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Because of the critical roles
2024-04-30
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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This suggestion was confirmed by immunohistochemical studies
2024-04-29
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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Some of the earliest LOX inhibitors were
2024-04-29
Some of the earliest 12-LOX inhibitors were redox inhibitors, including nordihydroguaiaretic nor-Binaltorphimine dihydrochloride receptor (NDGA), BW 755C, and baicalein 48, 49, 50. Redox inhibitors block the oxidation of the nonheme iron at the cataylytic site, preventing its conversion from the in
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The reactions and the control mechanisms
2024-04-29
The reactions and the control mechanisms described are all supported by observations. For example the reactions require that different compounds are formed in different groups of dpat cells and this has been observed [15]. Intravenous injection of glycine results in reduced utilisation of glucose b
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KT203 Heat shock protein Hsp is a molecular chaperone
2024-04-29
Heat shock protein 90 (Hsp90) is a molecular chaperone that plays a central role in regulating the maturation, activation and stability of numerous “client proteins” that drive the development and progression of many cancers. Therefore, inhibition of Hsp90 would result in degradation of the client p
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AKT has been shown to be important for G S
2024-04-29
AKT1 has been shown to be important for G1-S checkpoint transition and proliferation, whereas AKT2 regulates cell-cycle exit through its interaction with p21 (Héron-Milhavet et al., 2006). In a recent study in triple negative breast cancer, AKT3, rather than AKT1 activity was most important for cell
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During the course of our ACK inhibitor program a high
2024-04-29
During the course of our ACK1 inhibitor program, a high-throughput screening (HTS) campaign of our internal sample collection was conducted. A series of -aryl pyrimidine-5-carboxamides of the general structure () was identified. Earlier studies of the structure–activity relationship (SAR) of ident
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br Introduction Myasthenia gravis MG is an
2024-04-29
Introduction Myasthenia gravis (MG) is an autoimmune disease in which antibodies against targets on the postsynaptic muscle membrane cause neuromuscular transmission failure. About 85% of patients with MG have autoantibodies against g protein coupled receptors receptor (AChR) [1]. In AChR negati
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The adoptive transfer experiments additionally demonstrated
2024-04-29
The adoptive transfer experiments additionally demonstrated the role of cholinergic regulation in the antibody immune response. Injection of LPI-stimulated B lymphocytes significantly up-regulated both the IgM and IgG responses to cytochrome c in the host. Obviously, this effect was due to activatio
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To identify the kinase s mediating H
2024-04-29
To identify the kinase(s) mediating H3.3S31 phosphorylation, we devised a 96-well-plate-compatible immunostaining assay, with Nitrotetrazolium Blue chloride specific for H3.3S31ph, and utilized it to screen both a Qiagen siRNA library covering 720 human kinases and a kinase inhibitor library (Sellec
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br Materials and methods br Results br Discussion
2024-04-28
Materials and methods Results Discussion Recently, we showed that stimulation of TRPM3 and TRPC6 channels triggers a signaling cascade leading to the activation of AP-1 [11], [12], [13], [15]. The objective of this study was to investigate whether stimulation of TRPV1 channels leads to an a
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br Introduction Increasing number of mycosis infections has
2024-04-28
Introduction Increasing number of mycosis infections has been reported during the past several years because of the rise in the number of immuno-compromised individuals in subtropical and tropical countries with high mortality and morbidity [1], [2]. Trichophyton mentagrophytes, Trichophyton rubr
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In light of several reports of defects in memory
2024-04-28
In light of several reports of defects in memory-related tasks for the dysbindin-deficient mice (Cox et al., 2009, Takao et al., 2008), it was rather unexpected that an enhancement of CA3–CA1 LTP was observed in our investigation as well as in another independent study (T.T. Tang et al., 2009). The
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LOXs and CYPs are a series
2024-04-28
LOXs and CYPs are a series of iron-containing enzymes that metabolize arachidonic reductase enzyme to form biologically active products, such as epoxyeicosatrienoic acids (EETs) hydroperoxyeicosatetraenoic acids (HETEs), prostaglandins, leukotrienes and thromboxanes [6]. Among these mediators, 12/1
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Lorlatinib is an orally active brain
2024-04-28
Lorlatinib is an orally active brain penetrant cyclic 2-aminopyridine derivative that is a type I½ B ALK inhibitor (Fig. 5F) [61]. This medicinal is an effective antagonist against the more common L1196M and G1269A crizotinib-resistant mutations as well as the less common T1151Ins, L1152R, C1156Y, F
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