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Because of the critical roles
2023-10-01
Because of the critical roles played by AMPK in energy sensing and cancer cell survival, a huge number of drugs have been proposed to exert their pharmacological effects by means of AMPK activation (Kim and He, 2013). For example, metformin has been shown to activate AMPK in muscle (Sajan et al., 20
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Most intriguingly however there was no change in
2023-10-01
Most intriguingly, however, there was no change in basal glutamatergic neurotransmission despite a loss of about half of the neuronal AMPAR population. Highest levels of ammonia did neither affect the amplitude nor the frequency of AMPAR mediated mEPSCs. As revealed by our recordings from somatic ou
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Pyridostatin The G R mutation is
2023-10-01
The G1202R mutation is located at the solvent front of the ALK kinase domain adjacent to the inhibitor's binding pocket. Although barely reported in the setting of crizotinib resistance, it has emerged as the most refractory mutation to both the first- and second-generation ALK inhibitors. The large
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Aldose reductase AR is an
2023-10-01
Aldose reductase (AR), is an NADPH-dependent aldo-keto reductase very well studied as a catalyst of glucose conversion to sorbitol in the polyol pathway [11], [12]. In the diabetic lens characterized by chronically high levels of glucose, AR is responsible for production of high levels of sorbitol a
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In contrast to the beneficial treatment of skin inflammation
2023-10-01
In contrast to the beneficial treatment of skin-inflammation with PAH containing coal tar, epidemiology showed that environmental pollution, containing AHR-activating PAH, lead to more eczema [80]. Of note, other epidemiological data suggested that Th17 cell polarization may be enhanced air pollutio
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Mechanisms implicated in antinociception by A R
2023-10-01
Mechanisms implicated in antinociception by A3R agonists in neuropathic pain are summarized in Box 3. Cellular transduction mechanisms for A3Rs include inhibition of cyclic AMP, PKA via Gαi, interactions with PLC/IP3/DAG and signaling via Gαi and Gαq, and interactions with PI3K/MEK/ERK via βγ subuni
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br Disclaimer br Conflicts of interest br
2023-10-01
Disclaimer Conflicts of interest Role of the Sponsor Acknowledgements Funding/support: This project was supported by a grant from the Department of Surgery (R5129), Western University and by the Institute for Clinical Evaluative Sciences (ICES) Western site. ICES is funded by an annual g
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Later the same group designed and prepared several steroidal
2023-10-01
Later, the same group designed and prepared several Δ16-steroidal C17 benzoazoles and pyrazines and evaluated their CYP17 and 5α-reductase inhibitory activities, binding to and transactivation of the AR, as well as their antiproliferative effects against two human PC cell lines (LNCaP and LAPC4) [18
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br Ataxia telangiectasia and Rad related as a therapeutic
2023-09-28
Ataxia–telangiectasia and Rad3 related as a therapeutic target Several concerns revolving around functional inhibition of ATR have hindered the exploitation of ATR as therapeutic target in cancer therapy and delayed the development of specific ATR kinase inhibitors. It was anticipated that pharma
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The uterine muscle also changes to meet the
2023-09-28
The uterine muscle also changes to meet the demands of pregnancy. Over the course of pregnancy, the myometrium undergoes structural remodeling to accommodate a growing fetus, followed by a functional switch from quiescent to contractile characteristics for parturition. Studies on the mouse model ind
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br Acknowledgements This work was supported in part
2023-09-28
Acknowledgements This work was supported, in part, by NIH grant R01-GM071760. Introduction The MADS box genes encode a eukaryotic family of transcriptional regulators involved in diverse and important biological functions. This class of proteins has been identified in yeasts, plants, insects,
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streptozocin br Conclusion br Competing interests br Funding
2023-09-28
Conclusion Competing interests Funding The Bolger Prostate Cancer Research Fund (no grant number), the National Institute of General Medical Sciences of the National Institutes of Health (1-R01-GM58553, G. B. Bolger, principal investigator), and the National Cancer Institute of the NIH to t
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Interestingly we noticed that LPS exposure was associated wi
2023-09-28
Interestingly, we noticed that LPS exposure was associated with decreased phosphorylation of AMPK and increased phosphorylation of p70S6K1, suggesting that AMPK inactivation and the subsequent mTOR activation might be involved in the development of LPS-induced inflammation. On the other side, treatm
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In the MT SGL two regularization parameters need
2023-09-28
In the MT-SGL, two regularization parameters need to be specified: λ1 and λ2. Using recent results on norm regularization (Banerjee et al., 2014), it is possible to express both parameters via a single parameter as follows: and (Meier et al., 2008, Banerjee et al., 2014), where and are computed as:
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Further evidence for action mechanism was provided by assays
2023-09-28
Further evidence for action mechanism was provided by assays using [3H]nisoxetine, a selective NET inhibitor used as standard radioligand for competitive binding experiments. The results showed dose-dependent blocking of [3H]nisoxetine binding by both xylazine and dexmedetomidine. Nisoxetine binds t
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