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The dependence of blood cell production
2024-12-11

The dependence of blood cell production on a limited number of HSC and HPC (hereafter collectively referred to as HSPC) means that protection from potential toxins is essential for maintenance of the hematologic system (see Fig. 1). For example, the generation of blood cells within the intramedullar
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Ethanol can affect biological systems directly or
2024-12-10

Ethanol can affect biological systems directly, or also through the interactions between these systems, which become important in the actions promoted by alcohol consumption. Its metabolites acetaldehyde and acetate play a key role in the nicotinic receptors mediating some effects of ethanol (Israel
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An alternative to the agonist or antagonist potential
2024-12-10

An alternative to the agonist or antagonist potential in drug discovery is the positive allosteric modulator (PAM) approach, which can augment the normal processes of neurotransmission as opposed to directly replacing or antagonizing them. PAMs are thought to bind to sites that are distinct from the
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br Role of autophagy in
2024-12-10

Role of autophagy in alcoholic cardiomyopathy Concluding remarks The genetic and phenotypic heterogeneity in alcoholic cardiac injury has been recognized despite the seemingly beneficial effects of low to moderate alcohol consumption [8]. Although oxidative stress is well established in the pa
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Roles of Aurora kinases in directly activating multiple onco
2024-12-10

Roles of Aurora kinases in directly activating multiple oncogenic pathways and promoting proliferation as well as transformation have also been demonstrated. Aurora-A has been shown to up-regulate telomerase reverse transcriptase mRNA through c-myc [26]. The kinase was also implicated in activating
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In our approach using BRET and FRET there is
2024-12-10

In our approach using BRET and FRET, there is a substantial increase in BRET and FRET signals between Giα2 or Giα3-YFP and CFP- Gγ2/Rluc-Gγ2 upon apelin-13 activation, indicating that Gαi2, Gαi3 and N-terminus of Gβ1γ2 subunits become closer without subunit dissociation. In contrast, both the FRET a
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br Introduction Chronic kidney disease CKD is a worldwide pu
2024-12-09

Introduction Chronic kidney disease (CKD) is a worldwide public health problem. This problem is even worse in socioeconomically deprived countries because lower income and social deprivation are associated with higher incidence of reduced GFR, progressive kidney function loss and end stage renal
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br Introduction Breast cancer is
2024-12-09

Introduction Breast cancer is the most frequently occurring cancer in women, and despite the development of new therapies there has been little decline in the mortality rate over the past decade (Siegel et al., 2015). This is partly due to the genetic diversity of breast cancers, such that there
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BAMB-4 br HIF HIF signaling in cancer cells contributes
2024-12-09

HIF-1α HIF-1α signaling in cancer cells contributes to tumor progression by promoting angiogenesis, invasion, metastasis, and the recruitment of immunosuppressive cells via secreted modulators 36, 37. One example of a HIF-1α immunosuppressive pathway is through increased expression of inducible n
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br The AHR functions in
2024-12-09

The AHR functions in the immune system – a tsunami of exciting findings The research of recent years has convincingly established an important function of the AHR in linking chemical environmental cues to immune responses [21,22], and reviewed in [1,23]. As a side effect, a view of the AHR as “Th
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In this article we have outlined the increasing
2024-12-09

In this article, we have outlined the increasing, as yet still circumstantial evidence that the 6TM domains of bacterial ACs might operate as receptors for as yet unknown ligands. Intriguingly, several architectural arguments are also applicable to the 6TM domains of mammalian membrane-bound ACs (mA
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cytochalasin d The A b action occurs in conditions where hig
2024-12-09

The A2b action occurs in conditions where high concentrations of adenosine is generated, so its blockage does not interfere with other physiological processes mediated by adenosine and others AR [105]. Furthermore the A3 receptor was shown to have pro-apoptotic effects on tumor lines of breast, lung
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br LOX in colorectal cancer Colorectal
2024-12-09

5-LOX in colorectal cancer Colorectal cancer (CRC) like other malignancies exhibits an overexpression of 5-LOX. Ohd et al. (Ohd et al., 2003) revealed in a study that malignant colon tissues overexpress 5-LOX activity and retain elevated levels of inflammatory mediators, leukotrienes. Additionall
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Having taken a step back from affinity to
2024-12-09

Having taken a step back from affinity to gain better exposure and solubility, we started work to replace the unstable oxazolinone, and address the selectivity over the hERG channel. Keeping in mind the binding mode of the series from crystal structures, triazole was identified as another mildly aci
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The synthetic route for the aminobenzoxazole
2024-12-09

The synthetic route for the aminobenzoxazole scaffold with a solvent accessible moiety is described in . Nitration of methoxyphenol and subsequent hydrogenation of the resulting nitro Volasertib afforded compound . Aminobenzoxazole was formed by the reaction of compound with BrCN in EtOH. The sol
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