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The objective of this study is to design and synthesize
2021-10-27

The objective of this study is to design and synthesize drug-like molecules with agonistic activity on both receptors; PPARγ and FFAR1. These agents would act as insulin sensitizers and insulin secretagogues through their action on PPARγ and FFAR1, respectively. The design of drugs with dual mode of
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We characterized the enzyme corresponding to N FPP was
2021-10-27

We characterized the enzyme corresponding to N1. FPP was the most effective substrate as allylic diphosphate, and the activities with GPP and DMAPP were 50% and 11% that with FPP, respectively. The analysis of the prenols resulting from the treatment of prenyl diphosphates with 11e phosphatase () r
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The exocytosis promotion is triggered upon the binding of Ca
2021-10-27

The ivosidenib receptor promotion is triggered upon the binding of Ca2+ to the C2 domains of two key protein groups, i.e. complexin and certain synaptogamins (Lai et al., 2017; Rizo and Xu, 2015). The first step of the vesicle fusion is the priming of the secretory vesicles, involved at the switchi
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br Discussion In our study the
2021-10-27

Discussion In our study the prevalence of severe periodontitis in patients with HIV infection was 66%, almost twice as high as in uninfected controls. Our results are in line with the prevalence of severe periodontitis found in HIV-infected patients in London, United Kingdom in the pre-cART era:
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br To explore further the functional impact of the similarit
2021-10-27

To explore further the functional impact of the similarity of the UTY and KDM6A proteins, the FANTOM5 human dataset was analysed to determine whether or not the genes were expressed at the same time in the same tissues (which would suggest that they are controlled by the same regulators) or with o
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Here we report the kinetics
2021-10-27

Here, we report the kinetics of inhibition of the MYST HAT family member KAT8 by MG149, and a calculation of the inhibitory constant Ki of MG149 for KAT8. The inhibition of HATs by MG149 could be correlated to inhibition of histone acetylation in murine PCLS upon MG149 treatment, as determined by a
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Maillard reaction also known as
2021-10-27

Maillard reaction, also known as non-enzymatic browning reaction, is a complex chemical reaction between carbonyl groups of reducing sugars and free amino groups of amino acids, peptides, proteins or some other nitrogen containing compounds. Maillard reaction plays an important role in food industry
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br Histamine and glycaemia Histamine is involved in a wide
2021-10-27

Histamine and glycaemia Histamine is involved in a wide variety of pathophysiological events mostly related to the inflammatory response through four receptors, namely H1-4Rs. The first studies of Pravastatin sodium and diabetes date back to the 1950s. Since that time the involvement of histamine
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br General aspects of HDACs br General aspects of HDAC
2021-10-26

General aspects of HDACs General aspects of HDAC inhibitors Based on the previous elements, inhibitors designed for HDAC have in common a well-admitted pharmacophore model (Fig. 7A). This model is composed of a zinc binding group (ZBG), attached to a linker chain mimicking the lysine side chai
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Furthermore we observed a striking difference
2021-10-26

Furthermore, we observed a striking difference between BR 11257 and activators from the dicarboxylic Azaperone type in thermofluor measurements on thermostability. The dicarboxylic acids cinaciguat [30] and BAY 60-2770 (see Fig. 3) induced a significant melting temperature increase of sGC. In combi
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br Experimental br Results and discussion
2021-10-26

Experimental Results and discussion Conclusion In the current work, a novel method for separation and preparation of flavonoid glycosides from L. chinensis was successfully developed using a 2 D-HILIC × RPLC system based on a zwitterionic Click XIon column and a polar-modified Atlantis T3 c
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Alpha synuclein AS is a protein located
2021-10-26

Alpha synuclein (AS) is a protein located in presynaptic terminals of neurons that functions in recycling and storage of neurotransmitters [17]. Under conditions of inflammation and oxidative stress, AS proteins misfold and accumulate into ap4 [81], [90]. The aggregates of misfolded AS oligimorize
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GlyRs are members of the superfamily of Cys loop
2021-10-26

GlyRs are members of the superfamily of Cys-loop receptors (CLRs) [3]. They form postsynaptic pentameric receptor complexes of α1 and β subunits anchored via the scaffolding protein gephyrin [4]. GlyRs are composed of several domains with the large N-terminal extracellular domain (ECD) important for
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The simple carrier model for GLUT transport activity
2021-10-26

The simple carrier model for GLUT1 transport activity proposes that the transporter alternates between an outward facing glucose binding site and an inward, cytoplasmic, facing glucose binding site. Cytochalasin B is an endofacial inhibitor and appears to preferentially bind to the open, inward faci
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Studies regarding secretase nowadays aim at elucidating how
2021-10-26

Studies regarding γ-secretase nowadays aim at elucidating how APP is recognized and recruited. It has been suggested based on coarse-grained molecular simulation that the recognition and recruitment of substrate can occur on an extended surface covering PS1's TM2/6/9 domains and PAL motif [15]. Tran
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