• psoralen Primarily because secretase was a therapeutic targe

  2021-11-12

  

  Primarily because γ-secretase was a therapeutic target in AD, a plethora of γ-secretase inhibitors (GSIs) have been developed that effectively inhibit γ-secretase cleavage in humans [16]. Indeed, “druggability” of γ-secretase has not been an issue even when the identity of the target was unknown in

• uPAR promotes cell associated proteolysis

  2021-11-12

  

  uPAR promotes cell-associated proteolysis by binding to uPA which locally converts plasminogen into active plasmin [10]. Ligand-engaged uPAR also acts as a potent regulator of cell migration and matrix attachment. Being a membrane receptor, uPAR needs to interact with extracellular matrix (ECM) prot

• br Introduction Thrombosis is one of

  2021-11-12

  

  Introduction Thrombosis is one of the leading causes of deaths in the cardiovascular diseases such as myocardial infarction (MI), unstable melanotropin and acute coronary syndrome (ACS) in developed countries [1], [2]. It is estimated that venous thromboembolism (VTE) afflicts about 1 million (1–

• Before discovery of their histone demethylase function the J

  2021-11-12

  

  Before discovery of their histone demethylase function, the JARID1 isoforms were identified across diverse fields including stem cell biology and congenital disease, as detailed in Box 2. Their observed roles in cancer progression and therapy resistance have led to ongoing pursuit of inhibitors tail

• The finding of histamine action on ASICs also raises

  2021-11-12

  

  The finding of histamine action on ASICs also raises the question about possible action of other histamine receptor ligands. In the present work we selected several compounds and performed electrophysiological testing of their action on recombinant homomeric ASIC1a and ASIC2a. Nα-methylhistamine is

• vx 809 The mast cell has long been

  2021-11-12

  

  The mast cell has long been recognized as central to the mediation of allergic responses not least because it is the principal repository of histamine in the body. Following activation by allergens, the mast cell can release histamine as well as generate a host of additional mediators such as cystei

• In tumor cells HK II induction is mediated

  2021-11-12

  

  In tumor cells HK-II induction is mediated by Akt/mTOR pathway [6], [11]. HK-II dynamically shuttles between the mitochondria and cytoplasm under different metabolic conditions. In cardiomyocytes, Akt enhances HK-II binding to mitochondria, setting the heart at a state resistant to ischemic injury [

• br Introduction Hexokinase HK is an enzyme that catalyses th

  2021-11-12

  

  Introduction Hexokinase (HK) is an enzyme that catalyses the transfer of phosphate from ATP to glucose in the first step of glucose metabolism (Wilson, 1995, Wilson, 2003). In mammalian, HK has four important isozymes which are designated as HK1, HK2, HK3 and HK4 (Wilson, 1995, Wilson, 2003). HK1

• In the same research group

  2021-11-12

  

  In 2017, the same research group released a free internet accessible database (HemeOxDB, http://www.researchdsf.unict.it/hemeoxdb), to make it easier the analysis of the literature and, consequently, the design of potent and selective HO-1 inhibitors. The database reported the entire set of HO-1 and

• br Methods br Results and discussion br

  2021-11-12

  

  Methods Results and discussion Conclusions In this work, 100-ns MDSs were applied on the WT and on the R155K and D168A single point mutations of the NS3/4A protease in the apo form and in complex with ASV, a current drug in phase III clinical trials. According to the PCA, these two mutatio

• br GSK Glycogen synthase kinase GSK is a ubiquitous

  2021-11-11

  

  GSK-3 Glycogen synthase kinase-3 (GSK-3) is a ubiquitous serine/threonine kinase that is involved in multiple signaling pathways that are crucial for cellular metabolism and proliferation (Doble and Woodgett, 2003, Frame and Cohen, 2001, Grimes and Jope, 2001, Woodgett, 1990). GSK-3 is known to d

• In three groups independently proposed two

  2021-11-11

  

  In 2001, three groups independently proposed two different mechanisms for the catalytic reaction of GlxI [5], [6], [7]. Richter and Krauss (RK) used HF/4–31G calculations of the active site, coupled with a frozen effective fragment potential description [8], [9] of eleven residues in the binding sit

• In response to oxidative stress in DM antioxidant defence sy

  2021-11-11

  

  In response to oxidative stress in DM, antioxidant defence systems are activated in β-cells. Glutathione (GSH) is one of the most abundant antioxidants and has been shown to be expressed at lower concentrations in patients with DM [12], [13]. Furthermore, plasma levels of glycine, which is a synthet

• The post translational modification O GlcNAcylation is

  2021-11-11

  

  The post-translational modification O-GlcNAcylation is also dependent upon glucose fluctuations. O-GlcNAcylation has been linked to insulin resistance and glucose toxicity in diabetes and its comorbidities [11]. O-GlcNAcylation is a dynamic modification tightly regulated by the nutritional sensor UD

• br Materials and methods br Results Bgal from Alteromonas

  2021-11-11

  

  Materials and methods Results Bgal from Alteromonas sp. ML117 had an open reading frame of 3126 bp encoding 1042 amino Tivozanib mg residues with a predicted mass of 120 kDa and a theoretical pI (isoelectric point) of 5.44. The recombinant Bgal contained a His tag, as well as other additional

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