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Characterization of...
Characterization of the Aquaporin-9 Inhibitor RG100204 In Vitro and in db/db Mice
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- Florio, Marilina (author)
- University of Bari Aldo Moro
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- Engfors, Angelica (author)
- Lund University,Lunds universitet,Biokemi och Strukturbiologi,Centrum för Molekylär Proteinvetenskap,Kemiska institutionen,Institutioner vid LTH,Lunds Tekniska Högskola,Biochemistry and Structural Biology,Center for Molecular Protein Science,Department of Chemistry,Departments at LTH,Faculty of Engineering, LTH
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- Gena, Patrizia (author)
- University of Bari Aldo Moro
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- Larsson, Jessica (author)
- Red Glead Discovery AB
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- Massaro, Alessandro (author)
- LUM University,LUM Enterprise Srl
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- Timpka, Stella (author)
- Red Glead Discovery AB
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- Kvist Reimer, Martina (author)
- Red Glead Discovery AB
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- Kjellbom, Per (author)
- Lund University,Lunds universitet,Biokemi och Strukturbiologi,Centrum för Molekylär Proteinvetenskap,Kemiska institutionen,Institutioner vid LTH,Lunds Tekniska Högskola,Biochemistry and Structural Biology,Center for Molecular Protein Science,Department of Chemistry,Departments at LTH,Faculty of Engineering, LTH
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- Beitz, Eric (author)
- University of Kiel
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- Johanson, Urban (author)
- Lund University,Lunds universitet,Biokemi och Strukturbiologi,Centrum för Molekylär Proteinvetenskap,Kemiska institutionen,Institutioner vid LTH,Lunds Tekniska Högskola,Biochemistry and Structural Biology,Center for Molecular Protein Science,Department of Chemistry,Departments at LTH,Faculty of Engineering, LTH
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- Rützler, Michael (author)
- Lund University,Lunds universitet,Biokemi och Strukturbiologi,Centrum för Molekylär Proteinvetenskap,Kemiska institutionen,Institutioner vid LTH,Lunds Tekniska Högskola,Biochemistry and Structural Biology,Center for Molecular Protein Science,Department of Chemistry,Departments at LTH,Faculty of Engineering, LTH,Apoglyx AB
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- Calamita, Giuseppe (author)
- University of Bari Aldo Moro
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(creator_code:org_t)
- 2022-10-04
- 2022
- English 11 s.
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In: Cells. - : MDPI AG. - 2073-4409. ; 11:19
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http://dx.doi.org/10... (free)
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Abstract
Subject headings
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- Aquaporin-9 (AQP9) is a facilitator of glycerol and other small neutral solute transmembrane diffusion. Identification of specific inhibitors for aquaporin family proteins has been difficult, due to high sequence similarity between the 13 human isoforms, and due to the limited channel surface areas that permit inhibitor binding. The few AQP9 inhibitor molecules described to date were not suitable for in vivo experiments. We now describe the characterization of a new small molecule AQP9 inhibitor, RG100204 in cell-based calcein-quenching assays, and by stopped-flow light-scattering recordings of AQP9 permeability in proteoliposomes. Moreover, we investigated the effects of RG100204 on glycerol metabolism in mice. In cell-based assays, RG100204 blocked AQP9 water permeability and glycerol permeability with similar, high potency (~5 × 10 -8 M). AQP9 channel blocking by RG100204 was confirmed in proteoliposomes. After oral gavage of db/db mice with RG100204, a dose-dependent elevation of plasma glycerol was observed. A blood glucose-lowering effect was not statistically significant. These experiments establish RG100204 as a direct blocker of the AQP9 channel, and suggest its use as an experimental tool for in vivo experiments on AQP9 function.
Subject headings
- NATURVETENSKAP -- Biologi -- Biokemi och molekylärbiologi (hsv//swe)
- NATURAL SCIENCES -- Biological Sciences -- Biochemistry and Molecular Biology (hsv//eng)
Keyword
- membrane transport
- aquaglyceroporins
- metabolic homeostasis
- energy balance
- glycerol metabolism
- gluconeogenesis
- calcein quenching
- Pichia pastoris
- proteoliposomes
- stopped-flow light scattering
Publication and Content Type
- art (subject category)
- ref (subject category)
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- By the author/editor
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Florio, Marilina
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Engfors, Angelic ...
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Gena, Patrizia
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Larsson, Jessica
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Massaro, Alessan ...
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Timpka, Stella
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show more...
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Kvist Reimer, Ma ...
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Kjellbom, Per
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Beitz, Eric
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Johanson, Urban
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Rützler, Michael
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Calamita, Giusep ...
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- NATURAL SCIENCES
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NATURAL SCIENCES
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Cells
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Lund University