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br STAR Methods br Acknowledgments This work was supported
2022-08-09

STAR★Methods Acknowledgments This work was supported by the American Diabetes Association (grant 1-12-BS-161 to J.D.P.), an NIH predoctoral T32 in Autoimmunity and Immunopathology grant (AI089443-05 to D.M.P.), the NIH (grant DK099550 to H.M.T.), the American Association for Cancer Research (S
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Molecular properties as well as metabolic stability in
2022-08-09

Molecular properties as well as metabolic stability in rat and human liver microsomes for the most active nitro (), nitrile (), methylsulfone (), and sulfonamides () analogues were measured (). All these derivatives possessed excellent membrane permeability as measured in the Pampa assay and further
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Apart from a few mutations which affect
2022-08-09

Apart from a few mutations, which affect intracellular and extracellular loops of hCRT-1, the mutations are primarily found in the hydrophobic core of the transporter; in fact, TMDs 7 and 8 appear to be a hot spot for mutations (Freissmuth et al., 2018). Several mutations are found at positions, whi
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br According to WHO estimates diabetes continues to present
2022-08-09

According to WHO 2014 estimates, diabetes continues to present an increasing health risk to the global population, affecting 422 million individuals worldwide. Type 2 diabetes (T2D), which affects the vast majority (ca. 90%) of the diabetic population, occurs when the body cannot effectively utili
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br Acknowledgements br Introduction Aminoacyl tRNA synthetas
2022-08-09

Acknowledgements Introduction Aminoacyl-tRNA synthetases catalyze the formation of an ester bond between an amino rucaparib and the 3′ end of a tRNA in a two-step reaction. First, the amino acid is activated and an enzyme-bound adenylate intermediate is formed. Then, the amino acid is transfe
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Optimization of the tetrahydroindazole series led to the
2022-08-09

Optimization of the tetrahydroindazole series led to the discovery of two moderately potent γ-secretase modulators, 2-cyclobutane and 2-hydroxy-2-methylpropane which were subsequently evaluated in a kinetic aqueous solubility assay. Unfortunately, neither analog demonstrated improved solubility ()
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Studies have indicated that formylated peptides FPRs and
2022-08-08

Studies have indicated that formylated peptides, FPRs, and in particular FPR-1 may be principal conductors in inflammatory processes in sterile-24, 26 and infection-related diseases. FPR-1 and formylated peptides, which are active components of CS, have been involved in smoking-induced lung damage,
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As for all DOACs measurement of DiXaIs
2022-08-08

As for all DOACs, measurement of DiXaIs activity requires the use of dedicated specific calibrators and controls. Each drug needs its own calibration and control material in a like to like manner. In no case can a drug concentration be extrapolated with the use of a calibrator established for anothe
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The cytotoxicity of these compounds against Hep
2022-08-05

The cytotoxicity of these compounds against Hep3B cells was assessed using the MTT assay. As shown in , compounds in series and (except ), which retained the carboxyl at C-17, showed no appreciable cytotoxic activity (IC > 100 μM), whereas compounds in series (except ,) were modestly cytotoxic, i
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br Materials and methods br Results Estimations of
2022-08-05

Materials and methods Results Estimations of OMP generated by the proposed mechanism (Fig. 1) were first performed for the range of 0.001–2 mM of cAMPS-Rp, triethylammonium salt concentration in the cytosol. It was assumed that only 5% of all VDACs in MOM form the ANT-VDAC1-HKI contact sites,
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Alzheimer s disease AD is a neurodegenerative disorder and c
2022-08-05

Alzheimer's disease (AD) is a neurodegenerative disorder and characterized by the presence of abnormal filamentous protein inclusions in nerve cells of the brain [2]. The neuropathological hallmarks of AD were first reported by Alois Alzheimer and date back to 1907 [3], [4]. These inclusions are for
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Another important question is what ligand
2022-08-05

Another important question is what ligand(s) bind to GPR84 in vivo? Previous studies have identified medium-chain FFAs of 9 to 14 carbons in length and two other organic molecules (6-n-octylaminouracil and 3,3′-diindolylmethane) as agonists of GPR84 in vitro (Wang et al., 2006, Suzuki et al., 2013).
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Beside its role in NF
2022-08-05

Beside its role in NF-κB and IL-1β activation, the NRLP3 pathway is closely involved in another essential pathophysiologic mechanism such as the cellular calcium homeostasis. Full activation of the NRLP3 inflammasome requires decreased extracellular K concentrations resulting in decreased osmotic pr
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We hypothesized that modulating redox stress by altering end
2022-08-05

We hypothesized that modulating redox stress by altering endogenous antioxidant content (overexpression of catalase) and/or via dietary intervention will improve energy metabolism, adipose tissue function, and overall glucose and lipid homeostasis. To better understand the interplay between redox re
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The mechanisms of action of MMF and DMF are not
2022-08-05

The mechanisms of action of MMF and DMF are not well understood, but a growing body of evidence has demonstrated that DMF may act on both the neurodegenerative and inflammatory response of MS patients. The majority of the data related to the mechanism of action of DMF/MMF demonstrates the associatio
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