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Showing 1 to 10 of 10 for “"mitochondrial uncoupler"”.
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Design and Synthesis of 8-Trifluoromethyl-Substituted Heterocyclic Small Molecule Mitochondrial Uncouplers for the Treatment of Metabolic Diseases
… converted into energy through a process called mitochondrial respiration. Through this process, mitochondria provide over 90% of cellular energy. However, during inflammatory events, mitochondrial respiration is less efficacious and could cause or progress diseases such as obesity, type 2 …
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Chemical probes for the study of mitochondrial oxidative stress
… were designed to react with H2O2 and release a mitochondrial uncoupler. These were synthesised and their reaction with H2O2 was examined using UV spectrophotometry. DNP-SUM vii reacted slowly with a second order rate constant of 0.20 M-1s-1 and was deemed unsuitable for further investigation. …
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Nitrite and insulin lower the oxygen cost of ATP synthesis in skeletal muscle cells by pleiotropic stimulation of glycolysis
… regulator of muscle function that increases mitochondrial efficiency, was explored to assess possible mechanistic overlap. Calculation of real-time intracellular ATP synthesis rates from simultaneous oxygen consumption and medium acidification measurements revealed the effects of sodium …
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Reactive oxygen and nitrogen species production in cardiomyoblasts during hypoxia and reoxygenation
… O2 and 10% O2 was dependent on the production of mitochondrial superoxide (O2-•) and nitric oxide (•NO), partly from nitric oxide synthase (NOS). Both apoptotic and necrotic cell death during 2% O2 for 4h could be rescued by the mitochondrial complex I inhibitor; rotenone and NOS inhibitor; …
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Complex Heterocycles as Mitochondrial Uncouplers
Small molecule mitochondrial uncouplers are compounds that dissipate the proton motive force independent of ATP synthase that results in increased energy expenditure. Mild mitochondrial uncoupling has therapeutic potential in treating obesity, diabetes, neurological diseases, non-alcoholic …
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Structure-Activity Relationship Studies of Mitochondrial Uncouplers and PilB Inhibitors
… limited side effects is thus desirable. Chemical mitochondrial uncouplers are protonophoric, lipophilic small-molecules that transport protons from the mitochondrial intermembrane space into the matrix independent of ATP synthase, thus uncoupling nutrient oxidation from ATP production. Such a …
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Structure-Activity Relationship Studies of Imidazo[4,5-b]pyrazine Derivatives as Mitochondrial Uncouplers and their Potential in the Treatment of Obesity
Mitochondrial uncouplers have the capacity of passively shuttling protons from the mitochondrial intermembrane space to the mitochondrial matrix, independent of ATP synthase. This results in the disruption of oxidative phosphorylation and increased rate of metabolism as a counter action from the …
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Exploring Parkinson’s disease associated LRRK2 and PINK1/Parkin signal transduction pathways within immune cells
… blood neutrophils and treated them with the mitochondrial uncoupler CCCP for durations of 3-20 hours, and analysed neutrophil lysates for PINK1 stabilisation through immunoblotting with the PINK1 (Novus) antibody. I also conducted PINK1 immuno-precipitation (IP) experiments to confirm the …
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Structure-Activity Relationship Studies of Sphingosine Kinase Inhibitors and Mitochondrial Uncouplers
… in vivo activity will also be discussed. Mitochondrial uncouplers are small molecules that shuttle protons from the inter membrane space to the mitochondrial matrix independent of ATP synthase, which disrupts oxidative phosphorylation and promotes increased nutrient metabolism for …
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Metaboloptics: In Vivo Optical Imaging to Enable Simultaneous Measurement of Glucose Uptake, Mitochondrial Membrane Potential, and Vascular Features in Cancer
… primary axes of metabolism are glycolysis and mitochondrial metabolism (OXPHOS), and alteration of either can promote unwanted outcomes in cancer. In particular, increased glucose uptake independent of oxygenation is a well-known mark of aggressive cancers that are more likely to metastasize …