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The evidence points toward a role for
2025-01-24
The evidence points toward a role for 12/15-LO activity in WAT in modulating chronic local inflammation and subsequent systemic metabolic decline in the obese state. However, little is known as to the role of 12- and 15-LOs in BAT. Indeed, in addition to WAT, platelet- and leukocyte-type 12-LO are e
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br Development of lorlatinib from crizotinib to a clinical
2025-01-24
Development of lorlatinib from crizotinib (1) to a clinical candidate (6) Xalkori (1, PF-02341066, crizotinib), was the first-in-class ALK inhibitor approved by the Unites States Food and Drug Administration (FDA) in 2011 as a first-line treatment for ALK+- NSCLC patients. This section describes
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br Co http www apexbt
2025-01-24
Conclusions This paper is the first meta-analysis about the association between SRD5A2 V89L polymorphism and hypospadias risk. The results of this meta-analysis have revealed that V89L polymorphism definitely increases the risk of hypospadias, and the C allele is a genetic risk factor for hypospa
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br Regulation and pharmacology of mPGES mPGES kDa amino acid
2025-01-24
Regulation and pharmacology of mPGES-1 mPGES-1 (16 kDa, 152 amino acids) is a trimeric integral membrane protein of the endoplasmic reticulum with each monomer containing four transmembrane domains (Samuelsson et al., 2007; Sjogren et al., 2013). The three active site cavities are located at the
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Thirty six of the analogs synthesized showed ATX inhibition
2025-01-23
Thirty-six of the analogs synthesized showed ATX inhibition greater than 50% at 10μM with FS-3, twelve of which had improved potency over the lead (Fig. 5). Of these, 22 was sub-micromolar (IC50 670nM). The 3,5-dichlorophenoxy ring of 22 is reminiscent of the 3,5-dichlorophenylthiourea ring in Hoegl
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Imatinib is a well known anticancer drug used
2025-01-23
Imatinib is a well-known anticancer drug used in Chronic Myeloid Leukemia (CML) against the altered expression/activity of tyrosine kinase resulting from the fusion of BCR-ABL in leukemic blasts. It has been demonstrated that Imatinib can induce autophagy in BCR-ABL expressing Wnt signaling suppress
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In the pituitary of R quelen mRNA levels of cyp
2025-01-23
In the pituitary of R. quelen mRNA levels of cyp19a1b were found to be higher in males than females, suggesting a sex-specific function, and perhaps a local action to regulate gonadotropins or other pituitary hormone secretion (Olivereau and Callard, 1985; Zhang et al., 2014). Interestingly, the hig
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hexadimethrine bromide polybrene It has been proven that
2025-01-23
It has been proven that genetic polymorphisms can play an important role in development of hypertension and CVDs. In a Turkish population-based study, it was found that the APLNR gene (rs948847-A445C) polymorphism was not associated with coronary artery disease (CAD), but it was shown to be related
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br AR expression in breast tissue Although androgenic signal
2025-01-23
AR expression in breast tissue Although androgenic signalling is chiefly associated with the development and maintenance of primary and secondary male characteristics, especially during puberty when the testes are by far the major source of testosterone, the AR also plays important functions in f
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br Introduction Metabolic cues are crucial inputs in dictati
2025-01-23
Introduction Metabolic cues are crucial inputs in dictating acute responses through governing cellular signaling pathways as well as in shaping up long-term transcriptional and epigenetic profiles to control chronic cellular responses (Lu and Thompson, 2012). It has been well documented that meta
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While high fat diet models of
2025-01-23
While high-fat diet models of insulin resistance are acceptable approaches for the study of pre-diabetes in humans, they are not suitable for modeling progression towards established type2 diabetes. The pattern of activation of the lipoxygenase pathway in pre-clinical models of type2 diabetes has no
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Some of the earliest LOX inhibitors were
2025-01-23
Some of the earliest 12-LOX inhibitors were redox inhibitors, including nordihydroguaiaretic Catechol structure compound (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 inactive (Fe2+) to t
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A limitation of the NIA AA recommendations was that
2025-01-23
A limitation of the 2011 NIA-AA recommendations was that biomarkers were grouped into just two categories—amyloid and tau-related neurodegeneration. Tauopathy and neurodegeneration were placed into the same biomarker category. In persons with only AD, it is reasonable to assume that neurodegeneratio
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br Materials and Methods br Results In the
2025-01-23
Materials and Methods Results In the Base Analysis (53% of patients having access to the ALK test in both Current and Alternative Scenarios), a total of 16,583 patients were tested of whom 1,252 were assumed to be ALK-positive. A more extensive use of Ventana in the Alternative Scenario determ
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In conclusion phenolic hydroxyl was introduced not only
2025-01-23
In conclusion, phenolic hydroxyl was introduced not only to C3 side chain but also to C6 or C7 position of the quinoxalinone core, resulting in a new group of ARIs candidates exhibiting antioxidant activity. Biological activity tests suggested that compounds were not only sufficient to inhibit ALR2
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