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• W2912100707 abstract "The soluble guanylyl cyclase (sGC) plays a key role in NO/cGMP signalling and is widely recognised to be important in different disease pathomechanisms. The discovery of sGC agonists provides a new opportunity to stimulate the NO/cGMP pathway. One class of compounds are the heme-independent sGC activators, which are thought to bind to oxidised or heme-free sGC. This enzyme is preferentially formed under disease situations accompanied by oxidative stress. Accordingly, this binding mode of sGC activators has quite some appeal for the clinical use of sGC activator drugs in diseases with high oxidative stress burden. However, none of the previous sGC activators, most of them dicarboxylic acid derivatives, has passed clinical trials to date, also because of the potent blood pressure lowering effects. In the current study, we investigate the effects of a new monocarboxylic drug BR 11257 in vitro and in vivo. Activity measurements with purified enzyme indicated gentle sGC activation for BR 11257 resembling a partial agonistic behaviour. In thermal shift measurements, we observed an unexpected difference between BR 11257 and the sGC activators from the dicarboxylic acid type. While activators from the dicarboxylic acid type had a highly thermostabilising influence on sGC, this effect was absent with BR 11257. We hypothesize that the key interaction partner for thermostabilisation is the second carboxylic acid in BAY 60-2770 which is missing in BR 11257. The absence of this thermodynamic receptor stabilisation and the partial agonism may be advantageous to overcome limitations of this class of drugs by avoiding excessive hypotension." @default.
• W2912100707 created "2019-02-21" @default.
• W2912100707 creator A5002156709 @default.
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• W2912100707 creator A5079835977 @default.
• W2912100707 creator A5091353116 @default.
• W2912100707 date "2019-05-01" @default.
• W2912100707 modified "2023-09-25" @default.
• W2912100707 title "A novel soluble guanylyl cyclase activator, BR 11257, acts as a non-stabilising partial agonist of sGC" @default.
• W2912100707 cites W1117090353 @default.
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• W2912100707 cites W1974611305 @default.
• W2912100707 cites W1975677762 @default.
• W2912100707 cites W1978644822 @default.
• W2912100707 cites W1983771586 @default.
• W2912100707 cites W1987184004 @default.
• W2912100707 cites W1987712838 @default.
• W2912100707 cites W1988711065 @default.
• W2912100707 cites W1989738839 @default.
• W2912100707 cites W2000738532 @default.
• W2912100707 cites W2003630942 @default.
• W2912100707 cites W2003913161 @default.
• W2912100707 cites W2006605576 @default.
• W2912100707 cites W2007427423 @default.
• W2912100707 cites W2009257677 @default.
• W2912100707 cites W2014668801 @default.
• W2912100707 cites W2014822929 @default.
• W2912100707 cites W2017383525 @default.
• W2912100707 cites W2024198419 @default.
• W2912100707 cites W2029476307 @default.
• W2912100707 cites W2029583951 @default.
• W2912100707 cites W2031029799 @default.
• W2912100707 cites W2031556019 @default.
• W2912100707 cites W2045645578 @default.
• W2912100707 cites W2051488946 @default.
• W2912100707 cites W2055625563 @default.
• W2912100707 cites W2060259870 @default.
• W2912100707 cites W2063053685 @default.
• W2912100707 cites W2064860687 @default.
• W2912100707 cites W2066482395 @default.
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• W2912100707 cites W2081612114 @default.
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• W2912100707 cites W2115929723 @default.
• W2912100707 cites W2123016903 @default.
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• W2912100707 doi "https://doi.org/10.1016/j.bcp.2019.02.007" @default.
• W2912100707 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30753814" @default.
• W2912100707 hasPublicationYear "2019" @default.
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