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Finally the formation of a regular network of
2022-05-13
Finally, the formation of a regular network of fusion glycoproteins in their post-fusion state is not exclusive of vesiculovirus G. More or less regular networks have been also observed with other class III fusion glycoproteins such as pseudorabies gB [85] and several class II fusion glycoproteins [
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Moreover we revealed that alanine and taurine a structural a
2022-05-13
Moreover, we revealed that β-alanine and taurine, a structural analog of β-alanine, have different receptor affinity in the SG neurons of the spinal dorsal horn. Additionally, previous studies indicate that taurine regulates nociceptive information at the spinal cord level, and we have previously de
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At the second step blind docking simulation of independent r
2022-05-13
At the second step, blind docking simulation of 150 independent runs was performed with smaller grid box. Structures of open (1v4t.pdb), semi-closed (4dch.pdb) and two structures of closed configuration of GK (pdb codes are 1v4s and 3vev) were used for simulation (for detailed explanations on can se
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The effect of the selected compounds on
2022-05-13
The effect of the selected compounds on NF-kB transrepression was assessed using the well-studied HeLa B2 cell line that expresses endogenous GR and NF-kB family members and responds properly to glucocorticoids and pro-inflammatory cytokines (such as TNF). Our data revealed that the two hit compound
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The widespread involvement of HH GLI
2022-05-13
The widespread involvement of HH/GLI in human malignancies has initiated a remarkable effort to identify selective HPIs. As shown in Table 2.1, most of these small molecule inhibitors target the essential effector protein SMO, which should lead to pathway abrogation by eventually decreasing the GLIA
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The NVC response in the diseased
2022-05-13
The NVC response in the diseased or aging HBC may be altered, including changes in both the chemical mediators of NVC, ion channel behaviour, and the dynamics of the vascular system. For example, in Alzheimer’s disease the production of NO is shown to be inhibited (Lourenço et al., 2014), hypertens
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FXR agonists represent an attractive class
2022-05-12
FXR agonists represent an attractive class of drugs for patients with PFIC. Synthetic and semi-synthetic FXR agonists, with higher affinity and potency to activate FXR, have been successfully tested in animal models of cholestasis. In these murine models, the semi-synthetic steroidal FXR ligand obet
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Another TKI used in cancer therapy is
2022-05-12
Another TKI used in cancer therapy is the Abl inhibitor imatinib mesilate which has also a beneficial effect on glucose homeostasis in diabetic humans [39], [40], [41]. Imatinib has a clear impact on NFκB activation and anti-apoptotic preconditioning of β-cells [39], attenuating islet inflammation [
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Herein we describe the design and optimization of fused
2022-05-12
Herein, we describe the design and optimization of fused-ring phenyl propanoic acids as novel GPR40 agonists, leading to the discovery of compound 40a which exhibits excellent pharmacokinetic properties, improved hepatobiliary transporter inhibition, and significant glucose-lowering efficacy during
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br Fenton reaction based nanomaterials for ferroptosis In
2022-05-12
Fenton reaction-based nanomaterials for ferroptosis In Fenton reaction, H2O2 is converted by Fe2+ or Fe3+ to highly oxidative ROS (Eqs. (1) and (2)), which is commonly used to catalyze the degradation of refractory organics [34]. Since the tumor microenvironment is characterized by low acidity an
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br Conclusions Our in vitro and in vivo data collectively
2022-05-12
Conclusions Our in vitro and in vivo data collectively demonstrate that zifaxaban is effective in preventing thrombus formation via direct and specific inhibition of FXa in a dose-dependent manner. Furthermore, zifaxaban has a potency that is similar to that of rivaroxaban and shows a similar or
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Collectively these observations demonstrate that FAAH is fun
2022-05-12
Collectively, these observations demonstrate that FAAH is functionally positioned to modulate the actions of AEA and other NAEs on BLA neurons and anxiety processes mediated by this region. By extension, manipulations that lead to alterations in FAAH activity, such as stress or administration of com
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Whether histamine receptor distribution is altered in
2022-05-12
Whether histamine receptor distribution is altered in canine GI diseases remains unknown, but human research has documented altered histamine receptor density in certain GI diseases (Sander et al., 2006, Deiteren et al., 2015, Von Rahden et al., 2011). Additionally, a novel H4 receptor antagonist, J
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The relationship between the attention deficit hyperactivity
2022-05-12
The relationship between the attention deficit hyperactivity disorder (ADHD) and H3Rs is supported by several reports (Berlin et al., 2011; Passani, Bacciottini, Mannaioni, & Blandina, 2000; Vohora & Bhowmik, 2012). ADHD is a neurobehavioral disorder with high prevalence in children, with hyperactiv
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Finally life expectancy was strongly reduced in STK deficien
2022-05-12
Finally, life expectancy was strongly reduced in STK4-deficient patients. Even in those patients who received haematopoietic stem cell transplantation, the majority of patients died due to transplantation-related complications, raising the question whether MST1 expressed in nonhaematopoietic tissue
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