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During the activation of the coagulation cascade
2021-11-25

During the activation of the coagulation cascade, factor Xa (FXa) forms a complex with activated factor V and calcium sphingosine on the surface of platelet membrane (so called prothrombinase complex) and converts prothrombin to thrombin [5], [6]. Selective FXa inhibitors do not directly inhibit pl
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Recent findings of us suggest that compounds
2021-11-25

Recent findings of us suggest that compounds that inhibit both FAAH and TRPV1 may be more efficacious in pain relief than those targeting only one such protein. As continuation of our efforts to identify new molecules able to target simultaneously both FAAH and TRPV1 receptors, we hypothesized that
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In this current study we not only demonstrated
2021-11-25

In this current study, we not only demonstrated the growth-inhibitory effects of the 2nd generation analog SL-1-39 on the HER2+ breast cancer cells, MDA-MB-453 and SKBR3 (Table 1), but we also demonstrated that the decrease in cell number was associated with an interruption of Betamethasone Dipropio
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Biological evaluations of the compounds
2021-11-25

Biological evaluations of the compounds were done both using HCV protease and replicon assays. Results are shown in . The protease inhibitory IC’s were determined using a FRET assay with HCV NS3/4A 1a protease domain. The replicon EC’s were determined using a replicon luciferase cell-based assay. Th
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It is important to note that upon RIG
2021-11-25

It is important to note that upon RIG-I activation, IRF-3, p38, and ERK were activated by 3p-siHBx, leading to upregulated IFN response (Fig. 6). This suggests that 3p-siHBx has specific effects on HBV replication. In addition, 3p-siHBx induced type III IFN response (Fig. 6D), which could also inhib
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br Intracellular trafficking with concurrent signaling
2021-11-25

Intracellular trafficking with concurrent signaling of NPRA Our recent studies have shown internalization and concurrent signaling of NPRA in subcellular compartments; this had not been previously demonstrated [26,42]. Preparation of the enhanced GFP (eGFP)-tagged NPRA (eGFP-NPRA) construct has g
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In our previous studies examining erectile responses in sGC
2021-11-25

In our previous studies examining erectile responses in sGCα1−/− mice, we found that the sGCα1 subunit was required to obtain proper erectile responses to substances generally known to exert their actions by sGC.17, 18 Based on our previous observation of residual relaxing responsiveness to exogeno
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Based on work from our labs with mGlu
2021-11-24

Based on work from our labs with mGlu NAMs, and the ability of [3.3.0] systems, such as the octahydropyrrolo[3,4-]pyrrole, to effectively mimic piperazines, we focused our attention on the potential bioisoteric replacement of the [3.1.0] system of and , as well as the piperidine of , with a [3.3.0]
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It is becoming increasingly apparent
2021-11-24

It is becoming increasingly apparent that membrane lipids play a critical role in modulating and regulating protein function. For example, embedding the homologous SLC1 transporter GltPh in a POPE bilayer allowed a third Na+ binding site to be identified from MD simulations [42], and the binding ene
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The experiments indicate that a major
2021-11-24

The experiments indicate that a major component of the vasodilatation is due to antagonism of α 1-adrenoceptors. Evidence for α1-adrenoceptor antagonism is that vasodilatation was observed in Mouse Angiopoietin-2 / ANG2 / ANGPT2 Protein (His Tag) preconstricted with α1-adrenoceptor agonists, phenyl
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The first GSM was identified from the discovery of non
2021-11-24

The first GSM was identified from the discovery of non-steroidal anti-inflammatory drugs (NSAIDs). An amyloid reducing GSM that also suppresses inflammation is desirable. Inflammatory response is an invariable characteristic of AD pathogenesis, in part triggered by Aβ. During AD onset and progressio
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Evans Blue tetrasodium salt Interestingly GAL has also been
2021-11-24

Interestingly, GAL has also been shown to be co-expressed and/or secreted in luteinizing hormone releasing hormone (LHRH) (Merchenthaler et al., 1991, Marks et al., 1994) and kisspeptin (KISS) neurons (Porteous et al., 2011). Furthermore, GAL was shown to stimulate luteinizing hormone (LH) secretion
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br Pathological consequences of disruption in the
2021-11-24

Pathological consequences of disruption in the GABA/T current equilibrium This issue has been particularly investigated in the context of absence seizures. These seizures are non-convulsive epileptic attacks present in many generalized genetic epilepsies that are characterized by a sudden and rel
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br RESULTS br DISCUSSION In
2021-11-24

RESULTS DISCUSSION In this study, we found impaired apoptosis in the peripheral blood of RA patients when compared with peripheral blood from normal controls. Our previous studies have shown that the number of CD4 + T phosphodiesterase inhibitor increased while regulatory T (Treg) cells dimin
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Overall while cART has significantly prolonged
2021-11-24

Overall, while cART has significantly prolonged life and ameliorated HIV-associated disease, HIV infection of the CNS still induces a number of cognitive, behavioral and motor symptoms, along with substantial neuropathology. Data show that the inflammatory processes driving neurological disease pers
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