A photocaged inhibitor of acid sphingomyelinase
نویسندگان
چکیده
منابع مشابه
Small molecule inhibitors of acid sphingomyelinase.
Despite of the importance of the acid sphingomyelinase for sphingomyelin homeostasis and sphingolipid signalling, potent and selective inhibitors for this enzyme are rare. An increasing set of data on the inhibition of acid sphingomyelinase in different disease models using indirect inhibitors has been generated and strongly implies acid sphingomyelinase as an emerging drug target. Very recentl...
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The effect of saposins (A, B, C and D) on acid sphingomyelinase activity was determined using a crude human kidney sphingomyelinase preparation and a purified sphingomyelinase preparation from human placenta. Saposin D stimulated the activity of the crude enzyme by increasing its apparent Km and Vmax. values for sphingomyelin hydrolysis. Unlike the crude enzyme, the activity of the purified enz...
متن کاملCrystal structure of mammalian acid sphingomyelinase
Acid sphingomyelinase (ASMase, ASM, SMPD1) converts sphingomyelin into ceramide, modulating membrane properties and signal transduction. Inactivating mutations in ASMase cause Niemann-Pick disease, and its inhibition is also beneficial in models of depression and cancer. To gain a better understanding of this critical therapeutic target, we determined crystal structures of mammalian ASMase in v...
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Ceramides induce important intracellular signaling pathways, modulating proliferation, migration, apoptosis, and inflammation. However, the relevance of the ceramide metabolism in the reconvalescence phase after stroke is unclear. Besides its well-known property as a selective serotonin reuptake inhibitor, fluoxetine has been reported to inhibit the acid sphingomyelinase (ASM), a key regulator ...
متن کاملInvestigation of Furfural as Corrosion Inhibitor in Hydrochloric Acid Solution
Effectiveness of furfural as an organic inhibitor in 5 percent hydrochloric acid which is used in acid pickling of steel was evaluated. Lungmuir, Frumkin and Flory-Huggins isotherms [1, 2] were used to determine the parameters of effective adsorption, free energy and entropy of adsorption. Furfural indicated an inhibition less than 17 percent in concentrations of 0.001 mole per liter for a dura...
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ژورنال
عنوان ژورنال: Chemical Communications
سال: 2020
ISSN: 1359-7345,1364-548X
DOI: 10.1039/d0cc06661c