endocrinology (Baltimore, Md.) · 2014Review
- The dual PPARα/γ agonist aleglitazar increases the number and function of endothelial progenitor cells: implications for vascular function and atherogenesis.British journal of pharmacology · 2014Article
- The nuances of atherogenic dyslipidemia in diabetes: focus on triglycerides and current management strategies.Indian heart journal · 2013Review
- Selective peroxisome proliferator-activated receptor α modulators (SPPARMα): the next generation of peroxisome proliferator-activated receptor α-agonists.Cardiovascular diabetology · 2013Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
9 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Peroxisome proliferator-activated receptors (PPARs) are a family of nuclear hormone receptors that control the expression of genes involved in a variety of physiologic processes, through heterodimerization with retinoid X receptor and complex formation with various cofactors. Drugs or treatment regimens that combine the beneficial effects of PPARα and γ agonism present an attractive therapeutic strategy to reduce cardiovascular risk factors. Aleglitazar is a dual PPARα/γ agonist currently in phase III clinical development for the treatment of patients with type 2 diabetes mellitus who recently experienced an acute coronary event. The potency and efficacy of aleglitazar was evaluated in a head-to-head comparison with other PPARα, γ and δ ligands. A comprehensive, 12-concentration dose-response analysis using a cell-based assay showed aleglitazar to be highly potent, with EC(50) values of 5 nM and 9 nM for PPARα and PPARγ, respectively. Cofactor recruitment profiles confirmed that aleglitazar is a potent and balanced activator of PPARα and γ. The efficacy and potency of aleglitazar are discussed in relation to other dual PPARα/γ agonists, in context with the published X-ray crystal structures of both PPARα and γ.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.