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In three groups independently proposed two different mechani
2022-03-28

In 2001, three groups independently proposed two different mechanisms for the catalytic reaction of GlxI [5], [6], [7]. Richter and Krauss (RK) used HF/4–31G calculations of the active site, coupled with a frozen effective fragment potential description [8], [9] of eleven residues in the binding sit
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For several parasites of veterinary
2022-03-28

For several parasites of veterinary importance, there is a growing body of evidence that resistance to ML is, at least in part, mediated by ABC transporters (P-glycoproteins) (Whittaker et al., 2017). P-glycoproteins (Pgps) are members of the ATP-binding cassette transporter family that are well kno
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Indeed it was shown further in VSV G that
2022-03-28

Indeed, it was shown further in VSV G that the H80A mutation, and the E123L and D121L double mutation, which both abolish VSV G fusion properties, were rescued by the same compensatory Q112P mutation. In a single FD, residue 112 is located on the opposite side of the three-stranded β-sheet and is fa
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br Acknowledgement We like to thank the Austrian Federal Min
2022-03-26

Acknowledgement We like to thank the Austrian Federal Ministry of Science, Research and Economy for financial support (GZ402.000/00014-WF/V/6/2016 within the Sino-Austria project) as well as Andrea Szabo and Patricia Haiss for support regarding the drawing of figures and tables. Farnesoid X Re
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In the phylum Cnidaria which separated from the main
2022-03-26

In the phylum Cnidaria, which separated from the main line of Metazoa early during evolution, FGFR signaling is essential during development and morphogenesis. Two FGFRs and two FGFs antagonistically control formation of the apical organ in the anthozoan Nematostella and target the MAPK pathway (Ren
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FGF signals can be transduced to the
2022-03-26

FGF signals can be transduced to the signaling cascades of RAS-MAPK or PI3K-AKT through FRS2 and GRB2, to the pathways of PKC or PKD via PLCγ and DAG, and to Ca2+-releasing cascade via PLCγ and IP3, finally affecting cellular proliferation, cellular survival, and angiogenesis [48]. By increasing sy
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A new series of pyrimidones with C
2022-03-26

A new series of pyrimidones (14) with C-7 and C-9 modifications were furnished consisting of a hydroxypyridinone and a thiazole ring and checked against raltegravir resistant HIV mutant strains to determine their in vitro anti-HIV IN potency. Compounds 14a–14a, 14b–14b and 14c–14c appeared with 6.4
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One class of microbial derived metabolites that have
2022-03-26

One class of microbial-derived metabolites that have received significant attention are the short-chain fatty acids (SCFA), which include butyrate, acetate and propionate. The production of SCFA occurs in the colon following microbial fermentation of dietary fibers and SCFA can also be consumed in c
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ANT located in the IMM mediates
2022-03-26

ANT, located in the IMM, mediates the exchange of ATP/ADP between the mitochondrial matrix and the intermembrane space (IMS) (Brand et al., 2005; Palmieri and Pierri, 2010). Of the 4 known isoforms, ANT1 is the dominant isoform in the heart (Palmieri and Pierri, 2010). Under physiological conditions
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For the SAR study human haspin kinase inhibitory activity of
2022-03-26

For the SAR study, human haspin kinase inhibitory activity of the various compounds was evaluated using the same assay utilized for the HTS, except in the presence of varying test compound concentrations. DYRK2 kinase inhibitory activity was measured by P-incorporation into Woodtide peptide substrat
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It was revealed that various injured or
2022-03-26

It was revealed that various injured or infected organs of Hippeastrum produce a mixture of an orange-colored chalcone and flavans which can be oxidized to red-colored dimer (Wilmowicz et al., 2014, Wink and Lehmann, 1996), preventing the penetration of injured tissues by Phoma narcissi, Botrytis ci
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With this goal in mind we proceeded to
2022-03-25

With this goal in mind, we proceeded to explore the C5-heteroaryl class of pyrazole-acids. Initial efforts, focused on a thiophene replacement, demonstrated little improvement. The 2-thiophene derivative (0.25μM and 0.24μM), a surrogate to the phenyl moiety, demonstrated only a modest boost in acti
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Always some extra effort may
2022-03-25

Always, some extra effort may make great progress in sensing platform, for example, Ma's group discovered luminescent iridium (Ⅲ) complexes which were highly selective for G-quadruplex DNA and Al3+, then they utilized these complexes to develop a series of G-quadruplex-based probes and chemosensor r
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Initial studies generally focused on
2022-03-25

Initial studies generally focused on the co-administration of glutamate with transport inhibitors and clearly revealed the ability of the blockers to exacerbate excitotoxic injury in both in vitro and in vivo models (McBean & Roberts, 1985, Robinson et al., 1993a). In addition to demonstrating the c
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br Introduction Opioids have long been used in
2022-03-25

Introduction Opioids have long been used in pain management [1]. However, their non-medical use has grown rapidly in the last few years. Hydrocodone (HYD) is one of the most widely used short-acting opioids; with over 136.7 million prescriptions in 2011 [2]. HYD is a semi-synthetic opioid used fo
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