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Recent findings of us suggest that compounds that
2021-10-21

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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Thus from this preliminary study
2021-10-21

Thus from this preliminary study, a working model of HIV-1 integrase was developed from which a selective inhibitor of the strand-transfer reaction displaying whole-cell activity and negligible cytotoxicity was produced. Compound 9 provides a promising scaffold for further elaboration, and current i
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br Introduction Local anesthetics LAs are
2021-10-21

Introduction Local anesthetics (LAs) are a set of common medicines used for pain management in clinical settings. Up to now, LAs have been extensively used for peripheral nerve blocks, interventional spinal procedures, and epidural anesthesia [1]. In addition to their anesthetic and analgesic eff
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Also considered very rare is progressive
2021-10-21

Also considered very rare is progressive encephalomyelitis with rigidity and myoclonus (PERM); sometimes called Stiff Person Syndrome Plus (SPS Plus) and with antibodies to glutamic IL-10, human recombinant protein decarboxylase (GAD). However, PERM is now increasingly found with glycine receptor an
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Because sleep and metabolism are intimately linked the autho
2021-10-21

Because sleep and metabolism are intimately linked, the authors next move to study whether Eaat2 also controls metabolic rate. First, we must ask how sleep and metabolism are connected at a functional level. The line allocation hypothesis of sleep posits that organisms temporally partition specific
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After ischemia expression of transcription factors
2021-10-21

After ischemia, expression of transcription factors, including products of immediate early genes, stress proteins and neurotrophic factors are also altered in CA1 neurons78, 79. These proteins are potential candidates for downregulating of GluR2 expression by reducing mRNA transcription or stability
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In a previous study M ykkynen et al we
2021-10-21

In a previous study (Möykkynen et al., 2003), we reported that ethanol lengthens the time needed for the AMPA receptors to recovery from desensitization in isolated hippocampal neurons. Here, we did not observe any effect of ethanol on recovery from desensitization in recombinant homomeric GluR-D re
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At the second step blind
2021-10-21

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 atomic model of Ce INX provides
2021-10-21

The atomic model of Ce-INX6 provides an additional interpretation to the Ce-INX6ΔN mutant structure at low-resolution [41]. Given that the N-terminal residues from 2 to 19 are deleted in the Ce-INX6ΔN mutant, the N-terminal funnel found in the pore of the wild-type Ce-INX6 should be lost in the Ce-I
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Activation of FXR or TGR has overlapping but also differing
2021-10-21

Activation of FXR or TGR5 has overlapping but also differing effects on metabolic regulation and inflammation [1]. In this report, we demonstrate that in addition to preventing the progression of obesity, NAFLD, and atherosclerosis, activation of BA receptors can also promote regression of these com
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On the other hand after injury of
2021-10-21

On the other hand, after injury of the adult heart, inflammatory monocytes are abundantly recruited to damaged myocardium and they differentiate into monocyte-derived macrophages (MDMs). They have strong proinflammatory phenotype and very limited capacity to promote angiogenesis and cardiomyocyte pr
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In the course of studies leading to the discovery
2021-10-21

In the course of studies leading to the discovery of , modifications at the P3-P4 interface of these tripeptide-based inhibitors were examined with the goal of improving potency while maintaining a PK profile similar to . In this report, we summarize those studies which led to the identification of
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Our data indicate that curcumin reduced MDA and LOOH formati
2021-10-21

Our data indicate that curcumin reduced MDA and LOOH formation in plasma and kidney induced by gentamicin treatment. The results demonstrate the protective effect of this compound against oxidative damage to these membranes. Moreover, the ability of curcumin to reduce the formation of LOOH induced b
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br Introduction Sister chromatid cohesion is established
2021-10-21

Introduction Sister-chromatid cohesion is established during DNA replication by a ring-shaped cohesin complex consisting of the core subunits Smc1, Smc3, Scc1, and SA1 or SA2, which recruit regulatory subunits Pds5 (Pds5A/B in vertebrates), Wapl, and Sororin to regulate the association of cohesin
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br All platelet agonists acting
2021-10-20

All platelet agonists, acting through specific receptors and triggering different signaling pathways, activate phospholipases (PLCß or PLCγ) and the subsequent messengers inositol 1,4,5-trisphosphate (IP3) and 1,2 diacylglycerol which activate inositol 1,4,5-trisphosphate (IP3) receptors (IP3R) or
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