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The excellent potencies selectivities and improved PK
2023-09-19

The excellent potencies, selectivities and improved PK associated with the piperazine class triggered more extensive off-target screenings of the highlighted compounds. A screen of more than 100 enzymes, receptors, and ion channels resulted in activity at the norepinephrine transporter (NET). This m
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Derivatives of M that possess either an alkyne or an
2023-09-19

Derivatives of (+)-M100907 that possess either an alkyne or an azide have been synthesized. The most active enantiomer was obtained by resolution of a relatively early intermediate in the synthesis. The ability of these bortezomib sigma to maintain 5-HTR antagonist properties as (+)-M100907 was dem
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Recent studies showed that the increased expression
2023-09-19

Recent studies showed that the increased expression of Aurora B kinase directly proportional to the tumor invasion and metastasis [61]. The Aurora B kinase regulates the PI2K/Akt signaling pathway has a significant role in tumor invasion and metastasis that leads to phosphorylation of GSK3β on ser 9
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br Conflict of interest br Acknowledgements br Introduction
2023-09-19

Conflict of interest Acknowledgements Introduction The mitogen-activated protein kinase (MAPK) pathway is an important intracellular signaling system that regulates diverse cellular functions, such as proliferation, differentiation, and apoptosis [1]. Apoptosis signal-regulating kinase 1 (A
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Although the exact mechanisms are not fully understood
2023-09-19

Although the exact mechanisms are not fully understood, IGF-1 is tightly linked with ER and estrogen actions and a crosstalk occurs between these two systems in breast cancer. To illustrate this close relationship, studies have identified a synergy between IGF-1 and estrogen in SAR405838 expressing
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While there is structural information
2023-09-18

While there is structural information on the core of the amyloid fibril, less is known about oligomer structure. There is evidence that the C-terminal of Aβ may form beta barrels in some oligomer species (Tay et al., 2013, Do et al., 2016), or may exist as loosely aggregated strands in other oligome
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The study by Lo http www
2023-09-18

The study by Lowry et al. (2001) pointed toward functionally uncharacterized DA- and 5-HT-accumulating neurons within the DMH as a potential target for rapid nongenomic effects of CORT. Similar DA- and 5-HT-accumulating systems are distributed throughout the central and peripheral nervous systems, s
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Mass spectrometry MS analysis and selective
2023-09-18

Mass spectrometry (MS) analysis and selective enrichment methods of phosphorylated proteins are powerful tools that can help address these challenges. Recent advances in MS have made it possible to analyze signaling pathways by facilitating high-throughput identification of phosphorylation sites wit
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The subdivision of HT receptors started in
2023-09-18

The subdivision of 5-HT receptors started in the 1950s by Gaddum and colleagues, when they realised that in the guinea pig ileum, the effects of 5-HT could be blocked in part by morphine (M), and in part by dibenzyline (D). Gaddum and Picarelli proposed two receptor classes, 5-HT M and 5-HT D (1957)
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It is important to note that stable amnesia
2023-09-18

It is important to note that stable amnesia is, apparently, a general biological phenomenon and can be found in different animal species. In studies on rats, it was found that if reconsolidation of conditioned olfactory aversion memory was impaired by the antagonist of NMDA glutamate receptors, amne
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Our in vitro data show that CyaA does not play
2023-09-18

Our in vitro data show that CyaA does not play a critical role in the bacterial adherence to mammalian cells. This observation is in contrast to previous studies that reported a role for CyaA in FHA-mediated adherence of B. pertussis bacteria to the respiratory epithelial SJB3-019A [37,38]. This di
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Given the powerful and ubiquitous nature
2023-09-18

Given the powerful and ubiquitous nature of adenosine action within the CNS, basal levels of extracellular adenosine are carefully regulated and are estimated to be in the region of 30–300 nM (Fredholm et al., 2001). The two main pathways for the control of extracellular adenosine involve phosphoryl
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br Experimental section br Results
2023-09-18

Experimental section Results and discussion Conclusions We present a simple, sensitive and selective assay of ADA activity and its inhibitor using the enzyme catalyzed reaction and the different interaction intensity of dye-labeled AD aptamer, aptamer/AD complex with GO. The as-proposed met
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A correlation analysis was performed to investigate a possib
2023-09-18

A correlation analysis was performed to investigate a possible relationship between serum resistin levels and MG-ADL. We observed a significant relationship between serum resistin levels and MG-ADL scores in AChR-GMG-positive cases (r=0.285, p=0.032; Fig. 1C). There were also significant correlation
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br Methods and results ACE is a Canadian
2023-09-18

Methods and results ACE is a Canadian satellite mission [7] that measures atmospheric tcid spectra in the limb geometry using the Sun as a light source (solar occultation). The ACE orbit (74° inclination to the equator, 650 km altitude) concentrates measurements at high latitudes but also provide
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