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IC values were obtained for an expanded version of the
2025-01-13
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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br Introduction In addition to ATP production
2025-01-13
Introduction In addition to ATP production, an important role of mitochondria in the pancreatic beta cell is anaplerosis, which is the net synthesis of citric sphingosine 1 phosphate receptor modulator cycle intermediates that are exported to the cytosol where they are converted to numerous other
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In bacteria H gler et al
2025-01-13
In bacteria (Hügler et al., 2007, Kanao et al., 2001), a glaucophyte alga (Ma et al., 2001), green algae/land plants (Fatland et al., 2002), and filamentous fungi (Nowrousian et al., 2000), ACL enzyme activity requires ACLA, and ACLB (referred to here as dual-subunit ACL, or dsACL) (Kanao et al., 20
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Although TP status has been shown to play
2025-01-10
Although TP53 status has been shown to play a role in ATR inhibition and platinum resistance [7], [27], [38], in inhibition of ATM and sensitivity to IR [39], and in the activation of Chk1 and Chk2 [3], [4], ATM and ATR signaling can occur through the p38MAPK/MK2 pathway in p53-deficient Cy3.5 NHS e
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Recently competitive inhibitors of arginase have been
2025-01-10
Recently, competitive inhibitors of arginase have been developed which have greater specificity for the enzyme. Initial development of these compounds involved determination of the crystal structure of arginase. Christianson and colleagues found that a binuclear manganese cluster was required for ca
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As regards LEPR Sun et
2025-01-10
As regards LEPR, Sun et al. showed that the rs1137101-223A > G polymorphism influences the effectiveness of simvastatin on plasma HDL-C levels in CHD patients [35]. In accordance with the results of García-Bermúdez et al., however, no such an association exists between leptin rs2167270 (G > A) polym
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Thalidomide is now a well known antiangiogenic
2025-01-10
Thalidomide is now a well known antiangiogenic agent. This property of thalidomide is being extensively researched upon, for its significant utility in the treatment of various malignant tumors. Studies show that thalidomide efficaciously inhibits various pro-angiogenic factors such as tumor necrosi
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For the first series we decided to
2025-01-10
For the first series we decided to verify the effects induced, on the ALR2 inhibitory properties, of an additional steric hindrance on the carbon in α position with respect to the carboxylic group, by introducing a methyl group (R2=Me). Therefore, we synthesized a series of new α-alanine derivatives
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We next considered the effect
2025-01-10
We next considered the effect of alkyl chain length on the inhibitory activity. As can be seen from , it is obvious that there is no proportional relationship between the methylene chain length and activity. The activity decreased when the chain length increased from 1 to 3 and increased with elonga
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Interestingly our transgenic mouse model with macrophages ex
2025-01-10
Interestingly, our transgenic mouse model with macrophages expressing AdipoR1 showed not only improved insulin sensitivity and inflammation in skeletal muscle and adipose tissues, but fat mass, macrophage and plasma lipid accumulation and foam cell formation was also favorably reduced resulting from
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Because activation of HT A receptor
2025-01-10
Because activation of 5-HT2A receptor is capable of facilitating dopamine cell activity and dopamine release (Bortolozzi et al., 2003), and this action of dopamine is known to mediate rat maternal behavior, especially maternal motivation (Afonso et al., 2007, Febo et al., 2010, Li and Fleming, 2003,
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br Introduction The chronic inflammation
2025-01-10
Introduction The chronic inflammation is one of the leading events involved in the aetiology of many chronic-degenerative diseases including diabetes, atherosclerosis, arthritis and cancer (Coussens and Werb, 2002). Monocytes/macrophages lineage plays an important role during inflammation through
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Most studies on d penicillamine induced MG
2025-01-10
Most studies on d-penicillamine-induced MG were performed before the discovery that some MG patients have anti-MuSK antibodies. After the identification of the present case, we retrospectively tested the stored frozen sera of ten earlier identified d-penicillamine MG patients with anti-AChR Triacsin
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Among the AXL positive tumors that we screened the TNBC
2025-01-09
Among the AXL-positive tumors that we screened, the TNBC cell line MDA-MB-231 showed the highest AXL expression level. Additionally, AXL protein levels were higher in TNBC patient samples than in other breast cancers. Considering the difficulty of, and the urgent need for, effective treatments of TN
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We have recently reported a regulatory effect of quercetin
2025-01-09
We have recently reported a regulatory effect of quercetin on the AChE activity in the brainstem during the demyelination and remyelination process [17]. It has also been observed that there is a protective effect on lipid peroxidation and worsening of motor functions caused by loss of myelin in the
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