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DDI is one of the main problems with serious clinical
2020-11-16
DDI is one of the main problems with serious clinical consequences in clinical settings. Several reports have highlighted the role of modulation of drug-metabolizing enzymes, especially CYP450 s, as a major mechanism involved in clinical DDIs [3,4,7]. The present study aimed to investigate the effec
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Physiological changes induced by CRF are
2020-11-16
Physiological changes induced by CRF are mediated through CRF1 and CRF2 receptors (Chang et al., 1993, Lovenberg et al., 1995). Previous findings with CRF1 receptor antagonists showed that activation of CRF1 receptor is involved in maternal separation-induced ultrasonic vocalizations (Kehne et al.,
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Under conditions of energy scarcity or
2020-11-16
Under conditions of energy scarcity or nutritional restriction, AMPK, a critical energy sensor, is activated in response to the increased ratio of AMP to ATP. Various kinases may phosphorylate AMPK, leading to its activation. For example, AMPK phosphorylation by liver kinase B 1 (LKB1) at Thr172 res
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br Objectives br Study design Thirty KTx http www
2020-11-16
Objectives Study design Thirty KTx recipients were enrolled in this pilot study from December 2015 to May 2016. Patient demographics are presented in Table 1. The inclusion criteria were: age ≥ 18 years and CMV-IgG serostatus (D+/R−, D+/R+, D−/R+) pre-Tx. All patients were enrolled during the
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estrone receptor To develop novel EPAC inhibitors Zhou
2020-11-14
To develop novel EPAC inhibitors, Zhou and co-workers optimized the HTS hit as the chemical lead. After modifications of the substituents on the phenyl ring or C6-position of compound , compound () was identified to be the more potent compound in this series with an IC value of 4.0µM (EPAC2). Dock
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OxLDL down regulates eNOS and up regulates iNOS thereby
2020-11-14
OxLDL down-regulates eNOS and up-regulates iNOS, thereby augmenting the formation of NO and protein S-nitrosylation in human endothelial PRX-08066 synthesis [26]. Importantly, iNOS-mediated S-nitrosylation plays an increasingly significant role in cardiovascular diseases [34]. For example, iNOS-med
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Although the reasons why viral RNA does
2020-11-13
Although the reasons why viral RNA does not bind to and activate PKR in WNV-infected cells are not known, some of the known characteristics of flavivirus infections provide possible clues. The viral ionomycin mg protein forms dimers that associate with ER membranes and viral RNA (Lindenbach et al.,
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br Multi subunit RINGs There are RING type E
2020-11-13
Multi-subunit RINGs There are RING-type E3s that exist as multi-subunit assemblies (see Fig. 3B). A striking example is the Cullin RING Ligase (CRL) superfamily [35], which exhibits enormous plasticity in substrate specificity. Each CRL subfamily is characterized by a cullin protein (Cul-1, 2, 3,
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br Activity based probes br Characterization of coronavirus
2020-11-13
Activity-based probes Characterization of coronavirus-encoded DUBs with activity-based probes To study the activity of specific DUBs, investigators frequently take advantage of the ~10kDa (monoUb or Ubl ABP) or ~20kDa (DiUb ABP) increase in MW on probe labeling. SDS-PAGE analysis or blotting f
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br Patients and Methods Patients who had been initiated
2020-11-13
Patients and Methods Patients who had been initiated on a DPP-4 inhibitor (see in the online version at doi:10.1016/j.clinthera.2018.06.002) between April 2012 and June 2017, when the common threshold for dose adjustment for all non-linagliptin DPP-4 inhibitors was a creatinine clearance (CrCl) l
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A range of inhibitors were therefore synthesized containing
2020-11-13
A range of inhibitors were therefore synthesized containing either carboxylic rgs protein 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 (). Analysi
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For a physiologically relevant interaction ligand and
2020-11-13
For a physiologically relevant interaction, ligand and receptor have to be expressed in the same place. Collagen II is found primarily in cartilage. DDR2 is expressed in proliferating chondrocytes in vivo, and its staining pattern in tibial growth plates is similar to that of collagen II. In additio
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The fibrillogenesis process of collagen is
2020-11-13
The fibrillogenesis process of collagen is understood to initiate in the extracellular space near the plasma membrane where secretory vesicles form regions of deep invagination. However, it is not clear how and when collagen-binding proteins interact with collagen molecules during fibrillogenesis or
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br The role of chemokine and AD Chemokines
2020-11-13
The role of chemokine and AD Chemokines are small cytokine proteins that are involved in various immunological and physiological functions. These proteins can be involved in cell migration and localization during homeostasis and inflammation, and as such, they were named chemokines [80]. Chemokin
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To date methods for the simultaneous analysis of multiple
2020-11-13
To date, methods for the simultaneous analysis of multiple probe drugs in the plasma have been described by using HPLC-DAD or LC–MS/MS. Although previous cocktail methods have used combinations of those four or other probe drugs with LC–MS/MS methods, most of those studies focused on only the analy
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