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Pharmacologic approaches of inhibiting GSNOR activity have r
2021-11-23
Pharmacologic approaches of inhibiting GSNOR activity have reached the point of clinical development with the recent announcement of the first cystic fibrosis patients treated with the first-in-class GSNOR inhibitor, N6022 (N30 Pharmaceuticals). Clinical development is ongoing for other indications
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br Cholecystokinin CCK CCK is secreted
2021-11-23
Cholecystokinin (CCK) CCK is secreted by enteroendocrine I-cells of the duodenum and jejunum in response to amino acids and lipids [14]. There are two forms of the CCK receptor, CCK1 which is expressed on pancreatic α- and β-cells while CCK2 is located on somatostatin-secreting δ-cells [8]. CCK r
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Molecular properties as well as metabolic stability in rat a
2021-11-23
Molecular properties as well as metabolic stability in rat and human liver microsomes for the most active nitro (), nitrile (), methylsulfone (), and sulfonamides () analogues were measured (). All these derivatives possessed excellent membrane permeability as measured in the Pampa assay and further
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Analysis of the i motif structures during biased unfolding
2021-11-23
Analysis of the i-motif structures during biased unfolding of G-quadruplexes leads to the conclusion that at acidic pH the i-motif is absolutely unaffected by that process. The hydrogen bonds within the i-motif are intact (Fig. 3D) and they only fluctuate around mean values. On the other hand, the i
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YAP TAZ nuclear function is also influenced by interaction
2021-11-22
YAP/TAZ nuclear function is also influenced by interaction with the TEAD family of transcription factors [96, 97, 98, 99, 100, 101]. The RAC1 BWX 46 exchange factor protein TIAM1 has recently been linked to YAP/TAZ regulation in the nucleus and cytoplasm. Nuclear TIAM1 inhibits YAP/TAZ binding to TE
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In the previous study concerning
2021-11-22
In the previous study concerning HO-1-mediated inhibtion of HCV replication, the mechanism underlying IFN-α/β indcuction by HO-1 involved in HO-1-catalyzed heme metabolic product, biliverdin (Zhu et al., 2010; Lehmann et al., 2010). However, in the present study SnPP, an inhibitor of HO-1 enzymatic
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epacadostat receptor Importantly other aspects of platelet f
2021-11-22
Importantly, other aspects of platelet function (aggregation, spreading, in vitro and in vivo thrombosis) important for haemostasis and thrombosis were unaltered in Ral DKO platelets and mice. Beyond haemostasis and thrombosis however, platelets have been implicated in numerous pathophysiological pr
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br Conflict of interest statements br
2021-11-22
Conflict of interest statements Acknowledgements Introduction Oral squamous cell carcinoma (OSCC) is the sixth most common cancer worldwide and is the major cause for cancer morbidity and mortality in developing countries. Age standardized incidence rate in India is 12.6 per 100 000 populat
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In summary through medicinal chemistry design and
2021-11-22
In summary, through medicinal chemistry design and computer-assisted conformational modeling, the initial lead was evolved into a series of dihydrobenzofuran derivatives, , as potent GPR119 agonists. Optimization of general structure at various regions of the molecule, including the substituent on
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Due to the high structural similarity between
2021-11-22
Due to the high structural similarity between GlxI and FosA, it is possible that GlxI directed evolution experiments could produce FosA enzymatic activity in a GlxI enzyme. Although the current investigation was unable to detect FosA activity by mutation of a key metal liganding residue in the activ
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Another group of secreted proteins that determine the
2021-11-22
Another group of secreted proteins that determine the virulence of V. dahliae are effectors and microbe associated molecular patterns (MAMP) that regulate plant immunity [10]. So far, there is only one chemokine receptor gene Ave1 cloned in V. dahliae, yet it does not exist in race 2 strains such a
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In spite of the impressive progress made in
2021-11-22
In spite of the impressive progress made in DNA glycosylase assays in recent years, few of them have clearly been viable candidates for further development and implementation in biomedical research and clinical practice. Future research efforts should be devoted to devising assays with improved perf
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Heterocysts provide the required microoxic environment for
2021-11-22
Heterocysts provide the required microoxic environment for the oxygen-sensitive N2-fixing nitrogenase enzyme complex. This environment is formed during heterocyst development. Developing heterocysts inactivate photosystem II and degrade antenna pigments, thereby decreasing oxygenic photosynthesis (F
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Prior to cellular uptake studies of compound
2021-11-22
Prior to cellular uptake studies of Pentylenetetrazole mg , docking simulation was performed (A). The result suggested this complex was capable of binding in the cavity of an outward open XylE. The orientation of the sugar moiety in the docked complex was similar to that of the glucose unit bound i
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SGLT inhibitors have been accepted as
2021-11-22
SGLT-2 inhibitors have been accepted as a new class of antidiabetic agent (Kurosaki and Ogasawara, 2013). They limit renal glucose reabsorption and promote urinary excretion of glucose, thereby reducing plasma glucose levels (de Leeuw and de Boer, 2016, Jojima et al., 2016, Pérez López et al., 2010,
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