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Flaviviruses consist of a nucleocapsid composed of multiple
2022-04-22
Flaviviruses consist of a nucleocapsid, composed of multiple copies of the capsid protein (C) and the single-stranded, positive-sense RNA genome. The nucleocapsid is surrounded by a lipid bilayer in which two transmembrane proteins are inserted, the envelope glycoprotein E and the membrane protein M
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In parallel we were also preparing and evaluating
2022-04-22
In parallel, we were also preparing and evaluating other piperidine bioisosteres and modifications to – to further access additional novel intellectual property (IP) space. Modeling work suggested that 4-position homologated piperidines, as well as 3-position homologated azetidines overlapped favora
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The kinetic data obtained from incubation of BAB with
2022-04-22
The kinetic data obtained from incubation of 4BAB with GLO1 show that 4BAB does not completely inactivate the enzyme (Figs. 2A and S6a). At low concentrations (4.7 and 14.4μM), 4BAB seemed to follow biphasic kinetics (Fig. 2A); even though regardless of the concentration 4BAB, there was a plateau at
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br Flavonoid function Antioxidants are compounds when presen
2022-04-22
Flavonoid function Antioxidants are compounds - when present at a lower concentration compared oxidizable substrate - that delay or prevent oxidation of the substrate [14], [106]. Antioxidants act as nucleophiles to reduce an oxidative molecule to prevent its interaction with another molecule [14
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Heparin and suramin are highly negatively charged
2022-04-22
Heparin and suramin are highly negatively charged molecules, and they are in this aspect, similar to DNA and likely to compete with DNA by binding to the protein cationic groups [17] (Fig. 1). The inhibitory effect of heparin and suramin on DNA and RNA binding proteins has been described [[18], [19]
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ATP is essential for maintaining
2022-04-22
ATP is essential for maintaining the ionic balance of the lens (Michael and Bron, 2011). Without sufficient ATP there is an ionic imbalance due to Na+K+ATPase dysfunction. Previous studies have shown that rabbit lenses incubated ex vivo without glucose rapidly lost ATP in their lens epithelium and f
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In Solloway and colleagues reported that
2022-04-21
In 2015, Solloway and colleagues reported that mice with alpha cell hyperplasia due to inactive hepatic glucagon receptor signaling may most likely be caused by amino 1186 dependent mechanisms [11]. The authors then showed these adaptations are regulated by ‘mechanistic target of rapamycin’ (mTOR)-d
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bosentan br Central control of GI ghrelin secretion
2022-04-21
Central control of GI ghrelin secretion The CNS communicates with the GI tract through the vagus nerve originating in the DMV and sympathetic spinal afferents emanating from the thoracic spinal chord (Bray, 2000). The cells that secrete peripheral ghrelin are under direct control of these two pat
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These reports have gradually established G quadruplex bindin
2022-04-21
These reports have gradually established G-quadruplex binding small molecules as promising anti-cancer therapeutic agents. Besides the stabilization of G-quadruplex structures, some of these molecules also serve as diagnostic probes and sensors for G-quadruplexes in vitro and in vivo. Of these, Thio
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Prion diseases are transmissible and result in
2022-04-21
Prion diseases are transmissible and result in fatal neurodegenerative disorders, which, similar to AD, also involve the infiltration and activation of mononuclear phagocytes in 84 9 lesions (reviewed in [61]). A 21 amino-acid fragment of the aberrant human prion protein, Prp106–126, can form fibri
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It has been reported that aberrant
2022-04-21
It has been reported that aberrant GPR120 expressions were detected in colorectal carcinomas, compared with normal tissues. In addition, GPR120 stimulated cell motile activity and angiogenic property in colon cancer cells [10]. Recently, we indicated that GPR40 suppressed cell motile and invasive ac
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In Apicomplexan parasites such as Toxoplasma gondii
2022-04-21
In Apicomplexan parasites such as Toxoplasma gondii isoprenoids are biosynthesized through the DOXP/MEP pathway as illustrated in Scheme 2. In addition, T. gondii possesses a bifunctional FPPS/GGPPS (TgFPPS) that is able to catalyze the formation of both FPP and GGPP.5, 6 The FPPS gene appears to be
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WT associated protein WTAP a nuclear protein is first
2022-04-21
WT1 associated protein (WTAP), a nuclear protein, is first identified by Little [6] who noticed its specific interaction with WT1. Besides several essential physiological processes, such as mRNA stabilization [7], eye development [8], m6A methylation [9], mRNA alternative splicing [10] and h89 regu
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Similar to in vitro data in vivo studies
2022-04-21
Similar to in vitro data, in vivo studies have also revealed modulation of TLR4-induced inflammatory responses by AEA. The proposed AEA reuptake inhibitor AM404 has been shown to attenuate TLR4-induced increases in plasma levels of IL-6 and IL-1β, the latter effect mediated by CB1 receptor activatio
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Finally worth of mention are
2022-04-20
Finally, worth of mention are few papers that report on the discovery of HO-2 selective inhibitors. In 2013, starting from the screening of a Ergosterol library, the above-mentioned Canadian research group identified Clemizole (Table 6) as a new hit compound for the development of the first series
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