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As also found by Stolarski et al
2023-03-11

As also found by Stolarski et al. [14], inclusion of N2O in the model is successful in reducing the effect of dynamics [13] in the lower stratosphere in the Northern Hemisphere (30–60°N in our case). The inclusion of N2O also decreased the error bars on the trend values, but the trend values still c
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We have previously shown that the antinociceptive effect of
2023-03-11

We have previously shown that the antinociceptive effect of tramadol, an analgesic that, like paracetamol is able to increase serotonin levels within CNS, is potentiated or antagonized respectively by a 5-HT1A/B nonspecific CA-074 Me blockade or activation (Rojas-Corrales et al., 2000). Moreover, it
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In order to increase the oral bioavailability abiraterone is
2023-03-11

In order to increase the oral bioavailability, abiraterone (157) is being used in the form of its 3β-acetoxy prodrug, abiraterone acetate (156). In spite of the fact that high-fat meals increase the oral TAI-1 of abiraterone acetate (156), it is recommended that this drug should be taken on an empt
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A variety of quinazoline or fused pyrimidine substituted
2023-03-11

A variety of quinazoline or fused pyrimidine-substituted diaminotriazoles showed sub-100nM inhibition of Axl (). Diaminotriazoles similarly substituted with quinolines, isoquinolines and benzothiazoles also showed potent Axl activity (data not shown), but generally exhibited potent cytotoxicity and
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ATX LPA signaling in cancer is also well known
2023-03-11

ATX/LPA signaling in cancer is also well known to promote chemotherapy and radiotherapy resistance [7]. Furthermore, others have recently shown that endothelial-derived ATX activity in renal cell carcinoma promotes renal tumorgenesis and acquired resistance to sunitinib through an IL-8-mediated mech
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br Autophagy inducers Macroautophagy is often
2023-03-11

Autophagy inducers Macroautophagy is often seen as a cellular process capable of increasing the fitness of BINA mg and overcome resistance to several forms of stress [9], [10]. As discussed above, it has been proposed by several authors that an effective strategy for enhancing sensitivity of can
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Nowadays more than kinases have been identified of
2023-03-11

Nowadays, more than 500 kinases have been identified of human genome [2]. Imatinib (Gleevec) was the first tyrosine kinase inhibitor approved by the US Food and Drug Administration (FDA) for the treatment of chronic myeloid leukemia [3], and kinases have become an attractive target for the developme
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What can we learn about the anticancer
2023-03-11

What can we learn about the anticancer therapeutic efficacy of Aurora kinase inhibitors from our experience with the Bcr-Abl inhibitors and the long term clinical consequence of their use in treating leukemias? As discussed, all Aurora kinase inhibitors developed to date are ATP-competitive inhibito
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In bacteria H gler et al
2023-03-11

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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Based on its kinetic parameters and
2023-03-11

Based on its kinetic parameters and quaternary structure, R. pycnus arginase is a typical ureotelic L-arginase [2]. The Km value of the enzyme was lower than other arginases from other organisms (Table 2), including S. cerevisiae (15.7mM), B. anthracis (10mM), B. caldovelox (3.4mM), human liver (2.3
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Thiol are reduced by two major redox systems glutathione glu
2023-03-10

Thiol are reduced by two major redox systems, glutathione/glutaredoxin (GRX) and thioredoxin (TRX), which have been extensively studied in plants [13], [14], [15]. Glutathione, a thiol-containing tripeptide, exists in a reduced (GSH) or an oxidized form (GSSG). It has a major role as a redox buffer.
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The cellular mechanism underlying the CGS mediated inhibitio
2023-03-08

The cellular mechanism underlying the CGS12066-mediated inhibition of glutamate release from hippocampal nerve terminals through presynaptic 5-HT1B receptors remains to be elucidated. 5-HT1B receptors are coupled to PTX-sensitive G proteins (Gi or Go) that have been shown to inhibit AC activity as w
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Since natural and recombinant glycoprotein hormones exhibit
2023-03-08

Since natural and recombinant glycoprotein hormones exhibit some differences in their carbohydrate structures, we checked whether this could affect the permissive effect on FSK-induced cyclic AMP response in MLTC-1 cells. Fig. 6 shows that the same sensitizing effect to FSK is observed with pituitar
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It has been reported that leukotrienes and their receptors e
2023-03-07

It has been reported that leukotrienes and their receptors, e.g. the cysteinyl leukotriene receptor 1 (CysLT1) may promote S63845 injury (Ding et al., 2007) and that increased 5-LOX expression and activity lead to production of brain-toxic molecules (Khan et al., 2010). However, differential effects
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The cellular mechanism underlying the CGS mediated inhibitio
2023-03-07

The cellular mechanism underlying the CGS12066-mediated inhibition of glutamate release from hippocampal nerve terminals through presynaptic 5-HT1B receptors remains to be elucidated. 5-HT1B receptors are coupled to PTX-sensitive G proteins (Gi or Go) that have been shown to inhibit AC activity as w
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