• Docking studies were performed on the selected compounds

  2022-10-27

  

  Docking studies were performed on the selected compounds to explore their binding patterns and to examine SAR in more detail. The co-crystal structure of ATX in complex with PF-8380 (PDB code: ) was selected for the docking studies due to structural similarity of the most potent compound with PF-838

• Pompe disease is accompanied by

  2022-10-27

  

  Pompe disease is accompanied by the deficiency of the lysosomal α-1,4-glucosidase that makes the NLG919 unable to hydrolyze glycogen to glucose, thereby resulting in the accumulation of glycogen in lysosomes, especially in skeletal muscles and cardiac tissues. This accumulation results in the struc

• br Autophagy and cell death pathways in ischemic

  2022-10-27

  

  Autophagy and cell death pathways in ischemic stroke Although very important for the effects on post-ischemic HBC injury, autophagy is not the only mechanism of action involved in cell death. Necrosis and apoptosis are two other distinct forms of cell death with great difference in morphology an

• Introduction The MMR system keeps the fidelity of

  2022-10-27

  

  Introduction The MMR system keeps the fidelity of replication by repairing replication errors such as base-base mispairs and insertions/deletions. It plays a substantial role in restoring the fidelity of DNA and contributing to genome integrity [1]. The components of MMR are conserved in a broad ra

• Enhanced arginase activity and the resultant decreases

  2022-10-27

  

  Enhanced arginase activity and the resultant decreases in L-arginine levels can also impair T cell mediated immune function and allow tumor growth by limiting the supply of L-arginine needed for the formation of cytotoxic levels of NO by iNOS [10]. Increased arginase expression/activity may also lim

• Plant defensins Vriens et al and linear AMPs Domingues et

  2022-10-27

  

  Plant defensins (Vriens et al., 2014) and linear AMPs (Domingues et al., 2015, Liu et al., 2008) have been shown to present several modes of action. Among these different mechanisms, permeabilization of the fungal membrane has been described as a secondary effect of plant defensin action (Vriens et 

• The current study was designed to investigate the effects of

  2022-10-26

  

  The current study was designed to investigate the effects of the 12/15-LOX inhibitor, LOXBlock-1 (LB1) in mice using a FeCl3-induced distal MCAO model, and to test its utility in conjunction with subsequent thrombolysis with tPA, which is to date the only FDA-approved drug for acute stroke treatment

• Both AD and dyslipidemias are global public

  2022-10-26

  

  Both AD and dyslipidemias are global public health problems, and an increase in their incidence over the next decades is expected. Among many triggering elements, the increase in life expectancy is one of the main risk factors associated with the increase in the incidence of AD. Meanwhile, dyslipide

• Two cell surface trans membrane receptors have been identifi

  2022-10-26

  

  Two cell-surface trans-membrane receptors have been identified for adiponectin, AdipoR1 and AdipoR2 [21], and adiponectin action is known to signal through these receptors and the docking protein APPL1 [22]. In muscle and liver cells, signal transduction involves the phosphorylation and activation

• Introduction Diabetic nephropathy is a rapidly

  2022-10-26

  

  Introduction Diabetic nephropathy is a rapidly growing cause of end-stage renal disease [1]. Glomerular, tubular and vascular toxicity resulting from hyperglycemia (glucotoxicity) have been evaluated extensively at the molecular level as contributing factors for diabetic nephropathy [[1], [2], [3]]

• br Conclusions Several lines of evidence have

  2022-10-26

  

  Conclusions Several lines of evidence have been established, which support the adenosine kinase hypothesis of epileptogenesis, which is based on a sequence of events leading from acute HPF injury to initial downregulation of ADK, rise in extracellular adenosine, changes in astrocytic adenosine re

• In terms of the ring B

  2022-10-26

  

  In terms of the ring B C5′ position, while C5′-F (compound ) was tolerated, C5′-Me (compound ) and C5′-Cl (compound ) substitutions resulted in a loss in potency. However, the C5′-OMe substitution (compound ) resulted in a ∼3-fold increase in potency compared to . Modeling suggested a pseudo hydroge

• serine threonine protein kinase To date more than different

  2022-10-26

  

  To date, more than 50 different mutations in the gene have been described (Human Gene Mutation Database at the Institute of Medical Genetics in Cardiff: SRD5A2 Gene: http://www.hgmd.cf.ac.uk). Most of them are missense mutations but premature stop codons and deletions leading to non-functional or su

• The knowledge on the structure of CYP including its

  2022-10-26

  

  The knowledge on the structure of CYP17, including its active site, provides a rationale for understanding many mutations that are found in enzyme dysfunction in clinical disease as well as the enzyme's dual hydroxylase and lyase catalytic capabilities. This knowledge will assist rational drug desi

• br Methods br Results br Discussion Autotaxin has been shown

  2022-10-26

  

  Methods Results Discussion Autotaxin has been shown to have effects on major cell types implicated in OA, notably chondrocytes, osteoblasts, osteoclasts, and synoviocytes, through its enzymatic product LPA [20]. However, a paucity of research exists on the involvement of autotaxin in OA. Fi

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