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Most human diseases e g cancer diabetes and neurodegenerativ
2024-08-05

Most human diseases (e.g., cancer, diabetes, and neurodegenerative diseases) are complex and multifactorial. Several investigations in the literature focused on new multi-target drug development, which implies active pharmacophores incorporation in one scaffold (Meunier, 2008, Lazar et al., 2004, Te
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br Emerging Vascular Mechanisms of
2024-08-05

Emerging Vascular Mechanisms of AA Therapy Resistance Experimental and clinical evidence indicates that physiological angiogenesis generates blood vessels capable of restoring perfusion [1], whereas tumoral angiogenesis gives rise to vessels that are structurally and functionally abnormal, therei
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Our previous study showed that TRIM could target
2024-08-05

Our previous study showed that TRIM31 could target TSC1-TSC2 complex and contributed to the clinical cancer progression [6]. In this study, we showed that TRIM31 could directly target p53 for ubiquitous degradation and further mediated anoikis-resistance of HCC cells. To further clarify the role of
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In most industrial areas which
2024-08-03

In most industrial areas which are in need of treatment, there are mixtures of different contaminants at different concentrations in soil, underground water or wastewater. These hazardous wastes include a variety of salts, organic matter, heavy metals, trace elements and radioactive compounds [5].Si
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br LOX in pancreatic cancer
2024-08-03

5-LOX in pancreatic cancer 5-LOX is a key player in pancreatic cancer (PC) progression. The upregulation of 5-LOX mRNA has been observed in pancreatic adenocarcinoma (PDAC) and also in neoplastic pancreatic tissues (Kennedy et al., 2003). Higher levels of 5-LOX transcripts (messengers) are presen
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br Methods br Results br Discussion br Acknowledgements
2024-08-03

Methods Results Discussion Acknowledgements This work was supported by the National Institutes of Health [Grant R21 NS081429], a Pilot Grant from the Vanderbilt Conte Center supported by the National Institutes of Health [Grant P50 M096972], and by the Department of Anesthesiology at V
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apexbio dilution br Conflicts of interest br Acknowledgments
2024-08-03

Conflicts of interest Acknowledgments The authors acknowledge National Institute for Medical Research Development (NIMAD) project no. 940943 and National Research Institute for Science Policy (NRISP) no. 1456 for financial support of this work. AM appreciates National Institute for Genetic Eng
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Ryoichi et al modified potent clinical candidate VX
2024-08-03

Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos
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To evaluate the ability of both sets of
2024-08-03

To evaluate the ability of both sets of compounds to inhibit the activity of 15-LOX an initial screen was performed, whose results are shown in . The comparison of inhibition values would seem to indicate that, in the HYD series, an electron donor group at the position increases and an electron at
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br Asthma The chronic airway inflammatory disease asthma is
2024-08-03

Asthma The chronic airway inflammatory disease Dyngo-4a is associated with enhanced levels of exhaled NO generated by iNOS in the airway epithelium [12]. In asthmatic patients local and systemic changes in iNOS, peroxynitrite, arginase, ADMA and arginine levels have been observed and are associa
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br Development of lorlatinib from crizotinib to
2024-08-02

Development of lorlatinib from crizotinib (1) to a clinical candidate (6) Xalkori (1, PF-02341066, crizotinib), was the first-in-class ALK inhibitor approved by the Unites States Food and Drug Administration (FDA) in 2011 as a first-line treatment for ALK+- NSCLC patients. This section describes
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Aldose reductase ALR EC the
2024-08-02

Aldose reductase (ALR2, EC1.1.1.21), the first enzyme in the polyol pathway, is a monomeric oxidoreductase that catalyses the NADPH-dependent reduction of a wide variety of carbonyl compounds, especially glucose. In this metabolism pathway, glucose is firstly reduced to sorbitol catalyzed by ALR2 wi
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ML-099 We found evidence of the interaction between AR
2024-08-02

We found evidence of the interaction between AR and hemiacetals by evaluating the effect of glucose on l-idose reduction. l-idose was recently proposed as the best AR substrate able to mimic glucose [38]. This aldose is structurally very closely related to d-glucose, from which it differs only in th
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There are human genes in the SLC A family and
2024-08-02

There are 12 human genes in the SLC5A family, and 6 of these are expressed in human heart (Table 2). Little is known about SGLT proteins in the heart. Zhou et al. [56] reported the presence of SGLT1 mRNA in the human heart. Researchers have found that levels of SGLT1 mRNA in heart are approximately
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br Adenosine receptors and innate immunity Monocytes and mac
2024-08-02

Adenosine receptors and innate immunity Monocytes and macrophages. All four adenosine receptor subtypes are expressed on monocytes and macrophages, and their levels and function undergo significant changes during the maturation of macrophages from monocytes. Indeed, quiescent monocytes are charac
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