The peroxisome proliferator-activated receptors (PPARs) are nuclear receptors involved in the regulation of the metabolic homeostasis and therefore represent valuable therapeutic targets for the treatment of metabolic diseases. The development of more balanced drugs interacting with PPARs, devoid of the side-effects showed by the currently marketed PPARγ full agonists, is considered the major challenge for the pharmaceutical companies. Here we present a chemoinformatics search approach for new ligands that let us identify a novel PPAR pan-agonist with a very attractive activity profile being able to reduce lipid accumulation and improve insulin sensitivity. This compound represents, therefore, the potential lead of a new class of drugs for treatment of dyslipidemic type 2 diabetes.

A chemoinformatics search for peroxisome proliferator-activated receptors ligands revealed a new pan-agonist able to reduce lipid accumulation and improve insulin sensitivity / Sblano S.; Cerchia C.; Laghezza A.; Piemontese L.; Brunetti L.; Leuci R.; Gilardi F.; Thomas A.; Genovese M.; Santi A.; Tortorella P.; Paoli P.; Lavecchia A.; Loiodice F.. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - ELETTRONICO. - 235:(2022), pp. 114240-114259. [10.1016/j.ejmech.2022.114240]

A chemoinformatics search for peroxisome proliferator-activated receptors ligands revealed a new pan-agonist able to reduce lipid accumulation and improve insulin sensitivity

Genovese M.;Santi A.;Paoli P.;
2022

Abstract

The peroxisome proliferator-activated receptors (PPARs) are nuclear receptors involved in the regulation of the metabolic homeostasis and therefore represent valuable therapeutic targets for the treatment of metabolic diseases. The development of more balanced drugs interacting with PPARs, devoid of the side-effects showed by the currently marketed PPARγ full agonists, is considered the major challenge for the pharmaceutical companies. Here we present a chemoinformatics search approach for new ligands that let us identify a novel PPAR pan-agonist with a very attractive activity profile being able to reduce lipid accumulation and improve insulin sensitivity. This compound represents, therefore, the potential lead of a new class of drugs for treatment of dyslipidemic type 2 diabetes.
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114240
114259
Sblano S.; Cerchia C.; Laghezza A.; Piemontese L.; Brunetti L.; Leuci R.; Gilardi F.; Thomas A.; Genovese M.; Santi A.; Tortorella P.; Paoli P.; Lavecchia A.; Loiodice F.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2158/1266892
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