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Consistent with previous reports of an association between
2021-11-29

Consistent with previous reports of an association between increased accumulation of cAMP and GLP-1 secretion [25, 44, 45], we hypothesized that Oleoyl-LPI may regulate GPR119 activation and secretion of GLP-1 secretion through the cAMP/PKA/CREB pathway. Pharmacological inhibition of PKA by H-89 was
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Milligan et al demonstrated the important role
2021-11-29

Milligan et al. [31] demonstrated the important role of TNF-α, IL-6 and IL-1β in the development of mechanical hyperalgesia induced by intrathecal injection of gp120. Because of this work, we decide to produce and purify gp120 to develop biological systems to study pain and behavior in rodents. Intr
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Among the compounds prepared at this stage the cyclopropylme
2021-11-29

Among the compounds prepared at this stage, the cyclopropylmethylenoxy analogue attracted our most attention since it demonstrated particularly good in vitro potency at GlyT1 (16nM), no activity at the GlyT2 isoform up to the highest concentration tested (30μM), good physical properties with modera
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Our results indicate that abcb
2021-11-29

Our results indicate that abcb5 is likely to be a XT in zebrafish ionocytes, although, like renal cells, the phenotypes observed likely arise from the action of multiple transporters. Zebrafish lack an abcb1 ortholog, and abcb4 and abcb5 have been identified as the P-glycoproteins in zebrafish (Fisc
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br Ligand binding free energies In
2021-11-26

Ligand-binding free energies In order to compute the absolute free BML-277 associated with binding a ligand to a flexible iGluR LBD, a theory that accounts for all the principal thermodynamic contributions from ligand docking and LBD closure had to be developed. This was accomplished using an ap
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Although most of the incretin effects on glucose metabolism
2021-11-26

Although most of the incretin effects on Diclofenac Sodium metabolism can be secondary to their action on insulin/glucagon secretion, some evidence strongly suggests that they could also act directly on liver glucose utilization and production [4], [13], [22], [27], [34], [44]. Supporting this conc
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AKR D is very highly expressed in human liver
2021-11-26

AKR1D1 is very highly expressed in human liver and based upon the observations outlined above, with respect to other steroid hormone pre-receptor metabolising enzymes, it is entirely plausible that AKR1D1 could represent a critical regulatory step in the control of metabolic phenotype within the liv
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Fig a and b illustrates a slow inhibition by
2021-11-26

Fig. 3a and b illustrates a slow inhibition by PMA in 2 μM Ca2+. Moreover, channel inhibition was reversed by addition of PKC19–31, a peptide inhibitor specific for PKC, as shown in Fig. 3c. In three experiments, Im was reduced to 14.5±0.6% of the control value by PMA to increase to 207.6±73.6% by a
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Studies regarding secretase nowadays aim at elucidating how
2021-11-26

Studies regarding γ-secretase nowadays aim at elucidating how APP is recognized and recruited. It has been suggested based on coarse-grained molecular simulation that the recognition and recruitment of substrate can occur on an extended surface covering PS1's TM2/6/9 domains and PAL motif [15]. Tran
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Previous research has suggested that
2021-11-26

Previous research has suggested that differences in spatiotemporal regulation of intracellular signaling pathways can confer specificity to cellular responses (Marshall, 1995). Conventional approaches based on gain- or loss-of-function genetic manipulations or small-molecule inhibitors, however, lac
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Following these discoveries the term ferroptosis was coined
2021-11-26

Following these discoveries, the term ferroptosis was coined in 2012 [25], to describe this iron-dependent, non-apoptotic form cell death induced by erastin and RSL3. This discovery was accompanied by the development of the first small molecule ferroptosis inhibitor, termed ferrostatin-1, and the de
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br Acknowledgements br Introduction Muscle FBPase is
2021-11-26

Acknowledgements Introduction Muscle FBPase is very sensitive to AMP inhibition and in the presence of physiological concentrations of this effector in muscle fibres FBPase should be almost completely inactive [1], [2]. Recently, we have presented evidence that, in vitro, muscle aldolase binds
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Apoptosis via Fas FasL system has been evidenced
2021-11-26

Apoptosis via Fas/FasL system has been evidenced to play a role in the pathogenesis of many diseases [26], [27], [28], [29], [30], [31], [32], [33], [34]. Along with these, Fas/FasL system has an important role in progressive renal disease and organ rejection in renal, cardiac and liver transplanta
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Two recently developed highly specific EZH enzymatic inhibit
2021-11-26

Two recently developed, highly specific EZH2 enzymatic inhibitors, GSK126 and EPZ-6438, are currently in clinical trials for treating lymphomas (Kim and Roberts, 2016). Although these EZH2 inhibitors have shown antitumor effects in lymphoma cells with enzyme-activating mutations of EZH2 (Knutson et
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Structurally HMTs can be broadly categorized into three func
2021-11-26

Structurally, HMTs can be broadly categorized into three functional enzymatic families, the SET (Suppressor of variegation, Enhancer of zeste, Trithorax)-domain- containing methyltransferases, the non-SET DOT1-like (DOT1L) lysine methyltransferases, the PRDM family, containing a PR (PRDI-BF1-RIZ1 ho
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