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One possible pitfall of using EPAC activators in
2020-03-20

One possible pitfall of using EPAC2 activators in the treatment of T2DM is their potential to increase glucagon levels. As discussed previously, although the ability of EPAC2 to increase glucagon expression and production is controversial, several studies show that this protein increases Gcg mRNA le
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Programmed cellular death or apoptosis is a process genetica
2020-03-19

Programmed cellular death or apoptosis is a process genetically controlled that plays an important role in cellular homeostasis, being an important defense mechanism to remove cells that have been infected, damaged or mutated (Smith and Smith, 2012, Wlodkowic et al., 2011). Nevertheless, apoptosis s
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Our recent discovery M P
2020-03-18

Our recent discovery (M.P., H.R., A.S.) of a highly selective and in vivo active DDR1 small-molecule inhibitor provides evidence that DDR1 is a druggable pharmaceutical target, and some details of our efforts are provided below. To avoid the repurposing of known kinase inhibitor structural motifs, w
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DDI is one of the
2020-03-18

DDI is one of the main problems with serious clinical consequences in clinical settings. Several reports have highlighted the role of modulation of drug-metabolizing enzymes, especially CYP450 s, as a major mechanism involved in clinical DDIs [3,4,7]. The present study aimed to investigate the effec
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Itraconazole Most data regarding fish CXCR functions have ac
2020-03-18

Most data regarding fish CXCR4 functions have accumulated from work in zebrafish where a range of genetic tools and imaging technologies have been developed. As mentioned above, in teleost fish the two CXCR4s (CXCR4a and 4b) are assumed to interact with two ligands (CXCL12a and 12b) and this differe
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To determine the time course of ZD P CPG
2020-03-18

To determine the time course of ZD2767P+CPG2 DNA–DNA interstrand cross-link formation, HT29 and LS174T colorectal tumour cp-690550 receptor were exposed to the drug for 10, 30 or 60 min. The levels of DNA interstrand cross-links in HT29 or LS174T cells did not increase with exposure time, suggesting
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The transcription factor CREB has been extensively studied
2020-03-18

The transcription factor CREB has been extensively studied for its role in hippocampus-dependent learning and memory (West et al., 2002, Lonze and Ginty, 2002). Previous research has demonstrated that the phosphorylation of CREB at Ser133, performed by the ERK1/2 signaling pathway, initiates a casca
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EP is the major receptor to
2020-03-18

EP4 is the major receptor to mediate PGE2-induced inflammatory pain. EP4 is upregulated by 5-Iodotubercidin australia in DRG neurons [16]. Intrathecal injection of the EP4 agonist produced pain responses [25]. Either systemic or local injection of EP4 antagonists relieves inflammatory pain [3], [16
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A major open question in the
2020-03-18

A major open question in the field of lipid mediators is the molecular nature of the PLA2 enzyme involved in the release of DHA and related omega-3 fatty acids from phospholipids as a first committed step for the generation of SPMs. Although by analogy with AA it is often assumed that cPLA2α may ser
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In conclusion using human liver microsomes supersomes from b
2020-03-18

In conclusion, using human liver microsomes, supersomes from baculovirus-transformed insect cells expressing different human CYP450 isoforms, and V79MZh3A4 cells, MB2 and MB4 were formed from TRB and MC from TRC. The amounts of MB2, MB4, and MC formed were related to the 6β-testosterone hydroxylase
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A study profiling chemokine expression in LCLs revealed high
2020-03-18

A study profiling chemokine expression in LCLs revealed high expression levels of CCR6, CCR7, and CCR10 and low expression of CXCR4 and CXCR5 in EBV immortalized cells. Accordingly, LCLs showed a markedly increase in migration in response to the ligands of CCR6 (CCL20), CC7 (CCL21), and CCR10 (CCL28
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The collagen binding membrane proteins discoidin
2020-03-18

The collagen-binding membrane proteins, discoidin domain receptors 1 and 2 (DDR1 and DDR2) belong to the family of receptor tyrosine kinase and are expressed in a variety of mammalian cells.7, 8 These transmembrane glycoproteins (∼125 kDa) have been found to be over-expressed or atypically expressed
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A further quandary concerning rediscoveries arises in habita
2020-03-17

A further quandary concerning rediscoveries arises in habitats modified and frequented by humans, where rediscovered species may occur through accidental or deliberate introductions (Metcalf et al., 2007) rather than having persisted despite adverse conditions. Confusion regarding origin could evoke
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The importance of mitochondria as site of
2020-03-17

The importance of mitochondria as site of aerobic oxidation of metabolic fuels, such as FA, has been recognized for a long time. It has been observed that the number of mitochondria may vary in response to cellular metabolic requirements and hormonal environment (Gao et al., 2014). In order to susta
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Nevertheless of the different types of
2020-03-17

Nevertheless, of the different types of scoring systems so far proposed, each of these [14], [29], [30] considered some aspects that could describe the fibrotic evolution, though none provided a quantitative assessment. Calvaruso et al. [8] showed that CPA had a better histological correlation with
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