• The inhibition of NSAIDs towards GLOI

  2022-02-25

  

  The inhibition of NSAIDs towards GLOI provides a direction for the development of novel effective GLOI inhibitors. Although the inhibitory activity of indomethacin was determined and the interactions between it 98 8 australia and GLOI were probed by NMR titration experiments, no detailed inhibitory

• To test our refinement protocol we considered

  2022-02-25

  

  To test our refinement protocol, we considered a benchmark set of 12 N-linked glycan-containing protein structures determined by X-ray crystallography at resolutions ranging between 1.9 Å and 3.5 Å and comprising a total of 133 glycan units. We identified four incorrect anomeric configurations and 2

• Resolving the molecular details of glyco

  2022-02-25

  

  Resolving the molecular details of (glyco)proteome variation in different tissues and organs of the human body is critical for the understanding of human biology and disease [59]. Glycoproteomic analysis of disease-related tissues and cells has provided valuable information to identify promising tar

• br Perspectives br Contributors BP study concept

  2022-02-25

  

  Perspectives Contributors BP: study concept & design, literature review, data analysis & synthesis & presentation, primary draft of the manuscript; JDR: data analysis, Fig. 1 illustration, manuscript review & revision; ZP: study concept & design, manuscript review & edit; MI: manuscript review

• The amino hydroxy methyl isoxazolepropionic acid AMPA recept

  2022-02-25

  

  The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic zj to j (AMPA) receptors are related ionotropic glutamate receptors (iGluRs) that mediate fast excitatory neurotransmission, and are also typically heteromeric ion channels, composed of GluA2 subunits in conjugation with GluA1, GluA3, or GluA4 subu

• br Results and discussion A diverse set of compounds were

  2022-02-25

  

  Results and discussion A diverse set of compounds were synthesized to improve the PK and physicochemical properties of 2. Compounds' agonist effects on hGPR40 were assessed by calcium mobilization assay using hGPR40-HEK293 cell line which stably expressed human GPR40. Preliminary explorations fo

• br Results br Discussion Postsynaptic trafficking of AMPA re

  2022-02-25

  

  Results Discussion Postsynaptic trafficking of AMPA receptors, a process responsible for maintaining the steady-state level of AMPA receptor synaptic transmission, is believed to also actively partake in glutamatergic synaptic plasticity in principal neurons, such the hippocampal CA1 cells. He

• Given the important role of Cx in

  2022-02-25

  

  Given the important role of Cx43 in maintaining the function of gap junctions, to investigate the effects of stress on Cx43 may be an important step towards understanding the mechanism underlying CUS-induced dysfunction of gap junctions. Corticosterone (CORT), as an important stress hormone, has bee

• Glucocorticoid is a major regulator of body s response to

  2022-02-25

  

  Glucocorticoid is a major regulator of body's response to stress (Armario, 2006). Repeated injections of the glucocorticoid corticosterone (CORT) in mice have been shown to produce an animal model of depression (Zhao et al., 2008). Further study of this phenomenon suggested that prolonged CORT expos

• Our own search towards aryl imidazole derived GSMs

  2022-02-25

  

  Our own search towards aryl-imidazole derived GSMs led to the discovery of the benzimidazole derivative (). It is one of the most potent GSMs to date, suffering however from sub-optimal drug-like properties. More recently, we have described the design and synthesis of bicyclic triazolo-derivatives,

• The active site of PS is

  2022-02-25

  

  The active site of PS1 is located at the interior of its TM horseshoe-like fold (29) (Fig. 1). TM2 and TM6 serve as “doors” for substrate entry (30), as also observed in recent molecular dynamics (MD) simulations of the PS1 subunit (31). Recent coarse-grained (CG) and atomic simulations also showed

• RDL is of interest as it is the

  2022-02-25

  

  RDL is of interest as it is the target of highly effective insecticides (Buckingham et al., 2005, Raymond-Delpech et al., 2005). Point mutations, particularly an alanine to serine or glycine mutation in TM2, underlie resistance to several insecticides, including dieldrin, picrotoxinin and fipronil (

• We focus here on the historical discoveries that led to

  2022-02-24

  

  We focus here on the historical discoveries that led to the development of the concept of ferroptosis. Ferroptosis is defined as an iron-dependent form of regulated cell death, which occurs through the lethal accumulation of lipid-based reactive oxygen species (ROS) when glutathione (GSH)-dependent

• The normal function of the FBPase enzyme is to

  2022-02-24

  

  The normal function of the FBPase enzyme is to catalyze the hydrolysis of F1,6BP to F6P. This activity is induced by diabetes and starvation and is increased in diabetic rats. The level of FBPase can be normalized by insulin, however, similar information is not available from diabetic patients. FBPa

• Data of initial analogs have been shown

  2022-02-24

  

  Data of initial analogs (±)-– have been shown in wherein SAR was observed for the intended change of the right-hand side pyridin-3-yl ring of to various other -containing heteroaryl ring (Ar) disposing the ring- at different directions. Based on consistent human and rat FAAH potency as well as int

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