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br Discussion In the present
2022-04-22
Discussion In the present paper it was shown for the first time that the conjugation of ethacrynic X-Gal and glutathione catalyzed by GSTP1-1 stereospecifically forms one of the diastereoisomers of the glutathione conjugate (EASG). Chemical conjugation results in formation of a mixture of both d
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Recent studies on detailed biochemical and structural charac
2022-04-22
Recent studies on detailed biochemical and structural characterization of plant GSNOR Sitafloxacin Hydrate receptor confirmed their similarities to mammalian homologues [16], [17], [18], [19]. Compared to human GSNOR, plant GSNORs exhibit differences in the composition of the anion-binding pocket,
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br Molecular mechanisms underpinning GSNOR function in the
2022-04-22
Molecular mechanisms underpinning GSNOR1 function in the defence response Recently, Arabidopsis GSNOR1 has been shown to govern the extent of S-nitrosylation of two key regulatory proteins, Non-Expresser of Pathogenesis-Related Genes 1 (NPR1) and SA binding protein 3 (SABP3), which are integral t
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The differential tissue and ligand dependent signaling
2022-04-22
The differential tissue- and ligand-dependent signaling described here has important implications for the therapeutic potential of synthetic GPR109A agonists for the treatment of atherosclerosis. The failure of MK-0354, a biased, partial GPR109A agonist, to activate signaling pathways upstream of va
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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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