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In the past few years several experimental findings
2024-12-18

In the past few years, several experimental findings have demonstrated a pivotal involvement of adenosine also in driving the phenotypic switch of macrophages. In particular, the stimulation of A2A and A2B receptors seems to play a critical role in switching macrophages from M1 to M2 phenotype [37,6
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The gene SRD A encodes the reductase enzyme
2024-12-18

The gene SRD5A2 encodes the 5-α-reductase enzyme, which converts testosterone into dihydrotestosterone. Although dihydrotestosterone levels are considerably lower than testosterone, dihydrotestosterone has a five-fold stronger binding capacity to the androgen receptor and, thereby, a considerably mo
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Many metalloenzyme inhibitors consist of two chemical compon
2024-12-18

Many metalloenzyme inhibitors consist of two chemical components: the MBG, the portion of the inhibitor designed to bind to the metal, and the scaffold, the portion of the inhibitor recognized by the amino Fludara residues that form the substrate-binding site of the metalloenzyme. The MGB is often a
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br Introduction The principal pathways of adrenal
2024-12-18

Introduction The principal pathways of adrenal and gonadal steroidogenesis have been known for over 50 years (reviewed by Miller and Auchus, 2011). Cholesterol is first converted to pregnenolone via three reactions, 20-hydroxylation, 22-hydroxylation and scission of the 20,22 carbon–carbon bond,
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S63845 australia br Aurora A Aurora B and Aurora C small mol
2024-12-18

Aurora-A, Aurora-B and Aurora-C small molecule inhibitors Nicholas et al. described phenotypic cellular screening of new highly potent and selective class of Aurora kinase inhibitors. Fragment based approach was utilized; core structure of 57 (Fig. 5) was optimized and selective inhibitor 58 (Fig
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br Synthetic lethal approaches In
2024-12-18

Synthetic lethal approaches In addition to the potential utility of ATM and ATR as chemo- or radiosensitisers, recent studies suggest that such compounds may have single agent activity in certain subsets of patients through induction of synthetic lethality. Two genes are considered synthetically
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The accumulation of oxidized low density lipoprotein oxLDL i
2024-12-18

The accumulation of oxidized low-density lipoprotein (oxLDL) is one of the many causes of the initiation and progression of atherosclerosis (Virmani et al., 2002; Pirillo et al., 2013; Sun et al., 2016; Huang et al., 2016; Tabas, 2010). oxLDL-induced apoptosis of macrophages contributes to the forma
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br Concluding Remarks and Future Perspectives Fluorescent
2024-12-17

Concluding Remarks and Future Perspectives Fluorescent Pancuronium dibromide have helped researchers to elucidate antibiotic MOA and off-target interactions, to screen for new antibiotics, to detect antibiotics in the environment, to track antibiotic uptake throughout cells and organisms, and to
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cdc42 pathway br Antiangiogenic therapy in non small cell lu
2024-12-17

Antiangiogenic therapy in non-small cell lung cancer (NSCLC) Antiangiogenic targeted therapy is an area of active research in which numerous agents have been studied and have been shown to be effective for many tumor types including NSCLC. Angiogenesis is frequently upregulated in malignant solid
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We designed SSOs that block APP
2024-12-17

We designed SSOs that block APP exon 17 splicing and induce the production of an alternatively spliced APP mRNA lacking exon 17 (APPΔex17). APPΔex17 mRNA encodes an APP protein isoform that lacks 49 polycomb repressive complex including the γ-secretase cleavage sites that give rise to the toxic, AD
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Pathogen infected macrophages release exosomes
2024-12-17

Pathogen-infected pei max release exosomes associating with pathogen-associated molecular patterns (PAMPs) such as LPS and lipoprotein derived from microorganisms [29,30]. Exosomes released by bacterially infected, but not uninfected, macrophages stimulate macrophages to release inflammatory mediat
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This suggestion was confirmed by immunohistochemical studies
2024-12-17

This suggestion was confirmed by immunohistochemical studies in which the immunoreactivity of the enzyme was actually higher at the earlier rather than at the advanced stages of the disease. Importantly, a later study showed that the biochemical signature of 12/15LO enzymatic activation (i.e., 12-HE
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Recent genome wide association studies have
2024-12-17

Recent genome-wide association studies have indicated SORL1 as a risk factor for AD (Meng et al., 2007, Rogaeva et al., 2007, Wen et al., 2013). SORL1, is expressed in neurons (Yin et al., 2015) and also regulates APP traffic from the cell membrane to the Golgi apparatus. A reduction in its expressi
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br Author contributions br Funding This work
2024-12-17

Author contributions Funding This work was supported by the Czech Science Foundation, project no. 14-16220S. Additional support was provided by NIH R01CA117907 grant awarded to J.M.E. Conflict of interest Introduction The dioxin-like family includes polyhalogenated aromatic hydrocarbons
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MPC 6827 hydrochloride synthesis Constitutive tyrosine kinas
2024-12-17

Constitutive tyrosine kinase activity of BCR/ABL fusion genes causes uncontrolled cell growth and is also thought to be responsible for a variety of changes in normal cellular functions like differentiation, adhesion, migration and apoptotic response in CML. Therefore it is important to know the exp
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