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The pharmacokinetic properties of were amenable to oral dosi
2022-05-09
The pharmacokinetic properties of 12 were amenable to oral dosing allowing in vivo comparison to 6. Compared to a maximum efficacious dose of 6 (60mg/kg), 12 demonstrated improved glycemic control during OGTT in high-fat fed/STZ treated (HF/STZ) and BDF/diet-induced obesity (DIO) mouse models of typ
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br Molecular mechanisms and pathways
2022-05-09
Molecular mechanisms and pathways for ferroptosis regulation As to the regulation of lipid peroxidation, iron and related ROS metabolism involved in ferroptosis, many molecular mechanisms and pathways have been presented. It is generally believed that cystine/glutamate antiporter system Xc−, GPX4
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integrin signaling pathway The replenishment time course of
2022-05-09
The replenishment time course of already-tethered vesicle to became release ready, was examined by TIRFM imaging combined with calcium uncaging. By UV-flash photolysis of caged calcium, intracellular calcium concentration raises rapidly and homogenously throughout the cell (Ellis-Davies, 2008). Upon
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KDM D also known as JARID D or SMCY is
2022-05-09
KDM5D (also known as JARID1D or SMCY) is encoded on the Y chromosome and until now it has been implicated in prostate cancer invasion and metastasis [42], spermatogenesis [43], and sex-specific tissue transplantation rejection [44]. KDM5D acts as a direct epigenetic modulator, and as one of the four
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br HO and cerebral malaria In a post mortem evaluation
2022-05-09
HO-1 and cerebral malaria In a post-mortem evaluation of human cerebral (falciparum) malaria, strong HO-1 immunostaining was consistently noted in microglia/macrophages within and surrounding the pathognomonic Durck’s granulomas (Schluesener et al., 2001). As witnessed in cerebral trauma specimen
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PD 151746 Furthermore we observed a striking difference betw
2022-05-09
Furthermore, we observed a striking difference between BR 11257 and activators from the dicarboxylic PD 151746 type in thermofluor measurements on thermostability. The dicarboxylic acids cinaciguat [30] and BAY 60-2770 (see Fig. 3) induced a significant melting temperature increase of sGC. In combi
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CAY10683 br Introduction Soluble guanylyl cyclase GC maintai
2022-05-09
Introduction Soluble guanylyl cyclase (GC-1) maintains vascular function through the NO/GC-1/cGMP pathway [1,2] by catalyzing the conversion of GTP into cGMP (Fig. 1). The GC-1 heme prosthetic group binds NO with picomolar affinity, resulting in a 100- to 200-fold increase in catalytic activity.
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For several years CXCL had
2022-05-07
For several years, CXCL17 had been classified as an orphan chemokine, until Maravillas-Montero et al. claimed that orphan G-coupled protein receptor GPR35 is the receptor of CXCL17 [15], [16]. However, no following research has been produced to further explore the function of the CXCL17-CXCR8 (GPR3
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One difficulty in studying gp is that it binds
2022-05-07
One difficulty in studying gp120 is that it binds to more than one receptor. Understanding how Mouse GDF-8 / Myostatin / MSTN Protein (Fc Tag) (Cytokine) respond to gp120 is complex because of this promiscuity. In an attempt to establish the contribution of CXCR4 in the antagonistic effect of gp12
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As preclinical toxicity and efficacy both appear
2022-05-07
As preclinical toxicity and efficacy both appear to be associated with GlyT1 inhibition, it remains to be determined whether on-target toxicity can be separated from efficacy. The present study evaluated a series of GlyT1 inhibitors for target potency, mode of inhibition, residence time, activity in
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To further explain the energy differences between
2022-05-07
. To further explain the energy differences between Group-A and Group-B, the average distances between ligands and the zinc cation were obtained from the last 1ns trajectory. It turns out that the members of group A were within the coordination distance of the zinc ion, whereas those of group B stay
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orthopoxvirus variola For several parasites of veterinary im
2022-05-07
For several parasites of veterinary importance, there is a growing body of evidence that resistance to ML is, at least in part, mediated by ABC transporters (P-glycoproteins) (Whittaker et al., 2017). P-glycoproteins (Pgps) are members of the ATP-binding cassette transporter family that are well kno
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In the latent inhibition model a conditioned stimulus CS
2022-05-07
In the latent inhibition model, a conditioned stimulus (CS) is pre-exposed alone without any consequences (i.e., unconditioned stimulus [US]) in the pre-exposure phase. The CS is then associated with a US to form a CS-US association. The strength of the CS-induced response in the pre-exposure group
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ICH induced striatal lesion produced a reduction of
2022-05-07
ICH-induced striatal lesion produced a reduction of EAAT1 expression analogous to the decreased glutamate uptake at 6 h. The combined reduction of excitatory amino UNC1999 transporters and of glutamate uptake activity might explain the well-known glutamate excitotoxicity following brain ischemia (Ra
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cAMP is a key secondary messenger which transduces extracell
2022-05-07
cAMP is a key secondary messenger which transduces extracellular signals at glucagon receptors to intracellular effector molecules. cAMP-protein kinase A (PKA) pathway increases the gene expression of enzymes including phosphoenolpyruvate carboxykinase (PEPCK) and glucose 6-phosphatase (G6Pase) whic
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