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Roflumilast GABAB receptor is associated with
2024-01-19
GABAB receptor is associated with Roflumilast and behavioral diseases, including epilepsy, spasticity, anxiety and neuropathic pain (Bettler et al., 2004, Bowery et al., 2002, Froestl, 2010). Baclofen, a clinical drug and selective GABAB receptor agonist, is used to treat muscle spasticity in patie
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Several alterations have been or can be associated to the
2024-01-19
Several alterations have been or can be associated to the decreased tolerance of steatotic liver to I/R injury. Previous studies demonstrated that upregulation of the mitochondrial uncoupling protein-2 (UP2) is strictly related to the increase of I/R injury in steatotic liver [4]. UPR induction is c
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Besides one should also consider that all antioxidant compou
2024-01-18
Besides, one should also consider that all antioxidant compounds (free soluble or insoluble bounds) exist all together in colon, where radicals and antioxidant compounds react continuously with each other. At this point, after the consumption of antioxidants bound to dietary fiber, they reach the co
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It remains to elucidate whether proteolytic
2024-01-18
It remains to elucidate whether proteolytic activity is the cause or the consequence of changing levels of peptidergic substrates. In fact, in some cases, the expression of the enzyme does not necessarily parallel with its activity [26], [55], [57] and other factors such as a definite biochemical en
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Derivatives of M that possess either an
2024-01-18
Derivatives of (+)-M100907 that possess either an alkyne or an azide have been synthesized. The most active enantiomer was obtained by resolution of a relatively early intermediate in the synthesis. The ability of these fda approved to maintain 5-HTR antagonist properties as (+)-M100907 was demonst
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AMPK modulates changes in lipid metabolism
2024-01-18
AMPK modulates changes in lipid metabolism via the regulation of fatty Cyclosporin D oxidation and cholesterol synthesis in the liver. The key enzymes involved include ACC and HMGCR [27,28]. Both participate in the rate-limiting steps of fatty acids and cholesterol synthesis and are inactivated on p
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br Experimental section br Results and
2024-01-18
Experimental section Results and discussion Conclusion In the present study, 3a,8a-dihydroxy-8-oxo-1,3,3a,8a-tetrahydroindeno[1,2-d]imidazol-2(1H)-iminium chloride (3) has been synthesized and characterized by spectral studies and single crystal X-ray crystallography. DFT calculations have
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The relatively high concentration of HT
2024-01-18
The relatively high concentration of 5-HT used in this study (100 µM) is consistent with the concentrations used in other published ex vivo studies (Ropert and Guy, 1991, Passani et al., 1994, Shen and Andrade, 1998). In our paradigm 5-HT was focally applied at the surface of the slice via a fast pe
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Here we show that the co activation
2024-01-17
Here, we show that the co-activation of RTKs and non-RTKs is a common trait in treatment-naïve EGFR-mutation-positive NSCLC Fluoxymesterone and patients, with AXL and CDCP1 being commonly over-expressed. The combination of gefitinib or osimertinib with the Src/FAK/Janus kinase 2 (JAK2) inhibitor TP
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The molecular mechanisms involved in the pathogenesis of
2024-01-17
The molecular mechanisms involved in the pathogenesis of cholestatic pruritus remain unknown [45], [46]. Indeed, there has been an enormous effort at understanding the etiology of PBC-related pruritus, including work at the cellular and molecular level, but such efforts have not been translated into
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Aurora A or B selective and pan aurora inhibitors have
2024-01-17
Aurora -A or -B selective and pan-aurora inhibitors have demonstrated different preclinical and clinical therapeutic efficacies [2,[19], [20], [21], [22], [23]]. For example, clinical trials for a pan-Aurora inhibitor VX-680 (developed by Vertex) were halted at phase II for toxicity reasons (one cas
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In the present study we sought
2024-01-17
In the present study we sought to decipher the role of ATP-citrate lyase and of the mitochondrial NADH-dependent Mae in the oleaginous yeast Y. lipolytica. Indeed, although this yeast is one of the major models for lipid metabolism, the function of these enzymes is still not clear. As the study of t
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As with most G protein
2024-01-17
As with most G protein-coupled receptors (GPCRs), sustained activation of APJ can cause desensitization and this has been reported to occur for APJ-mediated effects on cytoplasmic Ca2+ concentration, as well as for effects on activity of adenylyl cyclase, ERK and Akt (Ishida et al., 2004, Masri et a
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We have shown that an extensive region in
2024-01-17
We have shown that an extensive region in SERBP1 (amino acids 354 to 474, using co-ordinates based on the full-length isoform, Figs. 1a and 2) is necessary for it to interact with RACK1; since this region has substantial homology to the corresponding region of HABP1 (Fig. 3) it is a reasonable hypot
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br Concluding Remarks and Future Perspectives The
2024-01-17
Concluding Remarks and Future Perspectives The collective evidence from studies detailing the functions of AMPK in the neuromuscular system, combined with those in DMD, SMA, and DM1 surveyed in the present review, strongly suggests that AMPK is a central mediator of neuromuscular determination, m
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