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Negative regulation of AR expression by
2023-03-02
Negative regulation of AR expression by NFκB was also correlated with the ‘age-dependent desensitisation’ of androgen action in the rat liver (Supakar et al., 1995). In this case the binding site was mapped upstream of the gene to sequences −555 to −565 bp, that binds heterodimers of p65 and p50, as
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Circular dichroism CD provides useful information about prot
2023-03-02
Circular dichroism (CD) provides useful information about protein structure, the extent and rate of structural changes and ligand binding. CD is a form of light a83 spectroscopy that measures differences in the absorbance of right- and left-circularly polarized light (rather than the commonly used
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br Conflict of interest statement br Acknowledgement br Intr
2023-03-02
Conflict of interest statement Acknowledgement Introduction Lipoxygenases (LOs) are enzymes catalyzing the positional as well as stereo-specific introduction of molecular oxygen into 1,4-pentadiene structures found in unsaturated fatty acids such as arachidonic Spadin or linoleic acid [1],
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br Development of lorlatinib from crizotinib to a
2023-03-02
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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Di ethylhexyl phthalate DEHP is one of the
2023-03-02
Di-(2-ethylhexyl) phthalate (DEHP) is one of the most widely used environmental chemicals in the production of polyvinyl chloride. After AZD1390 into human body, DEHP can be converted to the metabolite mono-ethylhexyl phthalate (MEHP), which has higher toxicity than DEHP and can influence reproduct
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AHR mediated MMP upregulation has been shown in response
2023-03-02
AHR-mediated MMP1 upregulation has been shown in response to tobacco smoke [32]. Tobacco smoke contains various AHR ligands such as benzo[a]pyrene. Both benzo[a]pyrene [15] and FICZ [13] are high-affinity ligands for AHR and upregulate CYP1A1 and CYP1B1. FICZ is rapidly degraded by CYP1A1 [20], [33]
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br Adenosine as a mediator of procedures used to manage
2023-03-02
Adenosine as a mediator of procedures used to manage pain The issue of caffeine Caffeine, from dietary sources, is perhaps the most widely consumed behaviorally active agent in the world (Fredholm et al., 1999). Initial characterization indicated caffeine had a higher affinity at A1−, A2A− and
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Because LTs are proved to
2023-03-02
Because LTs are proved to mediate multiple biological and pathological responses in various disease states, the 5-LO biosynthetic pathway producing LTs from AA have been the target of drug discovery efforts for over two decades. As observed from literature, a pile of research efforts has been direct
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Tobramycin Plant defensins are cysteine rich cationic peptid
2023-03-01
Plant defensins are cysteine-rich cationic peptides of 5–8 kDa whose mature domain comprises 45 to 54 amino Tobramycin residues, with an isoelectric point around 9. The global fold of plant defensins consists of a cysteine-stabilized motif (CSα/β) made up of an α-helix and a triple-stranded β-sheet
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AT7519 Hydrochloride Sustained release property is also asso
2023-03-01
Sustained release property is also associated with side effects reduction [16] that could be confirmed by histopathological analyzes. Massive infiltrating inflammatory cells, hyperproliferation of skin layers and keratin pearls, caused by DMBA and croton oil application [32] are attenuated in Imq-lo
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Consistent with the in vitro results memantine ameliorated A
2023-03-01
Consistent with the in vitro results, memantine ameliorated Aβ-induced cytotoxicity in rat primary cortical cultures. Studies reported that memantine protected neurons against the damage caused by aggregated Aβ40 or Aβ42 oligomers in vivo[26], [27]. These results suggest that, in addition to its neu
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Although only Leu CysAP IRAP Herbest et al Keller and
2023-03-01
Although only Leu/CysAP (IRAP) (Herbest et al., 1997, Keller, 2004) and DPPIV (Alponti and Silveira, 2010, Kirino et al., 2009) had been identified and studied in adipocytes, our kinetic analysis suggested the highest physiological significance for AspAP (highest affinity) and APM and PSA (highest e
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Tephrosia purpurea Linn pers Fabaceae
2023-03-01
Tephrosia purpurea (Linn.) pers, (Fabaceae), a widely growing herbaceous perennial is reported to exhibit significant anti-hyperglycemic activity in animal models [7], [8], [9] as well as able to delay the development of diabetic complications [10], [11]. Recently, we have reported T. purpurea for i
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Diabetes or inflammation is associated with up
2023-03-01
Diabetes or inflammation is associated with up-regulation of A2AAR (Pang et al., 2010). High levels of A2AARs are found in macrophages and microglial cells that are poised, on activation, to abrogate the immune response (Trincavelli et al., 2008). In addition, hyperglycemia is associated with increa
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In this study PRP positively regulated MIIP levels
2023-03-01
In this study, PRP4 positively regulated MIIP levels and significantly inhibited the invasion of HCT116 cells. Further investigations elucidated that PRP4 dephosphorylated MIIP via PP1A regulation, which was confirmed by PP1A inhibition in the presence of OA. Upon dephosphorylation, MIIP possibly in
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