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Collectively these data suggest the potential clinical utili
2019-10-28
Collectively, these data suggest the potential clinical utility of COMT inhibitors for the treatment of addiction disorders. Similar to current pharmacotherapies such as naltrexone, tolcapone\'s effects were not ethanol specific, therefore tolcapone may be effective in reducing other drug reinforced
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Phenylbenzofurans are a very important molecule
2019-10-28
Phenylbenzofurans are a very important molecule skeleton due to their synthetic versatility and their proved pharmacological properties [2]. They are synthetic compounds in which an additional phenyl ring is present in any position of the benzofuran nucleus. This could be easily obtained possible by
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trk inhibitor br Sources of funding br Disclosures br Acknow
2019-10-28
Sources of funding Disclosures Acknowledgments Introduction Insulin secretion from pancreatic β cells is a fundamental process to maintain blood glucose homeostasis. During glucose-stimulated insulin secretion, high glucose causes closure of ATP-sensitive K+ channels (KATP channels), sub
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The isomeric phenyloxazole not only exhibited
2019-10-28
The isomeric 5-phenyloxazole not only exhibited increased potency against NEP, but also a decreased ACE inhibition thus providing encouraging selectivity. Changing the P1 group from an -propyl to a more polar methoxyethyl at the left hand glucose transporter (as seen in compound pairs – and –) decre
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The in vitro enantioselective metabolism of pesticides has b
2019-10-28
The in vitro enantioselective metabolism of pesticides has been investigated by employing human liver microsomes, which are a reliable resource to perform MCL enantioselective risk assessment in humans (Carrão et al., 2019; de Albuquerque et al., 2018, 2016; Yao et al., 2016). The enantioselective m
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br Materials and methods br Results br
2019-10-28
Materials and methods Results Discussion In this work, we have studied the contribution of different pathways to the slow but stable progression of replication forks through DNA damaged by MMS [15]. The in vivo analysis of DNA replication forks along a specific chromosome of S. cerevisiae h
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br Conclusions br Acknowledgements br Introduction Liver can
2019-10-28
Conclusions Acknowledgements Introduction Liver cancer was the fifth most common cancer and the second leading cause of cancer-related death worldwide [1]. Most of primary liver cancers (70–90%) occurring worldwide are hepatocellular carcinoma (HCC) [2]. Persistent hepatitis B virus (HBV) i
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Among the various neurotransmitter systems
2019-10-25
Among the various neurotransmitter systems pointed out to play a role in the mediation of defensive and antinociceptive responses elicited by environmentally aversive stimuli, the neuropeptide corticotropin-releasing factor or hormone (CRF or CRH) has attracted the interest of many researchers inves
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PGE EP activation has been found to
2019-10-25
PGE2-EP4 activation has been found to attenuate the activation of microglia and to prevent lipid peroxidation and pro-inflammatory gene expression in a murine model of lipopolysaccharide (LPS)-induced apexbio calculator inflammation [15]. Moreover, PGE2/EP4 signaling has elicited a protective functi
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Given its high frequency it is not
2019-10-25
Given its high frequency, it is not surprising that different strategies have been developed to restore the sensitivity of EGFR T790M-mutant mao inhibitors to EGFR inhibition. To date, several different strategies have been evaluated in both preclinical and clinical models, but only few have been p
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Despite the weak and transient nature of E
2019-10-25
Despite the weak and transient nature of E2–E3 interactions, this binding is required for the transfer of ubiquitin to the substrate. The low affinity characteristics of this interaction may be due to the fact that E2s use the same surface to interact with E1s and E3s, and hence while binding to an
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These studies suggested that PV PVH might promote bone
2019-10-25
These studies suggested that PV/PVH might promote bone formation activities and/or inhibit bone resorption activities probably due to its anti-inflammation activity; however, the underlying mechanism remained unknown. Furthermore, it is unclear if PVH shows better activity than that of PV; this is i
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Furegrelate sodium salt Introduction The number of patients
2019-10-25
Introduction The number of patients with type 2 diabetes is increasing globally, and has become a serious public health problem. Type 2 diabetic patients exhibit a higher risk of bone fracture [1]. In addition, clinical studies have indicated that increased fracture risk is associated with long-ter
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Iohexol To examine the influence of aromatic motifs on the
2019-10-25
To examine the influence of aromatic motifs on the bridging lysine esters we analysed DNA alkylating activity of the set of compounds 1–6. The lysine derivatives were chosen as it is relatively easy to prepare different esters and thereby study the impact of different groups on the reactivity toward
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CRF and urocortin I are
2019-10-25
CRF and urocortin I are not only readily found throughout the spinal cord (Korosi et al., 2007), CRF analogs are clearly able to alter nociceptive signals (Imbe et al., 2010; Lariviere and Melzack, 2000). However, it was unclear whether they are released endogenously and involved in the spinal modul
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