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An intriguing feature of the
2020-03-11

An intriguing feature of the pre and postsynaptic processes at the level of the VTA that have been shown to be mediated by CRF2 receptors [9], [34] is that they are exerted only by agonists with high affinity for both CRF2 receptors and CRF-BP. The four endogenous peptides of the CRF system have hig
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br Materials and methods br Results br
2020-03-11

Materials and methods Results Discussion One novel finding in our study is that CK2 inhibition preserved axon function and structure in WM against ischemia. Consistent with these findings, oligodendrocytes, astrocytes, myelin, and alpha-Endorphin mg were found to express CK2α. The robust e
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br Funding br Conflict of interests br
2020-03-11

Funding Conflict of interests Introduction DAG is generated by the hydrolysis of phosphatidylinositol-4,5-bisphosphate (PtdIns(4,5)P2) by PtdIns-specific phospholipase C (PLC) enzymes [1]. Remaining in the membrane, it binds proteins with cysteine-rich, C1 domains, and activates several of
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Eltrombopag Olamine Interestingly several ES cell lines are
2020-03-11

Interestingly, several ES cell lines are null for p53, possibly because the EWS-FLI1 chimeric protein can directly and indirectly interfere with p53 activity [38], [39]. The inhibition, loss and/or mutation of p53, one of the most common events in tumorigenesis, results in a decreased oxygen consump
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Prostaglandin E PGE is involved
2020-03-11

Prostaglandin E2 (PGE2) is involved in several biological processes such as renal function, inflammation, angiogenesis, and tumor growth. The various biological effects of PGE2 are mediated by the so-called E-type prostanoid receptors (EP1 to EP4). Among these, the EP4 receptor has been well studied
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We should also note that oxygen pressure
2020-03-11

We should also note that oxygen pressure of Krebs solution bubbled with 95% O2+5% CO2 as we used in our study is reported to around 400 mmHg in several studies [48], [49], which is higher than normal arterial O2 pressure (80–100 mmHg). Although superoxide generation at elevated O2 tensions are noted
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br Introduction Our understanding of how ligands interact wi
2020-03-11

Introduction Our understanding of how ligands interact with G protein coupled receptors is evolving, particularly the recognition that some have the ability to preferentially activate a subset of intracellular signalling cascades – so called pathway biased ligands [1]. Additionally, it is now ac
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Metal ions are known not to be necessary
2020-03-11

Metal ions are known not to be necessary for catalytic activity of serine proteinases. Nevertheless, Co2+ and Ca2+ ions were found to stabilize glutamyl endopeptidase molecule [1], [7], [19]. In our previous study, we have described significant stimulating effect of Ca2+, Mg2+, and Co2+ on biosynthe
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A factor that complicates the use of human liver cells
2020-03-10

A factor that complicates the use of human liver Ezatiostat hydrochloride is one of variability, which arises in part because many of the human liver samples available for research show various stages of a variety of disease states (steatosis (fatty liver), cirrhosis, carcinogenesis in adjacent tis
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Several highly potent CysLT receptor antagonists with large
2020-03-10

Several highly potent CysLT1 receptor antagonists with large structural PFI-2 synthesis have been developed. Beyond antagonists with structures analogous to cysteinyl leukotrienes, other subclasses comprise: (a) hydroxyacetophenones, (b) indoles and indazoles, (c) quinolines, benzothiazoles, and th
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It would be very useful if unphosphorylated CK
2020-03-10

It would be very useful if unphosphorylated CK1s could be prepared using an E. coli expression system without the troublesome in vitro phosphatase treatment. So far, it has been shown that coexpressed λPPase, a Mn2+-dependent protein phosphatase that can dephosphorylate phospho-Ser/Thr/Tyr [20,21],
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MTX and MTXPGs block the activity of the key enzyme
2020-03-10

MTX and MTXPGs block the activity of the key enzyme DHFR (Fig. 1), which converts folates to their active forms – dihydrofolate (DHF) and tetrahydrofolate (THF). MTXPGs also potently inhibit thymidylate synthase (TS). Furthermore, during dTMP synthesis, TS utilizes the cofactor 5,10-methylene THF, w
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cyclin dependent kinases br Fragment based drug discovery FB
2020-03-10

Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical cyclin dependent kinases space with libraries which are smaller in size, producing drug leads with high ligand-binding e
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On the other hand p responds to environmental
2020-03-10

On the other hand, p38 responds to environmental stress, including ultraviolet light, heat, osmotic shock, and inflammatory cytokines (Pearson et al., 2001, Kumar et al., 2003), and is activated in astrocytes after ischemia-like injury (Yung and Tolkovsky, 2003, Niu et al., 2009). Moreover, p38 acti
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Introduction Cysteinyl leukotrienes CysLTs LTC
2020-03-10

Introduction Cysteinyl leukotrienes (CysLTs), LTC4, LTD4 and LTE4, are 5-lipoxygenase pathway metabolites of arachidonic AM095 and deeply involved in bronchial asthma via activation of CysLT1 receptors [1], [2]. Specific CysLT1 receptor antagonists, including pranlukast [3], [4] and montelukast [5
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