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G protein coupled receptor GPCR ligands
2021-12-17
G-protein-coupled receptor (GPCR) ligands can be classified as either orthosteric or allosteric modulators. Orthosteric and endogenous ligands bind to the same site, which is topologically distinct from the allosteric site. In general, the binding domains of different orthosteric ligands may not exa
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br Author contributions br Acknowledgements The work
2021-12-17
Author contributions Acknowledgements The work was financially supported by a grant from the Investigator-Initiated Studies Program (Ref. #38124) from Merck Sharp & Dohme, and, in part, from Research Grants Council of the Hong Kong Special Administrative Region, China (Ref. No.: 14110314), awa
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Another group of secreted proteins that determine the virule
2021-12-17
Another group of secreted proteins that determine the virulence of V. dahliae are effectors and microbe associated molecular patterns (MAMP) that regulate plant immunity [10]. So far, there is only one Camptothecin gene Ave1 cloned in V. dahliae, yet it does not exist in race 2 strains such as V592
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Variants of NEIL were also analysed in Primary
2021-12-17
Variants of NEIL1 were also analysed in Primary sclerosing cholangitis (PSC) and cholangiocarcinoma (CCA) patients by Forsbring et al. to identify effect of variants on these diseases. Four variants were identified i.e., one earlier validated (G83D) and three novel (E181K, H275, R339W). E181K was fo
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In contrast to UDG SMUG exhibits dramatically
2021-12-17
In contrast to UDG, SMUG1 exhibits dramatically lower product yield in its excision of U, and this is not dependent on sequence context. Though we cannot rule out that a small amount of the product is derived from a duplex contaminant, our extensive purification techniques limit the amount of contam
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In this present study the availability of
2021-12-17
In this present study, the availability of commercial GLUT and SGLT GSK461364 australia directed against different epitopes, enabled us to screen for members of the SGLT family and compare the expression patterns of GLUTs and SGLTs in the different regions of the rat lens. Based on these regional a
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The role of the ER EK variant which is
2021-12-17
The role of the ER22/23EK variant which is associated with relative resistance to GC, as shown by a reduction of transactivating capacity in vitro and less suppression of MK-8776 receptor levels after 1mg DST in vivo. Relative GC resistance associated with the ER22/23EK polymorphism might protect f
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Phylogenetic analysis of the secretin
2021-12-17
Phylogenetic analysis of the secretin-like hormones yields poorly supported trees due to the short length of their peptide sequences (Dores et al., 1996). However, phylogenetic analyses typically show that the secretin-like peptides encoded by the proglucagon (glucagon, GLP-1 and GLP-2) and GIP hpdp
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The chemical structure of BAs
2021-12-16
The chemical structure of BAs consists of a steroid nucleus with an acidic side chain. They are amphipatic molecules characterized by a hydrophilic α-face and a hydrophobic β-face. The hydrophobic pocket of the FXR LBD interacts with BAs largely through the β-face. The α-face contains several hydrox
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Although oxidative stress induces a decrease in
2021-12-16
Although oxidative stress induces a decrease in intracellular ATP level, the underlying mechanism is obscured. We hypothesized that oxidative stress induced by H2O2 could decrease astrocytes ATP level through lysosome exocytosis in Ca2+-dependent pattern. In present study, using H2O2 stimulation to
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An isoflavone type secondary metabolite
2021-12-16
An isoflavone type secondary metabolite, Glabrescione B (GlaB), from Derris glabrescens (Benth.) J.F. Macbr. from the family Fabaceae, was found to possess the capacity to bind the Gli1 zinc finger domain and to further block DNA binding capacity [118]. Pyrvinium, an anthelmintic drug approved by th
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Lastly haspin inhibitor was assessed against a panel
2021-12-16
Lastly, haspin inhibitor was assessed against a panel of 292 kinases at 10μM. At this high concentration, the BEC inhibited thirteen kinases, in addition to haspin, ⩾90%., These kinases were CaMK2b, CaMK2d, CDK7-CycH-Mat1, cGK2, CK1d, CLK1, CLK2, DYRK1A, DYRK1B, DYRK3, PASK, PIM1 and PKD3. Intere
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Introduction In the s nitric oxide
2021-12-16
Introduction In the 1980s, nitric oxide (NO) was first characterized as critical to both innate immunity and endogenous signaling in animals [[1], [2], [3], [4], [5]]. NO was the first gaseous signaling molecule synthesized by animals to have its biochemical signaling pathway fully described [2]. P
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Pyoluteorin synthesis br Conclusion The development discover
2021-12-16
Conclusion The development/discovery of compounds targeting small GTPases is challenging [43,44]. Our data point to RBC8 being efficient and potent as a Ral inhibitor in human and mouse platelets, but that it exhibits some activity beyond just Rals, particularly in mouse platelets. It is however
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br Mutagenesis and Receptor Modeling Studies br
2021-12-16
Mutagenesis and Receptor-Modeling Studies Signal Transduction and Receptor Desensitization Therapeutic Potential of HCA Receptor Ligands Although all members of the HCA receptor family are potentially interesting drug targets, only HCA2 is currently exploited as such. Therefore, this sectio
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