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Ponesimod A variety of quinazoline or
2022-11-29
A variety of quinazoline or fused pyrimidine-substituted diaminotriazoles showed sub-100nM inhibition of Axl (). Diaminotriazoles similarly substituted with quinolines, isoquinolines and benzothiazoles also showed potent Axl activity (data not shown), but generally exhibited potent cytotoxicity and
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In mice the Tfm mutation
2022-11-24
In mice, the Tfm mutation increased the anxiety-state assessed in the novel object and in light/dark box tests, whereas no changes were detected in the open field or elevated plus maze tasks (Zuloaga et al., 2008). As for Tfm rats, this seemed to be related to an increased HPA response to stress. Th
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br AR signals and chemosensitivity in urothelial
2022-11-24
AR signals and chemosensitivity in urothelial cancer A significant amount of patients with urothelial cancer fail to respond to cisplatin-based systemic chemotherapy, although it remains the mainstay of successful management of advanced disease. However, underlying mechanisms for chemoresistance
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Not all secondary metabolites or natural
2022-11-24
Not all secondary metabolites or natural products can be fully synthesized due to their very complex structures that are too difficult and expensive on industrial scale. Hence, there is an urgent need to search for alternative remedies as naturally occurring biologically active secondary metabolites
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Oxytocin br Experimental methods br Acknowledgments br Intro
2022-11-24
Experimental methods Acknowledgments Introduction Long-term potentiation (LTP) and long-term depression (LTD) at excitatory synapses are thought to underlie experience-dependent learning and memory. These synaptic plasticity mechanisms are best characterized at hippocampal CA1 synapses, whe
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With regard to participation of the S lipoxygenase in diabet
2022-11-24
With regard to participation of the 12S-lipoxygenase in diabetes mellitus, inconsistent results have been obtained. Earlier studies demonstrated that the leukocyte-type 12S-lipoxygenase is specifically expressed in pancreatic b-cells and is involved in regulating glucose-stimulated insulin secretion
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and LO are members of the
2022-11-24
5- and 12/15-LO are members of the lipoxygenase family that convert arachidonic meclofenamate into lipid mediators such as leukotriene B4 (LTB) and 12()-hydroxyeicosatetraenoic acid (HETE) and 15()-HETE, respectively. Evidence from several in vitro and in vivo studies has shown that activation of t
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There are two ways to transport FFAs into cells
2022-11-22
There are two ways to transport FFAs into cells. First by passive diffusion. Second as the putative long-chain fatty BAPTA-AM transporters are proposed, CD36 the plasma membrane-associated fatty acid-binding protein (FABPpm) and fatty acid transport proteins (FATP) [11], where CD36 is responsible f
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br Endocytosis of AdipoR Surface receptor activity may be
2022-11-22
Endocytosis of AdipoR1 Surface receptor activity may be shut down by endocytic uptake and subsequent lysosomal degradation of the proteins [20]. Clathrin-dependent endocytosis (CDE) has been extensively studied and internalization from the plasma membrane is mediated through clathrin-coated pits
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br Endocytosis of AdipoR Surface receptor activity may be
2022-11-22
Endocytosis of AdipoR1 Surface receptor activity may be shut down by endocytic uptake and subsequent lysosomal degradation of the proteins [20]. Clathrin-dependent endocytosis (CDE) has been extensively studied and internalization from the plasma membrane is mediated through clathrin-coated pits
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Some alterations in the integrity of cell membranes caused b
2022-11-21
Some alterations in the integrity of cell membranes caused by toxic agents can be determined by measuring certain enzymes released by damaged cells [8]. The cholinesterases, for example, catalyze the hydrolysis of Procainamide HCl (ACh) in choline and acetic acid. Theses enzymes are divided into tw
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gamma-Glu-Cys sale Our studies also reveal the
2022-11-19
Our studies also reveal the normal functional roles of the MIR. Interaction between the MIR loop and the N-terminal α helix nucleates conformational maturation of AChR subunits, thereby promoting assembly of mature AChRs [52], [55]. This interaction in homologous parts of all AChR subunits appears t
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IC values were obtained for an expanded version of
2022-11-18
IC50 values were obtained for an expanded version of the fragment library using the previously described mobility shift assay. Subsequently, Ki values were estimated from IC50 values to allow better comparison of the activity against targets which were measured at different substrate concentrations
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br Introduction In addition to ATP production an important
2022-11-18
Introduction In addition to ATP production, an important role of mitochondria in the pancreatic beta cell is anaplerosis, which is the net synthesis of citric na ca exchanger cycle intermediates that are exported to the cytosol where they are converted to numerous other metabolites that stimulat
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br Results br Discussion Context specific and dynamic post
2022-11-18
Results Discussion Context-specific and dynamic post-translational protein modifications are well-established regulators of the signaling pathways that protect eukaryotic DNA integrity during the tremendous task of replication. Advancements in speed, resolution, and sensitivity of MS-based tec
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