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We wanted to investigate the influence of substituents
2024-07-19

We wanted to investigate the influence of substituents on the pyrazole ring on the activity, but only a few substituted pyrazole-3-carboxylic acids/esters were commercially available in useful amounts at a reasonable price, for example, 4- and 5-nitro-pyrazole-3-carboxylic acid. The preparation of 4
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br Experimental procedures br Results br Discussion Our biop
2024-07-18

Experimental procedures Results Discussion Our biophysical and cellular analyses of mutant Aβ1–42 peptides support a role of the N-terminus of Aβ in peptide aggregation and toxicity. We demonstrate that double mutations constructed to humanize the rodent Aβ1–42 sequence result in a signific
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We also measured macrophage infiltration and CLS presence
2024-07-18

We also measured macrophage infiltration and CLS presence in peri-gonadal AT from db/db mice and controls. CLS are morphological features within AT that are accurate indicators of adipocyte death and macrophage infiltration [56]. An earlier study showed that CLS macrophages account for >90% of the t
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dynorphin A previous study showed that miR
2024-07-18

A previous study showed that miR-200c is involved in glucose-mediated pathological processes (Zhang, Guan, & Jin, 2017). Glucose metabolism is critical for the growth and proliferation of both normal dynorphin and cancer cells, and reprogramming glucose metabolism now has been considered as a targe
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br Materials and methods br Results br Discussion The
2024-07-17

Materials and methods Results Discussion The brain is endowed with the 5-LOX enzymatic system (Lammers et al., 1996, Lindgren et al., 1984), but its physiological and pathological roles are still not clear. Inflammation is a characteristic of many neurodegenerative diseases such as Alzheime
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br Conclusion To conclude it would be
2024-07-17

Conclusion To conclude, it would be fair to say that the research efforts on FLAP inhibitors for intervening with LT biosynthesis have reached to a considerably advanced state during the last decade as a result of growing interest from both pharmaceutical industry and academia [4], [37], [38]. Du
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Song et al reported series of triazolylsalicylamide derivati
2024-07-17

Song et al. reported series of 1,2,3-triazolylsalicylamide derivatives and screened over kinase panel and found compound 31 as most potent which inhibited Aurora-A, specifically with IC50 of 0.37 μM. Compound 31 was about 10-fold more active for Aurora-A than for Aurora-B (IC50 = 3.58 μM reported se
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GABAB receptor is associated with brain and behavioral disea
2024-07-17

GABAB receptor is associated with Aclacinomycin A and behavioral diseases, including epilepsy, spasticity, anxiety and neuropathic pain (Bettler et al., 2004, Bowery et al., 2002, Froestl, 2010). Baclofen, a clinical drug and selective GABAB receptor agonist, is used to treat muscle spasticity in pa
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hiv protease inhibitor Molecular simulation has proven usefu
2024-07-17

Molecular simulation has proven useful in describing the dynamics and energetics of NMDA receptor LBD cleft closure and the potentiating role of glycans (Yao et al., 2013, Dai and Zhou, 2013, Dai and Zhou, 2015, Dai and Zhou, 2016, Dutta et al., 2015, Omotuyi and Ueda, 2015, Sinitskiy and Pande, 201
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Interestingly metabolic dysfunction is also observed in amyo
2024-07-17

Interestingly, metabolic dysfunction is also observed in amyotrophic lateral sclerosis (ALS). Patients and mouse models of familial ALS exhibit higher levels of resting Bialaphos sodium salt expenditure and lower fat-free mass, indicating a hypermetabolic phenotype. Lim et al. (2012) found that red
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Although several ARIs have reached various phases of clinica
2024-07-17

Although several ARIs have reached various phases of clinical experimentation however most of them have been withdrawn either due to an insufficient bioavailability, their poor efficacy or adverse side effects. Currently Epalrestat is in clinical use for the treatment of diabetic neuropathy. The sid
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Considering our previous results with cfDNA in EGFR
2024-07-17

Considering our previous results with cfDNA in EGFR TKI-resistant NSCLC patients and growing evidence about different mutations in the ALK kinase domain as responsible for acquired resistance to ALK TKIs, we planned this study. Even if a next-generation sequencing approach after PD during crizotini
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br AhR Modulators It is now well recognized that ligand
2024-07-16

AhR Modulators It is now well recognized that ligand-activated AhR induces an immune tolerance response by acting directly on the antigen-presenting DCs and indirectly by increasing the population of immunosuppressive Tregs 24, 95, 96. In addition to inhibiting the formation or depleting the AhR
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There are two ways to transport FFAs into
2024-07-16

There are two ways to transport FFAs into cells. First by passive diffusion. Second as the putative long-chain fatty 9-AC transporters are proposed, CD36 the plasma membrane-associated fatty acid-binding protein (FABPpm) and fatty acid transport proteins (FATP) [11], where CD36 is responsible for u
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br Methods br Results br Discussion Adiponectin
2024-07-16

Methods Results Discussion Adiponectin is naturally expressed and secreted exclusively from adipocytes, and adiponectin levels and its isoforms in circulation have recently been reported to highly associate with human coronary artery disease (CAD) [46], [47], [48], [49], these studies clear
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