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The current antifungal pipeline contains several categories
2023-01-16

The current antifungal pipeline contains several categories of compounds at different stages of development [1], [9], [10], [96]. In Table 1 we summarize the most promising antifungal molecules that are in preclinical and in clinical development. Several compounds in the pipeline are derivatives of
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Introduction AMP activated protein kinase AMPK is mainly kno
2023-01-14

Introduction AMP-activated protein kinase (AMPK) is mainly known as a highly conserved and ubiquitously expressed energy sensor that is highly sensitive to changes in cellular energy levels (by sensing increases in AMP:ATP and ADP:ATP ratios) and makes appropriate adjustment to balance the consumpt
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br Conclusion These studies broadly demonstrate that dopamin
2023-01-14

Conclusion These studies broadly demonstrate that dopamine and endocannabinoid signaling in the NAc can have diverse effects on AMPAR-mediated synaptic function depending on previous psychostimulant experience. Here, we examined mechanisms underlying the depotentiation of AMPAR-mediated synaptic
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Furthermore to address the concern that the observed positiv
2023-01-14

Furthermore, to address the concern that the observed positive in vitro activity results might be stymied by the propensity of such assays to display false positives due to the inherent noxiousness of the tested compounds, all analogs were evaluated against Vero cells in an MTT assay. Some of the mo
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and LO are members of the lipoxygenase family that convert
2023-01-14

5- and 12/15-LO are members of the lipoxygenase family that convert arachidonic gli1 into lipid mediators such as leukotriene B4 (LTB) and 12()-hydroxyeicosatetraenoic acid (HETE) and 15()-HETE, respectively. Evidence from several in vitro and in vivo studies has shown that activation of the 5- and
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br Disclosure br Acknowledgments br
2023-01-14

Disclosure Acknowledgments Introduction Deeper understanding of the pathobiology of non-small cell lung cancer (NSCLC) has led to the development of small BIX 02188 that target genetic mutations known to play critical roles in the progression to metastatic disease. Mutations in epidermal g
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To understand the kinase selectivity
2023-01-14

To understand the kinase selectivity profile of this series, Bleomycin Sulfate , as a representative analog from this series, was profiled against 216 purified protein kinases representing the tyrosine and serine/threonine kinase families using an in-house Caliper EZ Reader mobility shift assay. Ass
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Fludarabine Phosphate Aminoglutethimide first generation aro
2023-01-13

Aminoglutethimide, first generation aromatase inhibitor, has been tried as an antiepileptic drug in combination with other standard drugs (Aguilar et al., 1961). Letrozole is a third generation reversible non-steroidal aromatase inhibitor, approved by US-FDA, for the treatment of postmenopausal wome
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Beside activation of adenosine receptors A a
2023-01-10

Beside activation of adenosine receptors (A2a.1, A2a.2, A2b) by FSK treatment, the expression of adenosine receptors was also upregulated, when embryos were exposed to inhibitors (SU5416 and DAPT) alone and also combined with FSK. Our data imply that adenosine receptor was associated with a positive
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A c and CD are
2023-01-10

A2c and CD73 are expressed in a small population of OSNs with pear-shaped morphology. In spite of the expression of molecular markers of ciliated OSNs such as Golf, ACIII, and OMP [1, 17], these OSNs have an extremely short dendrite and are located in the superficial layer of OE. In addition to the
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Having established the structural requirements for
2023-01-10

Having established the structural requirements for potency in both the biochemical and biomarker (CRA) assays, we evaluated key compounds in the metabolic stability assay. Disappointingly, we found that all compounds had high intrinsic clearances in mouse microsomes. To ascertain whether the in vitr
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Recent studies have demonstrated significant
2023-01-10

Recent studies have demonstrated significant cross-talk between XRCC1 (a key player in DL-AP5 Sodium salt excision repair (BER) and single strand break repair) and DDR [30], [31], [32]. ATM and DNA-PKcs are known to be involved in the phosphorylation of XRCC1 to promote BER [30], [31]. We have recen
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Aromatization of the pyrrole ring after
2023-01-10

Aromatization of the pyrrole ring after anion capturing, using acceptor atoms with electron deficiency (B & Be), and substitution of strong electron withdrawing groups such as CN were three strategies used to design a new class of anion receptors. Comparison of the anion affinities of these anion re
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Apelin APJ triggers a variety
2023-01-10

Apelin/APJ triggers a variety of cellular signaling pathways (Fig. 1). Recent studies from our laboratory showed that apelin-13 induces vascular smooth muscle cell (VSMC) proliferation by the upregulation of Cyclin D1 expression, which is involved in an ERK-dependent activation of Jagged-1/Notch3 si
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In summary present evidence suggests that antimicrobial
2023-01-10

In summary, present evidence suggests that antimicrobial therapy for intra-abdominal sepsis can be shortened in patients exhibiting a clinical response to treatment. Hence, clinicians should use the resolution of clinical signs of infection as a guide to determine when during the 4–7-day window anti
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