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IC values were obtained for an expanded version of the
2023-02-10
IC50 values were obtained for an expanded version of the fragment library using the previously described mobility shift assay. Subsequently, Ki values were estimated from IC50 values to allow better comparison of the activity against targets which were measured at different substrate concentrations
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The allosteric site of class C receptors
2023-02-10
The allosteric site of class C receptors is generally located on the extracellular side of the TM domain (Brauner-Osborne et al., 2007, Christopher et al., 2015, Dore et al., 2014, Gregory et al., 2011, Harpsoe et al., 2017, Kniazeff et al., 2011, Pin and Prezeau, 2007, Urwyler, 2011, Wu et al., 201
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The elevated levels of intracellular antioxidant such as
2023-02-10
The elevated levels of intracellular antioxidant such as reduced glutathione (GSH) are normally oberserved is various tumor beta-lactamase which confers the chemoresistant to chemotherapy [59]. Therefore, the induction of oxidative stress via elevation of intracellular ROS and dimunition of intrace
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br Introduction O Dowd et al identified
2023-02-10
Introduction O’Dowd et al. identified a gene very similar to angiotensin type-1 receptor in 1993 (O’Dowd et al., 1993). The specific selective ligand of this receptor called APJ receptor was determined by Tatemoto et al. in 1998 as apelin (Tatemoto et al., 1998). The high expression of apelin and
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Ketoconazole Evidence shows that glial activation increases
2023-02-10
Evidence shows that glial activation increases the expression of cytokines and chemokines in Parkinson's disease, which precede the degeneration of the substance nigra (Halliday and Stevens, 2011, Tansey and Goldberg, 2010). The use of non-steroidal anti-inflammatory drugs (except aspirin) can preve
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br Adiponectin in prostate cancer PC was
2023-02-08
Adiponectin in prostate cancer PC was documented as the leading type of malignancy in males in the US with respect to both the estimated number of cases (22,800) and deaths (27,540) (Siegel et al., 2016). Studies have reported an association between low APN levels and the progression of PC (Micha
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Given that there are substitutions between Anc and
2023-02-08
Given that there are 132 substitutions between βAnc and the human β subunit, we wondered whether βAnc could replace the human β subunit in hybrid AChRs formed from ancestral and human subunits. We first confirmed that the β subunit is required for expression of human AChRs in HEK293 prostanoid recep
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The combination of Aurora kinase inhibitors with standard
2023-02-08
The combination of Aurora kinase inhibitors with standard chemotherapeutics or radiotherapeutics are currently in progress, such as AZD1152 plus radiotherapy in various solid cancer models. In addition, Azzariti et al. found that AZD1152-HQPA enhanced oxaliplatin and gemcitabine effectiveness in the
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and LO are members of the lipoxygenase family that
2023-02-08
5- and 12/15-LO are members of the lipoxygenase family that convert arachidonic DMPO australia 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 t
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Estrogen exerts its genomic action via estrogen nuclear rece
2023-02-08
Estrogen exerts its genomic action via WAY 208466 dihydrochloride nuclear receptor: ERα and ERβ. The distribution of ERα and/or ERβ positive neurons in CNS of different species has been mapped extensively by various methods [41], [42], [43], [44], [45], [46], [47], [48], [49], [50], although there a
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The first objective of the
2023-02-08
The first objective of the present study was to investigate the impact of ageing on arginase activity in tissues which exhibit age-related impairments in their function. The second objective was to determine whether l-arginine supplementation modulated the effect of ageing on arginase activity. The
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This study evaluated the anti
2023-02-08
This study evaluated the anti-tumor influences of LA against HepG2 oxidative phosphorylation in vivro, and investigated the molecular mechanisms of inducing apoptosis. Overall, our studies suggested that LA is a promising anti-cancer drug and a possible novel therapeutic agent directed toward the m
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Our previous studies and others have identified that the inh
2023-02-08
Our previous studies and others have identified that the inhalational anesthetic isoflurane induces neuronal apoptosis via [Ca2+]i overload through the opening of synaptic voltage-dependent calcium channels (VDCCs) and the excessive Ca2+ release from the endoplasmic reticulum (Zhao et al., 2011; Zha
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br Conclusions In summary KLA isolated
2023-02-08
Conclusions In summary, KLA isolated from K. senegalensis exerted the anti-inflammatory activity via inhibiting the activation of NF-κB, AP-1, AKT and upregulating p38 MAPK/Nrf2/HO-1 signaling in LPS-stimulated RAW 264.7 and BV-2 tcY-NH2 (Fig. 9). These properties provide a potential mechanism t
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Thus we presumed that ALDH
2023-02-08
Thus, we presumed that ALDH1A3 might play an important role in TMZ-chemoresistance in glioblastoma patients. As we expected, the glioblastoma cell lines and primary glioma encorafenib were more sensitive to TMZ treatment when ALDH1A3 was inhibited or depleted. Consistently, it has been shown that do
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