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These mutations induce the gene auto
2025-03-03
These mutations induce the gene auto-activation in 10–40% of adenocarcinomas, triggering the EGFR-signaling pathway in the absence of ligand. That leads to an uncontrolled acceleration of cell proliferation, survival and anti-apoptotic signals (Couraud et al., 2012). The frequency of these mutations
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NLX a k a F or befiradol exhibits
2025-03-03
NLX-112 (a.k.a. F13640 or befiradol), exhibits nanomolar affinity at 5-HT1A receptors, and, in ep4 antagonist to the 5-HT1A receptor agonists listed above, it presents exceptional selectivity and high efficacy at these receptors (Colpaert et al., 2002, Newman-Tancredi et al., 2017). Additionally, it
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The anorexic effect observed when AR is
2025-03-03
The anorexic effect observed when AR231630 is infused into the VTA could be the result of the DA release inhibition, as previously described [11]. However, there is also a hedonic aspect in feeding that possibly involves dopaminergic mechanisms of reward. Helm et al. showed a functional link between
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In the late s Solvay Pharmaceuticals discontinued the Phase
2025-03-03
In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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Axl has been reported to mediate cell cell adhesion and
2025-03-03
Axl has been reported to mediate cell-cell adhesion and sphere-growth [11], [18] and to be important for metastasis to secondary organs [12], [14], [20]. We found an Axl-dependent CCRCC-ability of sphere-formation and repopulation after non-adhesive growth. Axl-inhibited cells could not attach to ea
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br Methods br Results br
2025-03-03
Methods Results Discussion Autotaxin has been shown to have effects on major cell types implicated in OA, notably chondrocytes, osteoblasts, osteoclasts, and synoviocytes, through its enzymatic product LPA [20]. However, a paucity of research exists on the involvement of autotaxin in OA. Fi
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Starting with commercially available or nitropyrazole carbox
2025-03-01
Starting with commercially available 4- or 5-nitropyrazole-3-carboxylic acid, anilides containing nitro, amino or methylsulfonamido were synthesized. Here, manipulation of the substituents on the pyrazole ring was conducted after the anilide formation (). The ixazomib of the nitro group was perform
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In addition to calpain I
2025-03-01
In addition to calpain I activity, cathepsin activities have been proven to be linked to apoptotic signaling. Cathepsin B and cathepsin D are two of the most abundant and well-investigated lysosome acid-dependent proteases that are involved in the apoptotic regulation (Ferri & Kroemer, 2001). Cathep
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An in vitro assay in which endothelial cells
2025-03-01
An in vitro assay in which endothelial cells form 3D tube-like structures was used to investigate effects of dNK on vessel stability. The results indicate that dNK cells from women with high spiral artery resistance index had reduced ability to activate endothelial cells, since endothelial cells pre
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Immunohistochemistry Hearts from young and aged mice were
2025-03-01
Immunohistochemistry: Hearts from young and aged mice were collected at the indicated times, fixed overnight in 10% formalin, and embedded in paraffin. Serial 5-μm heart sections from each group were analyzed. Samples were stained with H&E for routine histologic examination. Immunohistochemical stai
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Analysis of the enzyme activity expressed as rate of
2025-03-01
Analysis of the enzyme activity, expressed as rate of product formation per unit serum volume (20μl), between the diagnostic groups revealed that ApB activity was significantly decreased in the patient group both at recruitment and after 13months when the substrate concentration used was 1.5mM (pBYL
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The AHR potentially enhances IDO expression possibly via cro
2025-03-01
The AHR potentially enhances IDO-expression, possibly via crosstalk with several inflammatory signaling pathways (shown by now for IL6 and ‘signal transducer and activator of transcription’ (STAT) 3, and for NFκB, toll like receptor-pathways) [56,59,60]. IDO metabolizes Trp to kynurenines, which are
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However although in vitro studies in heterologous systems ha
2025-03-01
However, although in vitro studies in heterologous systems have provided very important indications of potential novel pharmacology, the studies with endogenous receptors in native tissues are essential to provide evidence for GPCR heteromerization in vivo and to confirm its physiological relevance.
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Moreover an increase of extracellular calcium stimulates BMP
2025-03-01
Moreover, an increase of extracellular calcium stimulates BMP-2 expression of pulp 1602 via L-type calcium channel and ERK signaling, which can be attenuated by PD98059 and nifedipine . Dental pulp cells expressed little calcium-sensing receptors . immunohistochemistry staining also shows the stro
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In eukaryotes class III ACs including GCs
2025-03-01
In eukaryotes, class III ACs (including GCs) are almost universally present, with the noteworthy exception of higher plants. Our dataset comprises 9690 sequences of class III nucleotide cyclases from 710 eukaryotic species. Approximately 80% thereof belong to subclass IIIa and 10% to subclasses IIIb