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In this study we implicate SCFFBXO E ligase as
2020-04-02
In this study, we implicate SCFFBXO3 E3 ligase as a critical modulator of inflammation in atherosclerosis and demonstrate the efficacy of a small molecule FBXO3 inhibitor in suppressing inflammatory responses important in atherosclerosis. Specifically, individuals carrying a hypofunctioning genetic
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Covalent inhibitors are well suited for targeting the E
2020-04-02
Covalent inhibitors are well suited for targeting the E1 MI-773 of Ubl modifications. Because the E1 enzymes in Ubl modifications, such as the SUMO E1 and Atg7, have a slow turnover rate (Boggio et al., 2004), prolonged inhibition can be achieved without requiring compounds to be stable in circulat
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br Introduction The ubiquitination status of a target protei
2020-04-02
Introduction The ubiquitination status of a target protein is achieved via a delicate balance between two opposing forces: ubiquitin E3 ligases and DUBs. It has been postulated that the majority of proteins in a cell are regulated and modified by ubiquitin at some point (Hershko and Ciechanover,
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A previous study suggested that DARs and octopamine
2020-04-02
A previous study suggested that DARs and octopamine/tyramine receptors (OARs/TARs) have close pharmacological properties (Beggs et al., 2011). Their relationships were also supported by phylogenetic analyses (Balfanz et al., 2005, Hauser et al., 2008, Wu et al., 2014), indicating that some of DAR an
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The intimate interactions between flavonoids and ER have bee
2020-04-02
The intimate interactions between flavonoids and ERα have been more extensively studied than their ERβ interactions because of the dominant role of ERα in some important diseases (Ye et al., 2018) including breast cancer (more than 80% of human breast cancers are ERα positive) (Turner et al., 2015),
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FDA-approved Drug Library mg Although enantioselective accum
2020-04-02
Although enantioselective accumulation of metalaxyl in organisms is an integrated outcome of bio-process including absorption, transportation, and transformation, it is observed in our study that catalysis of CYP450 may lead to the enantioselective accumulation of metalaxyl. However, the mechanisms
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VO-Ohpic trihydrate australia br Introduction br Sphingolipi
2020-04-02
Introduction Sphingolipid metabolism Sphingolipids, are fundamental constituents of all eukaryotic membranes and their metabolism is carried out by a broad array of anabolic and VO-Ohpic trihydrate australia with ceramide as their hub (for a review, (Hannun and Obeid, 2018)). Ceramide can be
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The CYP A genes are regulated physiologically
2020-04-01
The CYP3A genes are regulated physiologically by glucocorticosteroids, growth hormone, thyroid hormones and cytokines [13, 20, 30]. It has been shown that glucocorticoid receptor (GR), pregnane X receptor (PXR), constitutive androstane receptor (CAR) and vitamin D receptor (VDR) play an important ro
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br Conclusions The present study demonstrated that CuE posse
2020-04-01
Conclusions The present study demonstrated that CuE possesses strong hepatotoxicity. CuE is not only a mechanism-based inhibitor of human CYP3A4, but also inhibits P-gp activity in vitro. In whole animal studies, CuE induces CYP3A and P-gp after a long-term treatment but inhibits the activities o
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Coumarins also known as benzopyran
2020-04-01
Coumarins also known as benzopyran-2-ones are a family of nature-occurring lactones first isolated from Tonka beans in 1820. They are an important class of oxygen containing heterocycles widely found in nature, so much so that they have been routinely employed as herbal remedies since early days. Ov
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IAA sensitive Cl channels were shown
2020-04-01
IAA-94-sensitive Cl channels were shown to mediate cardioprotection due to IPC (Diaz et al., 1999) and cyclosporine A (Diaz et al., 2013). CLIC-like channel activity was also observed in cardiac mitoplast (Misak et al., 2013) but the molecular identity of these intracellular Cl channels and their pr
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Despite the weak and transient nature
2020-04-01
Despite the weak and transient nature of E2–E3 interactions, this binding is required for the transfer of ubiquitin to the substrate. The low affinity characteristics of this interaction may be due to the fact that E2s use the same surface to interact with E1s and E3s, and hence while binding to an
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In attempts to further purify His Artemis numerous
2020-04-01
In attempts to further purify [His]6-Artemis, numerous matrices were assessed including anion and cation exchange, and PD 169316 interaction chromatography. The results from these matrices were universally poor (data not shown). Fractionation via adsorption chromatography on a hydroxyapatite (HAP)
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ASC was reported as a potent antiviral and antifungal
2020-04-01
ASC was reported as a potent antiviral and antifungal agent, and its derivatives could modulate a variety of physiological activities, such as anti-tumor, anti-metastatic, and anti-diabetic activities in animals. Mie Tsuruga et al. found that 4-o-methylascochlorin had immunosuppressive activity, but
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Angiomatoid fibrous histiocytoma originally described as
2020-04-01
Angiomatoid fibrous histiocytoma (originally described as angiomatoid malignant fibrous histiocytoma) is a soft tissue tumor of intermediate biologic potential. AFH typically arises within extremity deep dermis and subcutis in children and young adults,157, 158, 159 but can arise in older adults and
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