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Nicastrin is heavily glycosylated contributing
2022-02-17
Nicastrin is heavily glycosylated, contributing 40–70KDa to the molecular weight of human γ-secretase. Among the 16 predicted N-linked glycosylation sites in the ECD, 11 have been unambiguously identified. The glycans appear to mostly stabilize the local structure, thus contributing to the folding a
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Target regulated the formation of G quadruplex was used
2022-02-17
Target-regulated the formation of G-quadruplex was used here to “kill two Ezatiostat with one stone” for the detection of melamine and I− with one probe DNA. G-quadruplexes are higher-order structures formed from G-rich oligonucleotides through the stacking of planar G-tetrads [43,44]. They have be
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br STAR Methods br Acknowledgments We would like
2022-02-16
STAR★Methods Acknowledgments We would like to thank V. Gladyshev (Harvard), H. Kornblum (UCLA), L. Greene (Columbia), and J. Baraban (Johns Hopkins) for constructive comments to the project and manuscript. We thank L. Gross and A. Kumar for assistance with editing. We thank L.M. Gerber and Z.
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It raises a question about origin
2022-02-16
It raises a question about origin of the sensitivity to Ca of both FBPase isozymes. Was the ancestral vertebrate FBPase inhibited by calcium similarly to the liver isozyme? And is the high sensitivity of FBP2 a new evolutionary feature of warm-blooded vertebrates? Additionally, since subcellular lo
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Several observations about structure activity relationships
2022-02-16
Several observations about structure–activity relationships can be made from this series, including that: (1) all lead compounds are NSAIDs of the 2-arylpropionic igf1r inhibitor class, (2) analogues with -oriented aryl substituents showed the best inhibition of FAAH, and (3) replacing the ether lin
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Pyronaridine Tetraphosphate mg Recent findings of us suggest
2022-02-16
Recent findings of us suggest that compounds that inhibit both FAAH and TRPV1 may be more efficacious in pain relief than those targeting only one such protein. As continuation of our efforts to identify new molecules able to target simultaneously both FAAH and TRPV1 receptors, we hypothesized that
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Interestingly evidence has emerged recently that suggests
2022-02-16
Interestingly, evidence has emerged recently that suggests noncanonical roles of EZH2 in various cancers. For example, in addition to histone H3, EZH2 has been shown to methylate non-histone substrates, such as Jarid2 and STAT3, to regulate their transcriptional activities (He et al., 2012, Sanulli
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Histamine H and H receptors
2022-02-16
Histamine H1 and H2 receptors are considered as low affinity receptors (pKi of 4.2 and 4.3 respectively), whereas histamine H3 and H4 receptors as a high affinity receptors (pKi of 8 and 8.2 respectively) (Schreeb et al., 2013). Therefore it might well be that other histamine receptors might be invo
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br Introduction Adenosine triphosphate ATP
2022-02-16
Introduction Adenosine-5′-triphosphate (ATP) is an organic molecule (nucleoside triphosphate) which consists of adenine, ribose, and three phosphoric AG014699 synthesis residues. ATP serves as a temporary carrier of energy in all living cells, so it is a common substance in any organism. In the
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HPgV coinfection has been associated with
2022-02-16
HPgV coinfection has been associated with reduced liver disease in HPgV/HCV/HIV triply infected patients (Barbosa Ade et al., 2009, Berzsenyi et al., 2007, Berzsenyi et al., 2009, Berzsenyi et al., 2011). It is possible that HCV NS3 protease inhibitors could inhibit HPgV replication diminishing its
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Glutathione in reduced form GSH the tripeptide glutamyl cyst
2022-02-15
Glutathione in reduced form (GSH, the tripeptide, γ-glutamyl cysteinyl glycine) is a non-enzymatic low-molecular-weight antioxidant necessary for the maintenance of a cellular redox state (Noctor et al., 2012). At the stage of the transition from germination to seedling growth the process of cell di
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In order to elucidate the mechanisms behind the observed cha
2022-02-15
In order to elucidate the mechanisms behind the observed changes in metabolic activity in the cardiomyoblasts we investigated changes in gene and protein expression subsequent to treatment with PSN632408 with or without concurrent exposure to palmitate. Activating GPR119 in basal and high palmitate
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br Animal models of NASH The human NAS system see
2022-02-15
Animal models of NASH The human NAS system (see above) is largely reproducible in NAFLD mouse models [37] and, therefore, has been increasingly applied in the preclinical assessment of liver histological responses to test compounds. In general, the NAS system is well suited for this purpose, alth
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However even if immunological tests with the
2022-02-15
However, even if immunological tests with the NQ21 peptide are mostly positive [8], it doesn't mean that the structure of the NQ21 peptide is the same as that of the corresponding gp120 region characterized by a long alpha helix. Therefore, the aim of the current work was to check whether the NQ21 p
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N6-Cyclopentyladenosine australia No compounds in this serie
2022-02-15
No compounds in this series showed any appreciable activity at GlyT2 and can thus be considered GlyT1-selective. For the GlyT2 IC was >20μM. To determine CNS penetration of -(2-(azepan-1-yl)-2-phenylethyl)-benzenesulfonamides, select compounds were evaluated in a cassette CNS exposure screen in mal
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