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We speculated modulation of redox balance in
2021-09-08

We speculated modulation of redox balance in brain, by activation of GIP receptor pathway. QA is known to mediate production of ROS, lipid peroxidation by its interactions with Fe2+ and formation of QA-Fe2+ complex (Braidy et al., 2010, Rios and Santamaria, 1991, Stipek et al., 1997). QA induces NOS
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Although the ramifications of non additive SAR are context d
2021-09-08

Although the ramifications of non-additive SAR are context-dependent, the knowledge that perturbations in one region of a chemical series are not synergistic with perturbations in another region of the same chemical series is clearly pertinent to any medicinal chemistry effort. In our experience, no
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In the present studies we
2021-09-08

In the present studies, we found that genistein did not antagonize fMLF-induced Ca2+ mobilization in FPR1-HL60 ITE and human neutrophils. Thus, the previously reported inhibitory effect of genistein on fMLF-stimulated degranulation, aggregation, and reactive oxygen species (ROS) production in human
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Sugar gliders and hedgehogs are insectivores and actively
2021-09-07

Sugar gliders and hedgehogs are insectivores and actively seek arthropods in nightly forays. It is suspected that Triatoma were not feeding on the sugar gliders and hedgehogs, but rather were being eaten. The oral route of infection is often nonfatal and induces a carrier state in South American did
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The PAS and CC domains of sGC have
2021-09-07

The PAS and CC domains of sGC have been studied less by comparison, though their function in sGC signal transduction is likely important. PAS domains are versatile as they can play varied roles in different proteins, such as quaternary structure organization, cofactor binding, and signal transductio
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serine threonine protein kinase We show that pharmacological
2021-09-07

We show that pharmacological inactivation of GSTP1 over a sustained period does not show any observable toxicity, and not only prevents breast tumor growth but even slows established breast tumor growth in mice. A highly potent GSTP1 inhibitor, ezatiostat (developed by Telik Inc.) has passed phase I
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The crystal structures of plant class ADH GSNOR
2021-09-07

The crystal structures of plant class ADH3/GSNOR from Arabidopsis thaliana (AtGSNOR) and Solanum lycopersicum cv. Amateur (SlGSNOR) with bound substrates and cofactors revealed important differences between plant and human enzyme, namely within the substrate-binding pocket. GSNOR are unusually homod
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The Berlin patient is a unique case and dependent
2021-09-07

The Berlin patient is a unique case and dependent on the histocompatibility-matched CCR5Δ32/Δ32 homozygous donors. These donors occur at a little higher rate in the European Caucasian population, but they are very rare in Asians and Africans.15, 16, 17 The recently developed genome-editing technolog
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Although the overall structures of mGlu and mGlu VFTs are
2021-09-07

Although the overall structures of mGlu2 and mGlu3 VFTs are highly similar, two major differences can be observed: (i) the number of functional Cl− binding sites, one in mGlu2 versus two in mGlu3 receptors and (ii) the loop 7 in lobe 2 is longer in mGlu3 than in the mGlu2 receptor. These two particu
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Because AM had limited efficacy
2021-09-07

Because (AM-3189) had limited efficacy on rodent GPR40, we used two rodent models expressing human GPR40 to demonstrate efficacy of (AM-3189). First, we used human islet transplanted nude mice. In this model, endogenous pancreatic β-cells were ablated using streptozotocin, and mice were rescued to e
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br Acknowledgments We would like to acknowledge Jenna Hall
2021-09-07

Acknowledgments We would like to acknowledge Jenna Hall, Marita Rivir, Kathleen Smith, Joyce Sorrell, and Emily Yates for assistance with in vivo pharmacology studies. We would like to acknowledge Joe Chabenne and Steph Mowery for assistance with in vitro cell-based assays, and Patrick J. Knerr f
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br Acknowledgments br Introduction When human red
2021-09-06

Acknowledgments Introduction When human red blood cell (hRBC) membranes are depolarized, either as intact Chk1 and MK2 Inhibitors set suspended in depolarizing (low Cl−) Ringers or under voltage clamp conditions using excised inside-out patches, they respond by opening a nonselective voltage-
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OCA has recently been approved for the treatment of
2021-09-06

OCA has recently been approved for the treatment of patients with PBC and is under study for diseases such as NASH, PSC and biliary atresia [30], [49]. Up to now, the beneficial effects of OCA have been related to its anti-cholestatic, anti-inflammatory and anti-fibrotic properties. We have here rep
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Besides its carcinogenic role WTAP
2021-09-06

Besides its carcinogenic role, WTAP was also discovered to participate in several physical processes in normal cells. As previously reported, WTAP was involved in cell proliferation, survival, apoptosis [7,29,30], eye development [8] and embryonic development [7] owing to its complex function in tra
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br Anandamide signaling and cardiovascular function The card
2021-09-06

Anandamide signaling and cardiovascular function The cardiovascular effects of cannabinoid compounds have been known for a long time. Studies in humans indicate that chronic use of marijuana causes long lasting decrease in blood pressure and heart rate, whereas the acute use increases heart rate
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