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A number of synthetic GPR
2021-11-10

A number of synthetic GPR119 agonists have been reported to date, several of which have advanced into clinical trials. Reported GPR119 agonists are often composed of three parts as depicted in : a piperidine or a piperazine ring -substituted with a carbamate or a heteroaryl group at the right side,
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CD binding to gp causes a large scale conformational change
2021-11-10

CD4 binding to gp120 causes a large scale conformational change of gp120 which involves the gp120 core structure and the transitions of inner-domain layers (layer 1, 2 and 3), but also involves the movement of the major loops (V1, V2 and V3) [16], [17], [18], [19]. For instance, the V2-loop joins th
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Armed with this knowledge we looked at ways to
2021-11-10

Armed with this knowledge, we looked at ways to reduce the log of through nitrogen incorporation while still maintaining potency via installation of ortho substituents such as chloro, methyl, bromo, and thiomethyl (). In general, pyridine analogs were less active ( vs ; vs ; vs ) than their simple p
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Among the various delivery strategies in the
2021-11-10

Among the various delivery strategies in the field of nano-DDS, developing smart targeted nanocarriers has long been a research focus for pharmaceutical scientists11., 12.. The ideal drug delivery outcome must be precisely delivering the therapeutic agents to their sites of action, especially for an
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With taurine or other molecules that might
2021-11-10

With taurine, or other molecules that might be transported by Eaat2, an important area of research will be how such a chemical regulates sleep. Indeed, taurine has been described to act on the nervous system in disparate ways — it can act as an inhibitory neurotransmitter, but also has a well-charac
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An important difference between glucokinase and
2021-11-10

An important difference between glucokinase and the other hexokinases is that it has a much lower affinity for glucose, such that it is not saturated at physiological blood glucose concentrations (Wilson, 1995, Wilson, 1997, Wilson, 2003, Wilson, 2004, Cárdenas et al., 1998). In addition, glucokinas
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The present study showed that
2021-11-10

The present study showed that the FPR2 antagonists PBP10 and BOC2 are potent antiviral molecules in vitro against a broad range of IAV and B viruses. Consistently, our previous report showed that FPR2 plays a deleterious role during IAV infections and that another FPR2 antagonist WRW4 inhibits IAV r
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br Materials and methods br Results br Discussion In this
2021-11-10

Materials and methods Results Discussion In this study, we identified a novel AMP scolopendrasin X from Scolopendra subspinipes mutilans through genome analysis. Scolopendrasin X stimulated neutrophil activity, resulting in calcium increase, chemotactic migration, and superoxide anion produ
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br FGF FGFR pathway as predictive factor Several
2021-11-10

FGF/FGFR pathway as predictive factor Several studies have identified FGFR1 amplification as the major predictive factor of response to FGFR inhibitors [26], [27]. However, in a recent study on lung cancer cell lines with ponatinib, FGFR1 mRNA and protein expression, together with FGF2 and FGF9 m
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Corresponding to the different insulinotropic signaling
2021-11-10

Corresponding to the different insulinotropic signaling, the competitive radioligand-binding studies demonstrated at least 3 distinct protein kinase g on GPR40: orthosteric binding site for endogenous ligands, allosteric binding site for partial agonists and another allosteric binding site for full
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br Significance Metabolites present in the extracellular env
2021-11-10

Significance Metabolites present in the extracellular environment can potently modulate cellular phenotypes and potentially serve as therapeutics for various diseases. Ferroptosis is a non-apoptotic cell death process characterized by the generation of toxic lipid reactive oxygen species (ROS). I
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br Experimental procedures br Conflicts of interests br Intr
2021-11-10

Experimental procedures Conflicts of interests Introduction Here we investigate differences in growth properties and short-term morphological changes in response to ET-1 in Chinese hamster ovary (CHO) cells stably and separately expressing ETA or ETB receptors. A stably transfected CHO syst
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It has been found that WHI P a JAK
2021-11-09

It has been found that WHI-P131, a JAK3 inhibitor, induced apoptosis of CD4+ T 740 Y-P (Cetkovic-Cvrlje et al., 2012). Also, other JAK3 inhibitors (AG490 and WHI-P154) caused apoptosis in anaplastic large cell lymphoma (Amin et al., 2003). Taking into account the proapoptotic action of JAK inhibito
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br Conflict of interest br Introduction
2021-11-09

Conflict of interest Introduction Milk and dairy products are nutritious foods that provide lactose, calcium, phosphorous, magnesium and proteins, among other nutrients, which have been reported to have a fundamental role in bone development and healthy diets. An adequate consumption of dairy
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It is noted that knee
2021-11-09

It is noted that knee swelling was milder and the intensity of IL-4 staining (MFI) in the vehicle-treated group was lower in the second (Fig. 7a and d) than the first (Figs. 1a and 3f) AIA experiment. The variation in joint swelling between the two studies is most likely due to the models being perf
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