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The most significant source of
2021-05-21

The most significant source of DAG originates from the PLC family of enzymes, which produces DAG in an agonist-regulated reaction. PLCs constitute a wide family of enzymes acting on both phosphatidilinositols (PI) and phosphatidilcoline (PC) (Li et al., 2010) in the plasma membrane and other intrace
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br Introduction Noncanonical nucleoside triphosphates NTPs s
2021-05-21

Introduction Noncanonical nucleoside triphosphates (NTPs; such as deoxyinosine triphosphate (dITP), deoxyxanthosine triphosphate (dXTP), 8-oxo-deoxyguanosine triphosphate, and 2-oxo-deoxyadenosine triphosphate are produced from oxidation, deamination, or other modifications of canonical nucleotid
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br Fragment based drug discovery FBDD is a
2021-05-21

Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical PHA-848125 synthesis space with libraries which are smaller in size, producing drug leads with high ligand-binding effici
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br Materials and methods br Results Metabolic stability of
2021-05-21

Materials and methods Results Metabolic stability of compounds was studied by incubation with pooled human liver microsomes. Piperine was the metabolically most stable compound, with a t1/2 of 141min (Fig. 2, and Table 1). SCT-29 and LAU 397 showed t1/2 of approx. 45min, whereas a t1/2 of only
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It is interesting to note
2021-05-20

It is interesting to note that Eibinger and colleagues [23] recently reported chemotactic movement to 25-OHC in THP1 cells as well as in primary human monocytes. RNA interference suggested that in part this migration was mediated by EBI2. Competing financial interest statement Acknowledgments
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A range of inhibitors were therefore synthesized containing
2021-05-20

A range of inhibitors were therefore synthesized containing either carboxylic GSK J4 free base sale or ester functionality at the ‘tail’ group as well as variations in the ‘head.’ These were assayed in vitro using the DCIP assay for binding affinity against and human DHODH at 50μM, respectively ()
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It has been reported that
2021-05-19

It has been reported that CysLT2 receptors negatively regulate CysLT1 receptor-mediated response in allergic airway inflammation in mice. Knockdown of CysLT2 receptors augmented CysLT1 receptor-mediated mast cell proliferation [31] and eosinophilic airway inflammation induced by antigen challenge in
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Zanamivir br Pre clinical combination studies
2021-05-19

Pre-clinical combination studies using CSF-1/CSF-1R inhibitors In preclinical models, the CSF-1R pathway can be blocked by using either small molecule kinase inhibitors (GW2580 [30], PLX3397 [31], Ki20227 [32], BLZ945 [33] and CYC11645 [34]), antibody-mediated inhibition of CSF-1 using 5A1 [35] o
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The corticotropin releasing factor CRF
2021-05-19

The corticotropin-releasing factor (CRF) also referred to as corticotropin-releasing hormone, is a key mediator of mammalian endocrine, behavioral, autonomic, and immune responses to stress (Vale et al., 1981, Owens and Nemeroff, 1991, Bale and Vale, 2004). Within the hypothalamic–pituitary–adrenal
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Z-Ligustilide Pahlavanzadeh and Fakouri Baygi employed PC
2021-05-19

Pahlavanzadeh and Fakouri-Baygi [6] employed PC-SAFT EoS to predict the Z-Ligustilide of carbon dioxide by aqueous MEA solutions. They used the ideal form of Smith–Missen algorithm to calculate liquid phase concentrations. The results illustrate acceptable accuracies so that the AAD was achieved eq
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br Conclusion br Introduction The morphological variability
2021-05-19

Conclusion Introduction The morphological variability of aquatic plants is well documented, and in some cases has seriously constrained taxonomic resolution (Sculthorpe, 1967, Santamaría, 2002). Many of these variations are caused by the extensive phenotypic plasticity of aquatic plants, but t
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br Pathophysiology of premature ovarian
2021-05-19

Pathophysiology of premature ovarian failure By the age of 40 years, 1% of women spontaneously develop POF [18]. The normal menopause occurs at an average age of 51 years [19] and results from ovarian follicle depletion [20], whereas POF is a heterogeneous disorder and can result from either foll
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The new ESC guidelines incorporate data from
2021-05-19

The new ESC guidelines incorporate data from a network meta-analysis of 100 studies confirming that new-generation drug-eluting stents (DES) improve survival compared with medical treatment, although this has not been demonstrated in any individual study. REVASCULARIZATION IN NON–ST-ELEVATION ACU
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Other studies have investigated the role of
2021-05-19

Other studies have investigated the role of HDAC inhibitors in particular signaling pathways mediated by EWS–FLI1 (Matsumoto et al., 2001). A recent investigation, showed a physical association of EWS–FLI1 and HDAC1 that helps mediate a disruption in the p53 activation of downstream targets (Li et a
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Epac proteins consist of a carboxyl terminal catalytic regio
2021-05-19

Epac proteins consist of a carboxyl-terminal catalytic region and an amino-terminal regulatory region, which harbors one cAMP-binding domain in Epac1 and two in Epac2 [22], [32], [51]. In the absence of cAMP, the regulatory region covers the CDC25-homology domain and autoinhibits Epac's enzymatic ac
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