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Repulsive interactions towards undesirable substrates are ar
2020-10-26
Repulsive interactions towards undesirable substrates are arguably a very efficient means to implement specificity [8]. In particular, it could be assumed that discrimination against a substrate that is larger than the cognate substrate may be achieved easily by restricting the active site and explo
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It is also critical that APC CCDC is inhibited
2020-10-26
It is also critical that APC/CCDC20 is inhibited by MCC during the spindle assembly checkpoint, prior to correct chromosome alignment on the mitotic spindle (Box 1, reviewed in 13, 34). As proposed in [13] and demonstrated in [82], human MCC is a heterotetrameric complex consisting of its own molecu
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Structural homology modelling Intensive Phyre modelling was
2020-10-26
Structural homology modelling. Intensive Phyre2 modelling [44] was performed using the primary amino nmda receptor antagonist sequence of A1S_0222 as input to generate an atomistic 3D-homology model of A1S_0222. The fit to the SAXS data of the homology model as well as the fit to the data of the E.
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br Inhibition of DHODH The final products a
2020-10-26
Inhibition of DHODH The final products 7a–n were assessed for their DHODH inhibitory activity on rat liver mitochondrial/microsomal membranes. A procedure adapted from the literature was employed (see Experimental), in which oxidation of DHO to ORO is monitored by following the concomitant reduct
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dna ligase An AmDH is engineered by mutating two conserved a
2020-10-26
An AmDH is engineered by mutating two conserved amino dna ligase residues in the active site of an amino acid dehydrogenase (AADH). Starting from the leucine dehydrogenase (LeuDH) from Bacillus stearothermophilus, substituting a serine and leucine at the K68 and N261 positions, respectively, result
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diacylglycerol kinase It was demonstrated that the addition
2020-10-26
It was demonstrated that the addition of 10-fold excess of α-synuclein without modifications (with respect to the molar concentration of tetrameric GAPDH) leads to partial inactivation of GAPDH after 1-h incubation by 20% (Fig. 4, curve 2) in diacylglycerol kinase to insignificant decrease of the s
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Our previous studies have demonstrated that
2020-10-26
Our previous studies have demonstrated that the DDR2 discoidin domain fully contains the binding site(s) for the fibrillar collagens I and II (Leitinger, 2003, Leitinger et al., 2004). The binding site for collagen I was mapped to three spatially adjacent surface loops within the DDR2 discoidin doma
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br Concluding Remarks Synthetic cytokine biology has become
2020-10-26
Concluding Remarks Synthetic cytokine biology has become an important research area with novel solutions and ideas for therapeutic approaches, for example, synthekines, fusokines, immunocytokines, neoleukins, MESA receptors, or synthetic Notch or cytokine receptors. In addition to their huge impa
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Compound was generated using a literature procedure and
2020-10-26
Compound was generated using a literature procedure and required two-step Dess–Martin-periodinane/Pinnick oxidation prior to the methylation of the sulfonamide. Compound () was obtained from the Suzuki coupling of the methyl ester intermediate (en route to ym express synthesis ). Hydrolysis of a
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The synthesis of tricyclic analogs is described in Scheme
2020-10-26
The synthesis of tricyclic analogs 28–33 is described in Scheme 3. Oxidative C–C bond cleavage of the terminal olefin of 39i afforded a tricyclic product 52 without isolation of an aldehyde expected as an intermediate. Aminolysis of the chloride 52 with optionally substituted anilines afforded 28–30
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(R)-baclofen Allele specific methylation has been
2020-10-26
Allele-specific methylation has been observed in CpG islands of imprinted genes.27, 32 In the present study, however, methylation of CpG1 was specific to ALL (R)-baclofen and occurred in the leukemia cells of 28% of children with ALL, but it was not found in normal leukocytes from the same patients
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br Related work Goal of this
2020-10-26
Related work Goal of this section is to show related work focused on methods useful to assess the reliability of clustered COTS-based systems. Connelly et al. [1] propose an approach to delineate safety assurance for the use of COTS OS in safety-related applications, which must fall in SIL2. The
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br Acknowledgments br Introduction Cholesterol is
2020-10-26
Acknowledgments Introduction Cholesterol is an essential lipid for the development, growth, and wellbeing of humans. In newborn children, cord blood cholesterol concentration is 1.5 mmol/l, on average [[1], [2], [3], [4]]. During the first year of life, cholesterol concentration in serum incre
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Another potential source of variable
2020-10-26
Another potential source of variable affinities is inherent in the method of RBA determination. While several reports simply use relative IC50 values as RBAs [11], [12], [13], [14], [15], these are only an approximate measure of relative affinity since IC50 varies due to experimental and biological
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Although the presence of calcium in RHA P active site
2020-10-23
Although the presence of calcium in RHA-P active site is confirmed by the homology modeling, some additional observations can be made following the metal depletion and reconstitution experiments performed on RHA-Phis. EDTA-treated RHA-Phis recovers its activity in the presence of divalent cations su
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