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Exploration of Novel Urolithin C Derivatives as Non-Competitive Inhibitors of Liver Pyruvate Kinase
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- Battisti, Umberto Maria (author)
- Gothenburg University,Göteborgs universitet,KTH,Nanobioteknologi,Science for Life Laboratory, SciLifeLab,Univ Gothenburg, Dept Chem & Mol Biol, SE-41296 Gothenburg, Sweden.,Institutionen för kemi och molekylärbiologi,Department of Chemistry and Molecular Biology
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- Monjas, Leticia (author)
- Gothenburg University,Göteborgs universitet,KTH,Science for Life Laboratory, SciLifeLab,Systembiologi,Univ Gothenburg, Dept Chem & Mol Biol, SE-41296 Gothenburg, Sweden.,Institutionen för kemi och molekylärbiologi,Department of Chemistry and Molecular Biology
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- Akladios, Fady (author)
- Gothenburg University,Göteborgs universitet,KTH,Nanobioteknologi,Science for Life Laboratory, SciLifeLab,Univ Gothenburg, Dept Chem & Mol Biol, SE-41296 Gothenburg, Sweden.,Institutionen för kemi och molekylärbiologi,Department of Chemistry and Molecular Biology
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- (creator_code:org_t)
- MDPI AG, 2023
- 2023
- English.
- In: Pharmaceuticals. - : MDPI AG. - 1424-8247. ; 16:5
- Journal article (peer-reviewed)
Abstract
Subject headings
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- The inhibition of liver pyruvate kinase could be beneficial to halt or reverse non-alcoholic fatty liver disease (NAFLD), a progressive accumulation of fat in the liver that can lead eventually to cirrhosis. Recently, urolithin C has been reported as a new scaffold for the development of allosteric inhibitors of liver pyruvate kinase (PKL). In this work, a comprehensive structure-activity analysis of urolithin C was carried out. More than 50 analogues were synthesized and tested regarding the chemical features responsible for the desired activity. These data could pave the way to the development of more potent and selective PKL allosteric inhibitors.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinsk bioteknologi -- Medicinsk bioteknologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Medical Biotechnology -- Medical Biotechnology (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmakologi och toxikologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmacology and Toxicology (hsv//eng)
Keyword
- NAFLD
- liver pyruvate kinase
- allosteric inhibitors
- urolithin C
- SAR studies
- NAFLD
- liver pyruvate kinase
- allosteric inhibitors
- urolithin C
- SAR studies
Publication and Content Type
- ref (subject category)
- art (subject category)
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