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oxytocin receptor Enzyme mimics belong to a type of rising c
2020-06-20
Enzyme mimics belong to a type of rising catalysts which show the similar function with their corresponding natural enzymes [20], [21], [22], [23], [24], [25], [26], [27], although their structures are different from natural enzymes. In the area of prodrug activation, the widely-used enzyme mimics a
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In light of the overall loss of activity and
2020-06-20
In light of the overall loss of activity and selectivity observed with this series of arylchromenone-4-ones bearing small -alkoxy substituents, we were pleased to identify a potent and relatively selective inhibitor , exhibiting IC values of 0.008μM and 0.07μM for DNA-PK and PI3Kα, respectively. The
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As the angular structure of compound cannot be
2020-06-20
As the angular structure of compound cannot be differentiated from the linear structure by H NMR spectroscopy, a NOESY NMR experiment was performed to unambiguously characterize the regioselectivity of the final compound. In the linear compound , a signature correlation between the proton of the t
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br Materials and methods br Acknowledgments br Introduction
2020-06-20
Materials and methods Acknowledgments Introduction Proton pumps convert the energy of high-energy compounds into the Desfuroylceftiofur of protons across biomembranes. They play two physiological roles: pH regulation and the formation of proton-motive forces in their membranes. The simplest
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Determination of relative potency EC by dose response assays
2020-06-19
Determination of relative potency (EC50) by dose response assays in vitro is subject to the same sources of variability as determination of affinity, since the EC50 and Hill slope of the dose response curve are highly dependent on the binding of ligand to a competing receptor that may be present, an
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In Fig results of this experiment are shown as the
2020-06-19
In Fig. 1 results of this experiment are shown as the contour plots of endopeptidase activity. Optimal for the enzyme production by this strain concentrations of peptone and inorganic phosphate were found to be 24 and 0.3g/l, respectively. For specific activity, the optima close to those for glutamy
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Our previous work has demonstrated that two glutamate residu
2020-06-19
Our previous work has demonstrated that two glutamate residues (Glu-305 and Glu-331 in murine and human TPP II) in the active site are important for exopeptidase activity in mTPP II [17]. At least one of these, Glu-331, seems to form a salt bridge to the N-terminal amino group of the substrate, posi
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The photocleaving properties of were
2020-06-19
The photocleaving properties of 1 were studied by performing ΦX174 photocleavage assays. Light irradiation of the mixtures of increasing amounts of 1 with supercoiled DNA caused>90% supercoiled form relaxation and approximately 5% of linearization for the higher concentrations of 1 (1:10bp and 1:2bp
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Since the initial identification of DNA
2020-06-19
Since the initial identification of DNA ligase inhibitors by a structure-based approach [[18], [26]], there have been several reports describing LigI inhibitors using computer modelling and derivatives of the original DNA ligase inhibitors [[49], [50], [51]]. While these studies have shown that the
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In this study we have developed and investigated three NADPH
2020-06-19
In this study we have developed and investigated three NADPH-regenerating fusion partners with two different enzyme systems: a BVMO and an ADH. With the exception of one fusion construct (StGDH with LbADH), all fusion Imiquimod resulted in good soluble expression as well as fully functional as self
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Recently we have observed that
2020-06-19
Recently, we have observed that pharmacological PPARα and PPARβ/δ activation regulates the expression of genes involved in FA metabolism such as FAT/CD36, CPT1, LCAD and MCAD in Sertoli cells. We have also observed that PPARβ/δ activation can simultaneously regulate the expression of the above-menti
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Introduction The carnitine choline acyltransferase family is
2020-06-19
Introduction The carnitine/choline acyltransferase family is a family of enzymes that play diverse roles, ranging from (the regulation of) Albendazole and fuel metabolism in mitochondria and peroxisomes to the generation of the neurotransmitter acetylcholine. In mammals, this family consists of se
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The previously described endogenous patterns of IGF induced
2020-06-19
The previously described endogenous patterns of IGF-1-induced kinase signaling, and resulting interaction between MAPK and PI3K, differ across neuronal sub-types. In R28 retinal neuron-like cells, IGF-1 treatment elicits prolonged activation (at least 80 min) of both PI3K and MAPK (Kong et al., 2016
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br Advantages of modified proteins over unmodified ones In
2020-06-18
Advantages of modified proteins over unmodified ones In contrast to small-molecule drugs, proteins are readily amenable to site-specific alterations through genetic engineering. In principle, therefore, it is possible to build in features that allow them to remain active for longer in the body an
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Constitutive activity of Ras Raf MEK ERK
2020-06-18
Constitutive activity of Ras/Raf/MEK/ERK pathway plays a critical role on melanoma growth, thus inhibition of activity of Ras, Raf and MEK can reduce ERK activity, leading to a decrease in melanoma cell proliferation, survival and invasion (Burotto et al., 2014; Paluncic et al., 2016). Our results a
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