Targeting Peroxisome Proliferator-Activated Receptors (PPARs): Development of Modulators

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Oleylethanolamide regulates feeding and body weight through activation of the nuclear receptor PPAR-α

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PPARs: therapeutic targets for metabolic disease

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Therapeutic roles of peroxisome proliferator-activated receptor agonists

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Structural basis for antagonist-mediated recruitment of nuclear co-repressors by PPARα

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Asymmetry in the PPARγ/RXRα Crystal Structure Reveals the Molecular Basis of Heterodimerization among Nuclear Receptors

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Effect of Muraglitazar on Death and Major Adverse Cardiovascular Events in Patients With Type 2 Diabetes Mellitus

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Structural determinants of ligand binding selectivity between the peroxisome proliferator-activated receptors

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Intestinal antiinflammatory effect of 5-aminosalicylic acid is dependent on peroxisome proliferator–activated receptor-γ

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Cannabinoids go nuclear: evidence for activation of peroxisome proliferator‐activated receptors

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PPARδ regulates glucose metabolism and insulin sensitivity

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Peroxisome proliterator-activated receptor-alpha activators regulate genes governing lipoprotein metabolism, vascular inflammation and atherosclerosis

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PPARγ AND G LUCOSE H OMEOSTASIS

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A Synthetic Antagonist for the Peroxisome Proliferator-activated Receptor γ Inhibits Adipocyte Differentiation

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Interdomain communication regulating ligand binding by PPAR-γ

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Modification of Metabolism and Distribution of Lipids by Ethyl Chlorophenoxyisobutyrate

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Distinct Properties and Advantages of a Novel Peroxisome Proliferator-Activated Protein γ Selective Modulator

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T0070907, a Selective Ligand for Peroxisome Proliferator-activated Receptor γ, Functions as an Antagonist of Biochemical and Cellular Activities

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Safety issues and prospects for future generations of PPAR modulators

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N-(2-Benzoylphenyl)- l -tyrosine PPARγ Agonists. 1. Discovery of a Novel Series of Potent Antihyperglycemic and Antihyperlipidemic Agents

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Studies on Antidiabetic Agents. X. Synthesis and Biological Activities of Pioglitazone and Related Compounds.

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A Unique PPARγ Ligand with Potent Insulin-Sensitizing yet Weak Adipogenic Activity

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Molecular Characterization of New Selective Peroxisome Proliferator–Activated Receptor γ Modulators With Angiotensin Receptor Blocking Activity

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[[.omega.-(Heterocyclylamino)alkoxy]benzyl]-2,4-thiazolidinediones as potent antihyperglycemic agents

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Peroxisome Proliferator-Activated Receptor-γ Calls for Activation in Moderation: Lessons from Genetics and Pharmacology

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A novel insulin sensitizer acts as a coligand for peroxisome proliferator-activated receptor-alpha (PPAR-alpha) and PPAR-gamma: effect of PPAR-alpha activation on abnormal lipid metabolism in liver of Zucker fatty rats.

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Studies on hindered phenols and analogs. 1. Hypolipidemic and hypoglycemic agents with ability to inhibit lipid peroxidation

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A New Selective Peroxisome Proliferator-Activated Receptor γ Antagonist with Antiobesity and Antidiabetic Activity

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Roles of PPAR delta in lipid absorption and metabolism: a new target for the treatment of type 2 diabetes

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Peroxisome proliferator-activated receptors: three isotypes for a multitude of functions

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Fenofibrate and Rosiglitazone Lower Serum Triglycerides with Opposing Effects on Body Weight

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PPAR agonists: multimodal drugs for the treatment of type-2 diabetes

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Identification of a subtype selective human PPARα agonist through parallel-array synthesis

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The Metabolic Syndrome: Peroxisome Proliferator-Activated Receptor γ and Its Therapeutic Modulation

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A novel N-aryl tyrosine activator of peroxisome proliferator-activated receptor-gamma reverses the diabetic phenotype of the Zucker diabetic fatty rat.

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A new thiazolidinedione, NC-2100, which is a weak PPAR-gamma activator, exhibits potent antidiabetic effects and induces uncoupling protein 1 in white adipose tissue of KKAy obese mice.

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Selective peroxisome proliferator-activated receptor γ (PPARγ) modulation as a strategy for safer therapeutic PPARγ activation

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A Novel Partial Agonist of Peroxisome Proliferator-Activated Receptor-γ (PPARγ) Recruits PPARγ-Coactivator-1α, Prevents Triglyceride Accumulation, and Potentiates Insulin Signaling in Vitro

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Scaffold-based discovery of indeglitazar, a PPAR pan-active anti-diabetic agent

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Novel Tricyclic-α-alkyloxyphenylpropionic Acids: Dual PPARα/γ Agonists with Hypolipidemic and Antidiabetic Activity

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Identification and Characterization of a Selective Peroxisome Proliferator-Activated Receptor β/δ (NR1C2) Antagonist

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Neuroprotective Efficacy of the Peroxisome Proliferator-Activated Receptor δ-Selective Agonists in Vitro and in Vivo

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(−)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic Acid [(−)DRF 2725]: A Dual PPAR Agonist with Potent Antihyperglycemic and Lipid Modulating Activity

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Indenone Derivatives: A Novel Template for Peroxisome Proliferator-Activated Receptor γ (PPARγ) Agonists

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A Selective Peroxisome Proliferator-Activated Receptor-γ (PPARγ) Modulator Blocks Adipocyte Differentiation but Stimulates Glucose Uptake in 3T3-L1 Adipocytes

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Substituted 2-[(4-Aminomethyl)phenoxy]-2-methylpropionic Acid PPARα Agonists. 1. Discovery of a Novel Series of Potent HDLc Raising Agents

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INT131: A Selective Modulator of PPARγ

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Regulation of Human ApoA-I by Gemfibrozil and Fenofibrate Through Selective Peroxisome Proliferator-Activated Receptor α Modulation

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Tesaglitazar, a novel dual peroxisome proliferator-activated receptor α/γ agonist, dose-dependently improves the metabolic abnormalities associated with insulin resistance in a non-diabetic population

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Insights into the Mechanism of Partial Agonism

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N-(2-Benzoylphenyl)- l -tyrosine PPARγ Agonists. 3. Structure−Activity Relationship and Optimization of the N-Aryl Substituent

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Identification of peroxisome proliferator-activated receptor ligands from a biased chemical library

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The Triterpenoid 2-Cyano-3,12-dioxooleana-1,9-dien-28-oic-acid Methyl Ester Has Potent Anti-diabetic Effects in Diet-induced Diabetic Mice and Lepr Mice

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The next generation of PPAR drugs: Do we have the tools to find them?

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Role of the PPAR family of nuclear receptors in the regulation of metabolic and cardiovascular homeostasis: new approaches to therapy

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Novel 2,3-Dihydrobenzofuran-2-carboxylic Acids: Highly Potent and Subtype-Selective PPARα Agonists with Potent Hypolipidemic Activity

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Structure-Based Drug Design of a Novel Family of PPARγ Partial Agonists: Virtual Screening, X-ray Crystallography, and in Vitro/in Vivo Biological Activities

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Effects of peroxisome proliferator‐activated receptor‐α and ‐γ agonist, JTT‐501, on diabetic complications in Zucker diabetic fatty rats

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Novel Indole-Based Peroxisome Proliferator-Activated Receptor Agonists: Design, SAR, Structural Biology, and Biological Activities

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Activation of Peroxisome Proliferator-Activated Receptor-δ by GW501516 Prevents Fatty Acid-Induced Nuclear Factor-κB Activation and Insulin Resistance in Skeletal Muscle Cells

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A Novel Potent Antagonist of Peroxisome Proliferator-Activated Receptor γ Blocks Adipocyte Differentiation But Does Not Revert the Phenotype of Terminally Differentiated Adipocytes

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MBX-102/JNJ39659100, a Novel Peroxisome Proliferator-Activated Receptor-Ligand with Weak Transactivation Activity Retains Antidiabetic Properties in the Absence of Weight Gain and Edema

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A New Class of Peroxisome Proliferator-activated Receptor Agonists with a Novel Binding Epitope Shows Antidiabetic Effects

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Pharmacological PPARγ modulation regulates sebogenesis and inflammation in SZ95 human sebocytes

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Preclinical Studies of a Specific PPARγ Modulator in the Control of Skin Inflammation

Mastrofrancesco, A., Kovacs, D., Sarra, M., Bastonini, E., Cardinali, G., Aspite, N., Camera, E., Chavatte, P., Desreumaux, P., Monteleone, G., et al. (2013) · Journal of Investigative Dermatology · doi:10.1038/jid.2013.448 · Cited by 49 · see citing works

Discovery of INT131: A selective PPARγ modulator that enhances insulin sensitivity

Taygerly, J. P., McGee, L. R., Rubenstein, S. M., Houze, J. B., Cushing, T. D., Li, Y., Motani, A. S., Chen, J., Frankmoelle, W. P., Ye, G., et al. (2012) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2012.11.058 · Cited by 45 · see citing works

A novel structural class of coumarin-chalcone fibrates as PPARα/γ agonists with potent antioxidant activities: Design, synthesis, biological evaluation and molecular docking studies

Niu, H., Wang, W., Li, J., Lei, Y., Zhao, Y., Yang, W., Zhao, C., Lin, B., Song, S., & Wang, S. (2017) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2017.06.033 · Cited by 45 · see citing works

The role and mechanism of fatty acid oxidation in cancer drug resistance

Lei, Y., Cai, S., Zhang, J., Ding, S., Zhang, Z.-H., Zhang, C., Dai, D., & Li, Y. (2025) · Cell Death Discovery · doi:10.1038/s41420-025-02554-1 · Cited by 44 · see citing works

A Selective Novel Peroxisome Proliferator-Activated Receptor (PPAR)-α Antagonist Induces Apoptosis and Inhibits Proliferation of CLL Cells In Vitro and In Vivo

Messmer, D., Lorrain, K., Stebbins, K. J., Bravo, Y., Stock, N. S., Cabrera, G., Correa, L. D., Chen, A. C., Jacintho, J. D., Chiorazzi, N., et al. (2015) · Molecular Medicine · doi:10.2119/molmed.2015.00139 · Cited by 42 · see citing works

Photohormones Enable Optical Control of the Peroxisome Proliferator-Activated Receptor γ (PPARγ)

Hinnah, K., Willems, S., Morstein, J., Heering, J., Hartrampf, F. W. W., Broichhagen, J., Leippe, P., Merk, D., & Trauner, D. H. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c00654 · Cited by 41 · see citing works

Structural development studies of PPARs ligands based on tyrosine scaffold

Filippis, B. D., Linciano, P., Ammazzalorso, A., Giovanni, C. D., Fantacuzzi, M., Giampietro, L., Laghezza, A., Maccallini, C., Tortorella, P., Lavecchia, A., et al. (2014) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2014.10.083 · Cited by 39 · see citing works

Sebocyte differentiation as a new target for acne therapy: an in vivo experience

Ottaviani, M., Flori, E., Mastrofrancesco, A., Briganti, S., Lora, V., Capitanio, B., Zouboulis, C. C., & Picardo, M. (2020) · Journal of the European Academy of Dermatology and Venereology · doi:10.1111/jdv.16252 · Cited by 39 · see citing works

The effects of olive leaf extract on cardiovascular risk factors in the general adult population: a systematic review and meta-analysis of randomized controlled trials

Razmpoosh, E., Abdollahi, S., Mousavirad, M., Clark, C. C. T., & Soltani, S. (2022) · Diabetology & Metabolic Syndrome · doi:10.1186/s13098-022-00920-y · Cited by 38 · see citing works

Identification and structural insight of an effective PPARγ modulator with improved therapeutic index for anti-diabetic drug discovery

Jiang, H., Zhou, X. E., Shi, J., Zhou, Z., Zhao, G., Zhang, X., Sun, Y., Suino-Powell, K. M., Ma, L., Gao, H., et al. (2020) · Chemical Science · doi:10.1039/c9sc05487a · Cited by 35 · see citing works

Design, Synthesis, and Biological Evaluation of Triazolone Derivatives as Potent PPARα/δ Dual Agonists for the Treatment of Nonalcoholic Steatohepatitis

Feng, Z., Xiang, J., Liu, H., Li, J., Xu, X., Sun, G., Zheng, R., Zhang, S., Liu, J., Yang, S., et al. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c02002 · Cited by 35 · see citing works

Synthesis and structure–activity relationships of fibrate-based analogues inside PPARs

Giampietro, L., D’Angelo, A., Giancristofaro, A., Ammazzalorso, A., Filippis, B. D., Fantacuzzi, M., Linciano, P., Maccallini, C., & Amoroso, R. (2012) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2012.09.111 · Cited by 34 · see citing works

Pioglitazone Alleviates Cardiac Fibrosis and Inhibits Endothelial to Mesenchymal Transition Induced by Pressure Overload

Wei, W., Zhang, N., Li, L., Ma, Z., Xu, M., Yuan, Y., Deng, W., & Tang, Q. (2017) · Cellular Physiology and Biochemistry · doi:10.1159/000486220 · Cited by 33 · see citing works

Structural and functional insights into PPAR-γ: Review of its potential and drug design innovations for the development of antidiabetic agents

Gupta, O., Pradhan, T., & Chawla, G. (2025) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2025.118264 · Cited by 32 · see citing works

SAR and Computer-Aided Drug Design Approaches in the Discovery of Peroxisome Proliferator-Activated Receptor γ Activators: A Perspective

Dixit, V. A., & Bharatam, P. V. (2013) · Journal of Computational Medicine · doi:10.1155/2013/406049 · Cited by 32 · see citing works

PPAR Ligands Induce Antiviral Effects Targeting Perturbed Lipid Metabolism during SARS-CoV-2, HCV, and HCMV Infection

Fantacuzzi, M., Amoroso, R., & Ammazzalorso, A. (2022) · Biology · doi:10.3390/biology11010114 · Cited by 32 · see citing works

Design, Synthesis, and Biological Evaluation of Indole Biphenylcarboxylic Acids as PPARγ Antagonists

Asteian, A., Blayo, A., He, Y., Koenig, M., Shin, Y., Kuruvilla, D. S., Corzo, C. A., Cameron, M. D., Li, L., Ruiz, C. H., et al. (2015) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.5b00218 · Cited by 31 · see citing works

Advanced Inhibition of Undesired Human Hair Growth by PPARγ Modulation?

Ramot, Y., Mastrofrancesco, A., Herczeg-Lisztes, E., Bı́ró, T., Picardo, M., Kloepper, J. E., & Paus, R. (2013) · Journal of Investigative Dermatology · doi:10.1038/jid.2013.473 · Cited by 30 · see citing works

Olive Oil Polyphenols Improve HDL Cholesterol and Promote Maintenance of Lipid Metabolism: A Systematic Review and Meta-Analysis of Randomized Controlled Trials

Zupo, R., Castellana, F., Crupi, P., Desantis, A., Rondanelli, M., Corbo, F., & Clodoveo, M. L. (2023) · Metabolites · doi:10.3390/metabo13121187 · Cited by 30 · see citing works

Efficacy and safety of N-acetyl-GED-0507-34-LEVO gel in patients with moderate-to severe facial acne vulgaris: a phase IIb randomized double-blind, vehicle-controlled trial

Picardo, M., Cardinali, C., Plaça, M. L., Lewartowska-Białek, A., Lora, V., Micali, G., Montisci, R., Morbelli, L., Nova, A., Parodi, A., et al. (2022) · British Journal of Dermatology · doi:10.1111/bjd.21663 · Cited by 29 · see citing works

New Approaches to Cancer Therapy: Combining Fatty Acid Amide Hydrolase (FAAH) Inhibition with Peroxisome Proliferator-Activated Receptors (PPARs) Activation

Brunetti, L., Loiodice, F., Piemontese, L., Tortorella, P., & Laghezza, A. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b00885 · Cited by 28 · see citing works

Metabolic reprogramming in the arsenic carcinogenesis

Ruan, Y., Fang, X. H., Guo, T., Liu, Y., Hu, Y., Wang, X., Hu, Y., Gao, L., Li, Y., Pi, J., et al. (2021) · Ecotoxicology and Environmental Safety · doi:10.1016/j.ecoenv.2021.113098 · Cited by 28 · see citing works

Effect of PPARγ on oxidative stress in diabetes-related dry eye

Wang, J., Chen, S., Zhao, X., Guo, Q., Yang, R., Zhang, C., Huang, Y., Ma, L., & Zhao, S. (2023) · Experimental Eye Research · doi:10.1016/j.exer.2023.109498 · Cited by 28 · see citing works

Blocking the Peroxisome Proliferator‐Activated Receptor (PPAR): An Overview

Ammazzalorso, A., Filippis, B. D., Giampietro, L., & Amoroso, R. (2013) · ChemMedChem · doi:10.1002/cmdc.201300250 · Cited by 27 · see citing works

Discovery of 4-benzyloxy and 4-(2-phenylethoxy) chalcone fibrate hybrids as novel PPARα agonists with anti-hyperlipidemic and antioxidant activities: Design, synthesis and in vitro/in vivo biological evaluation

Hassan, R. M., Aboutabl, M. E., Bozzi, M., El‐Behairy, M. F., Kerdawy, A. M. E., Sampaolese, B., Desiderio, C., Vincenzoni, F., Sciandra, F., & Ghannam, I. A. Y. (2021) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2021.105170 · Cited by 27 · see citing works

Design, Synthesis and Biological Evaluation of Phenoxyacetic Acid derivatives Linked to Pyrazole Scaffold as PPAR-α/γ Agonists and COX-2 Inhibitors with Dual Antidiabetic/Anti-inflammatory Activities

Fadaly, W. A. A., Amin, D. M. E., Bakr, R. B., Nemr, M. T. M., Ismail, B. S., & Mohamed, M. F. A. (2025) · Journal of Molecular Structure · doi:10.1016/j.molstruc.2025.142578 · Cited by 26 · see citing works

Polycerasoidol, a Natural Prenylated Benzopyran with a Dual PPARα/PPARγ Agonist Activity and Anti-inflammatory Effect

Bermejo, A., Collado, A., Barrachina, I., Marqués, P., Aouad, N. E., Franck, X., Garibotto, F. M., Dacquet, C., Caignard, D. H., Suvire, F. D., et al. (2019) · Journal of Natural Products · doi:10.1021/acs.jnatprod.9b00003 · Cited by 26 · see citing works

Impact of Obesity on the Course of Management of Inflammatory Bowel Disease—A Review

Michalak, A., Kasztelan‐Szczerbińska, B., & Cichoż‐Lach, H. (2022) · Nutrients · doi:10.3390/nu14193983 · Cited by 26 · see citing works

The discovery of novel isoflavone pan peroxisome proliferator-activated receptor agonists

Matin, A., Doddareddy, M. R., Gavande, N. S., Nammi, S., Groundwater, P. W., Roubin, R. H., & Hibbs, D. E. (2012) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2012.11.040 · Cited by 26 · see citing works

Identification of a novel selective PPARγ ligand with a unique binding mode and improved therapeutic profile in vitro

Yi, W., Shi, J., Zhao, G., Zhou, X. E., Suino-Powell, K. M., Melcher, K., & Xu, H. E. (2017) · Scientific Reports · doi:10.1038/srep41487 · Cited by 26 · see citing works

Discovery of novel allosteric site and covalent inhibitors of FBPase with potent hypoglycemic effects

Huang, Y., Wei, L., Han, X., Chen, H., Ren, Y., Xu, Y., Song, R., Rao, L., Chen, S., Peng, C., et al. (2019) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2019.111749 · Cited by 25 · see citing works

Fibrate-derived N-(methylsulfonyl)amides with antagonistic properties on PPARα

Ammazzalorso, A., D’Angelo, A., Giancristofaro, A., Filippis, B. D., Matteo, M. D., Fantacuzzi, M., Giampietro, L., Linciano, P., Maccallini, C., & Amoroso, R. (2012) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2012.10.019 · Cited by 25 · see citing works

Cytotoxic effect of a family of peroxisome proliferator‐activated receptor antagonists in colorectal and pancreatic cancer cell lines

Ammazzalorso, A., Lellis, L. D., Florio, R., Bruno, I., Filippis, B. D., Fantacuzzi, M., Giampietro, L., Maccallini, C., Perconti, S., Verginelli, F., et al. (2017) · Chemical Biology & Drug Design · doi:10.1111/cbdd.13026 · Cited by 25 · see citing works

Picrasidine N Is a Subtype-Selective PPARβ/δ Agonist

Zhao, S., Kanno, Y., Li, W., 若旅穂奈美, Sasaki, T., Koike, K., Nemoto, K., & Li, H. (2016) · Journal of Natural Products · doi:10.1021/acs.jnatprod.5b00909 · Cited by 25 · see citing works

The Emerging Role of COX-2, 15-LOX and PPARγ in Metabolic Diseases and Cancer: An Introduction to Novel Multi-target Directed Ligands (MTDLs)

Alaaeddine, R. A., Elzahhar, P. A., AlZaim, I., Abou-Kheir, W. G., Belal, A. S. F., & EL‐Yazbi, A. F. (2020) · Current Medicinal Chemistry · doi:10.2174/0929867327999200820173853 · Cited by 26 · see citing works

Design and synthesis of novel quinazolinone‐based fibrates as PPARα agonists with antihyperlipidemic activity

Hassan, R. M., Ali, I. H., Abdel‐Maksoud, M. S., Abdallah, H. M. I., Kerdawy, A. M. E., Sciandra, F., & Ghannam, I. A. Y. (2021) · Archiv der Pharmazie · doi:10.1002/ardp.202100399 · Cited by 24 · see citing works

An efficient synthesis of 2H-chromen-3-yl derivatives via CuI/(NH4)2HPO4 catalyzed reaction of O-propargyl salicylaldehydes with active methylene compounds

Kumari, K., Raghuvanshi, D. S., & Singh, K. N. (2012) · Tetrahedron · doi:10.1016/j.tet.2012.10.066 · Cited by 24 · see citing works

An insight to treat cardiovascular diseases through phytochemicals targeting PPAR-α

Sharma, S., Sharma, D., Dhobi, M., Wang, D., & Tewari, D. (2023) · Molecular and Cellular Biochemistry · doi:10.1007/s11010-023-04755-7 · Cited by 23 · see citing works

Drugs targeting peroxisome proliferator-activated receptors

Xie, Z., Xin, J., Huang, C.-J., & Liao, C. (2025) · Drug Discovery Today · doi:10.1016/j.drudis.2025.104318 · Cited by 22 · see citing works

Peroxisome proliferator‐activated receptor gamma (PPARγ) regulates lactase expression and activity in the gut

Fuméry, M., Speca, S., Langlois, A., Davila, A., Dubuquoy, C., Grauso, M., Mena, A. M., Figeac, M., METZGER, D., Rousseaux, C., et al. (2017) · EMBO Molecular Medicine · doi:10.15252/emmm.201707795 · Cited by 22 · see citing works

PPAR Medicines and Human Disease: The ABCs of It All

Apostoli, A. J., & Nicol, C. J. B. (2012) · PPAR Research · doi:10.1155/2012/504918 · Cited by 22 · see citing works

Design and Synthesis of Dual Modulators of Soluble Epoxide Hydrolase and Peroxisome Proliferator-Activated Receptors

la Buscató, E., Blöcher, R., Lamers, C., Klingler, F., Hahn, S., Steinhilber, D., Schubert‐Zsilavecz, M., & Proschak, E. (2012) · Journal of Medicinal Chemistry · doi:10.1021/jm301194c · Cited by 22 · see citing works

The Role of Peroxisome Proliferator-Activated Receptors (PPARs) in Pan-Cancer

Huang, R., Zhang, J., Li, M., Yan, P., Yin, H., Zhai, S., Zhu, X., Hu, P., Zhang, J., Huang, L., et al. (2020) · PPAR Research · doi:10.1155/2020/6527564 · Cited by 22 · see citing works

Identification of a novel PPARγ modulator with good anti-diabetic therapeutic index via structure-based screening, optimization and biological validation

Chen, F., Ma, L., Cai, G., Tang, J., Wang, Y., Liu, Q., Liu, X., Hou, N., Zhou, Z., & Yi, W. (2022) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2022.113653 · Cited by 21 · see citing works

A New Series of Aryloxyacetic Acids Endowed with Multi-Target Activity towards Peroxisome Proliferator-Activated Receptors (PPARs), Fatty Acid Amide Hydrolase (FAAH), and Acetylcholinesterase (AChE)

Leuci, R., Brunetti, L., Laghezza, A., Piemontese, L., Carrieri, A., Pisani, L., Tortorella, P., Catto, M., & Loiodice, F. (2022) · Molecules · doi:10.3390/molecules27030958 · Cited by 20 · see citing works

The Structure Basis of Phytochemicals as Metabolic Signals for Combating Obesity

Li, X., Zheng, L., Zhang, B., Deng, Z., & Luo, T. F. (2022) · Frontiers in Nutrition · doi:10.3389/fnut.2022.913883 · Cited by 20 · see citing works

Synthesis of novel benzothiazole amides: Evaluation of PPAR activity and anti-proliferative effects in paraganglioma, pancreatic and colorectal cancer cell lines

Ammazzalorso, A., Lellis, L. D., Florio, R., Laghezza, A., Filippis, B. D., Fantacuzzi, M., Giampietro, L., Maccallini, C., Tortorella, P., Veschi, S., et al. (2019) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2019.06.020 · Cited by 20 · see citing works

Discovery of the First Subnanomolar PPARα/δ Dual Agonist for the Treatment of Cholestatic Liver Diseases

Feng, Z., Xiang, J., Sun, G., Liu, H., Wang, Y., Liu, X., Feng, J., Xu, Q., Wen, X., Yuan, H., et al. (2023) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c02123 · Cited by 19 · see citing works

Multi-Target Drugs Against Metabolic Disorders

Scotti, L., Monteiro, A., Viana, J. D. O., Mendonça, F. J. B., Ishiki, H. M., Ernestine, N., Santos, R., & Scotti, L. (2018) · Endocrine Metabolic & Immune Disorders - Drug Targets · doi:10.2174/1871530319666181217123357 · Cited by 18 · see citing works

Metabolomics analysis of the protective effect of rubusoside on palmitic acid-induced lipotoxicity in INS-1 cells using UPLC-Q/TOF MS

Zheng, H., Wu, J., Huang, H., Meng, C., Li, W., Wei, T., & Su, Z. (2019) · Molecular Omics · doi:10.1039/c9mo00029a · Cited by 18 · see citing works

Synthesis, Characterization, Molecular Docking, and Anticancer Evaluation of 4‐Thiazolidinone Analogues

Mushtaque, M., Avecilla, F., Hafeez, Z. B., & Rizvi, M. M. A. (2019) · Journal of Heterocyclic Chemistry · doi:10.1002/jhet.3549 · Cited by 18 · see citing works

Synthetic Strategies and Biological Potential of Coumarin-Chalcone Hybrids: A New Dimension to Drug Design

Pasricha, S., & Gahlot, P. (2020) · Current Organic Chemistry · doi:10.2174/1385272824666200219091830 · Cited by 18 · see citing works

Evolution of a 4-Benzyloxy-benzylamino Chemotype to Provide Efficacious, Potent, and Isoform Selective PPARα Agonists as Leads for Retinal Disorders

Dou, X., Nath, D., Shin, H. Y., Nurmemmedov, E., Bourne, P. C., Ma, J., & Duerfeldt, A. S. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b01189 · Cited by 17 · see citing works

The Design of Multi-target Drugs to Treat Cardiovascular Diseases: Two (or more) Birds on One Stone

Caruso, L., Nadur, N. F., da Fonseca, M. B., Ferreira, L. A., Lacerda, R. B., Graebin, C. S., & Kümmerle, A. E. (2022) · Current Topics in Medicinal Chemistry · doi:10.2174/1568026622666220201151248 · Cited by 17 · see citing works

Synthesis, in vitro evaluation, and molecular modeling investigation of benzenesulfonimide peroxisome proliferator-activated receptors α antagonists

Ammazzalorso, A., Carrieri, A., Verginelli, F., Bruno, I., Carbonara, G., D’Angelo, A., Filippis, B. D., Fantacuzzi, M., Florio, R., Fracchiolla, G., et al. (2016) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2016.02.064 · Cited by 17 · see citing works

Triglyceride-lowering agents

Salakhutdinov, N. F., & Laev, S. S. (2014) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2014.05.008 · Cited by 17 · see citing works

Discovery of amide based fibrates as possible antidyslipidemic and antioxidant agents

Sashidhara, K. V., Palnati, G. R., Dodda, R. P., Sonkar, R., Khanna, A., & Bhatia, G. (2012) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2012.09.040 · Cited by 17 · see citing works

Pharmacophore elucidation of phosphoiodyn A – Potent and selective peroxisome proliferator-activated receptor β/δ agonists with neuroprotective activity

Kinarivala, N., Suh, J. H., Botros, M., Webb, P., & Trippier, P. C. (2016) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2016.03.028 · Cited by 17 · see citing works

Low GPR81 in ER+ breast cancer cells drives tamoxifen resistance through inducing PPARα-mediated fatty acid oxidation

Yu, J., Du, Y., Liu, C., Xie, Y., Yuan, M., Shan, M., Li, N., Liu, C., Wang, Y., & Qin, J. (2024) · Life Sciences · doi:10.1016/j.lfs.2024.122763 · Cited by 15 · see citing works

PPARα agonists based on stilbene and its bioisosteres: biological evaluation and docking studies

Filippis, B. D., Agamennone, M., Ammazzalorso, A., Bruno, I., D’Angelo, A., Matteo, M. D., Fantacuzzi, M., Giampietro, L., Giancristofaro, A., Maccallini, C., et al. (2015) · MedChemComm · doi:10.1039/c5md00151j · Cited by 12 · see citing works

Preclinical evidence that the PPAR γ modulator, N‐Acetyl‐ GED ‐0507‐34‐Levo, may protect human hair follicle epithelial stem cells against lichen planopilaris‐associated damage

Chéret, J., Piccini, I., Hardman, J. A., Ghatak, S., Alam, M. A., Lehmann, J., Jiménez, F., Erdmann, H., Poblet, E., Botchkareva, N. V., et al. (2019) · Journal of the European Academy of Dermatology and Venereology · doi:10.1111/jdv.16114 · Cited by 15 · see citing works

Discovery by Virtual Screening of an Inhibitor of CDK5-Mediated PPARγ Phosphorylation

O’Mahony, G., Petersen, J. F. W., Ek, M. S., Rae, R., Johansson, C. A., Jianming, L., Prokoph, N., Bergström, F., Bamberg, K., Giordanetto, F., et al. (2022) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.1c00715 · Cited by 15 · see citing works

Beyond the Canonical Endocannabinoid System. A Screening of PPAR Ligands as FAAH Inhibitors

Brunetti, L., Carrieri, A., Piemontese, L., Tortorella, P., Loiodice, F., & Laghezza, A. (2020) · International Journal of Molecular Sciences · doi:10.3390/ijms21197026 · Cited by 15 · see citing works

The development and application of peroxisome proliferator-activated receptor (PPAR) modulator

Ma, Y. (2018) · Journal of Chinese Pharmaceutical Sciences · doi:10.5246/jcps.2018.04.023

Rational Targeting of Peroxisome Proliferating Activated Receptor Subtypes

Nevin, D. K., Lloyd, D. G., & Fayne, D. (2011) · Current Medicinal Chemistry · doi:10.2174/092986711798347243 · Cited by 22 · see citing works

Peroxisome Proliferator-Activated Receptor

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Marine Natural and Nature-Inspired Compounds Targeting Peroxisome Proliferator Activated Receptors (PPARs)

D’Aniello, E., Amodeo, P., & Vitale, R. M. (2023) · Marine Drugs · doi:10.3390/md21020089 · Cited by 19 · see citing works

LES RÉCEPTEURS ACTIVÉS PAR LES PROLIFÉRATEURS DE PEROXYSOMES : intérêts médical et pharmacologique

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