A chemoinformatics search for peroxisome proliferator-activated receptors ligands revealed a new pan-agonist able to reduce lipid accumulation and improve insulin sensitivity
Copyright © 2022 Elsevier Masson SAS. All rights reserved..
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.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2022 |
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| Erschienen: |
2022 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:235 |
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| Enthalten in: |
European journal of medicinal chemistry - 235(2022) vom: 05. Mai, Seite 114240 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Sblano, Sabina [VerfasserIn] |
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| Links: |
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| Themen: |
Chemoinformatics search |
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| Anmerkungen: |
Date Completed 25.04.2022 Date Revised 25.04.2022 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.ejmech.2022.114240 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Copyright © 2022 Elsevier Masson SAS. All rights reserved. | ||
| 520 | |a 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 | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Chemoinformatics search | |
| 650 | 4 | |a Docking experiments | |
| 650 | 4 | |a Glucose uptake | |
| 650 | 4 | |a PPAR pan-agonist | |
| 650 | 7 | |a Hypoglycemic Agents |2 NLM | |
| 650 | 7 | |a Ligands |2 NLM | |
| 650 | 7 | |a Lipids |2 NLM | |
| 650 | 7 | |a PPAR gamma |2 NLM | |
| 650 | 7 | |a Peroxisome Proliferator-Activated Receptors |2 NLM | |
| 700 | 1 | |a Cerchia, Carmen |e verfasserin |4 aut | |
| 700 | 1 | |a Laghezza, Antonio |e verfasserin |4 aut | |
| 700 | 1 | |a Piemontese, Luca |e verfasserin |4 aut | |
| 700 | 1 | |a Brunetti, Leonardo |e verfasserin |4 aut | |
| 700 | 1 | |a Leuci, Rosalba |e verfasserin |4 aut | |
| 700 | 1 | |a Gilardi, Federica |e verfasserin |4 aut | |
| 700 | 1 | |a Thomas, Aurelien |e verfasserin |4 aut | |
| 700 | 1 | |a Genovese, Massimo |e verfasserin |4 aut | |
| 700 | 1 | |a Santi, Alice |e verfasserin |4 aut | |
| 700 | 1 | |a Tortorella, Paolo |e verfasserin |4 aut | |
| 700 | 1 | |a Paoli, Paolo |e verfasserin |4 aut | |
| 700 | 1 | |a Lavecchia, Antonio |e verfasserin |4 aut | |
| 700 | 1 | |a Loiodice, Fulvio |e verfasserin |4 aut | |
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