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We have compared the potency of a
2020-02-25
We have compared the potency of a series of DNA-directed alkylating agents, including N-mustard-acridine, N-mustard-quinoline, and N-mustard-quinazoline conjugates previously synthesized in our laboratory [7], [13], and currently used drugs (oxaliplatin, cisplatin, or 5-FU) for the treatment of CRC
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AZD-5438 synthesis Cryptosporidium is a protist causing seri
2020-02-25
Cryptosporidium is a protist causing serious diarrhea in humans and other animals (Bouzid et al. 2013). In its mitosomes, the most reduced forms of mitochondria, it is assumed that the membrane potential is generated by a simple respiratory chain consisting of transhydrogenase, type II NADH dehydrog
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The roles of ginsenoside in E and S
2020-02-24
The roles of ginsenoside in E1 and 26S proteasome inhibition are shown in Table 2. The nitro substitute on the furan ring may be important for PYR-41 inhibition of the E1 enzyme (Yang et al., 2007). The macrocycle core and aliphatic tail of Largazole are responsible for inhibiting E1 activity (Unger
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br Methods br Results br Discussion Preclinical
2020-02-24
Methods Results Discussion Preclinical data indicate that nepicastat modulates sympathetic drive to the Tasquinimod sale with a mild pressor effect in various animal models of hypertension (Stanney et al., 1998). However in this clinical study, the doses of nepicastat employed did not sign
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br Experimental br Results and
2020-02-24
Experimental Results and discussion Conclusions The fungus Mucor circinelloides MUT44, previously shown to have ene-reductase activity [11], possesses ten genes coding for putative ene-reductases belonging to the Old Yellow Enzymes family. Since the reduction of CC double bonds is one of th
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Some authors rather than using magnetic NPs as
2020-02-24
Some authors, rather than using magnetic NPs as heat sources, have enhanced the activity of the linked enzymes by applying low frequency AMF. Magnetic energy is converted into a rotational motion of the enzyme-particle system that increase the collision rate with the substrate [14], [15], or trigger
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To predict levels of SCF assembly Liu et al
2020-02-24
To predict levels of SCF assembly, Liu et al. (2018) first quantified the remaining necessary kinetic parameters and derived a model in combination with known functions and concentrations of components. The model agrees astonishingly well with many experimental observables. In terms of SCF assembly,
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br Results br Discussion Many assays in the
2020-02-24
Results Discussion Many assays in the literature for DBH require the use of catalase to protect the active site from hydrogen peroxide, which is a by-product in the initial step of the reaction. For the non-immobilized enzyme there was a visible increase in the rate with increasing amounts of
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glatiramer acetate mg br Fragment based drug discovery FBDD
2020-02-24
Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical glatiramer acetate mg space with libraries which are smaller in size, producing drug leads with high ligand-binding effi
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In the present study we combined activity based protein
2020-02-24
In the present study, we combined activity-based protein profiling, biochemical and genetic approaches to identify the PLCPs involved in the sphingolipid pathway leading to plant PCD. By using Arabidopsis CC-223 australia and leaves, we demonstrate that this sub-class of plant proteases is activate
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Increased knowledge about CRC pathogenesis has provided new
2020-02-24
Increased knowledge about CRC pathogenesis has provided new and remarkable treatments beyond the classical options of surgery, radiation and chemotherapy [11]. Despite these advances, chemotherapy remains the most important element of anti-cancer therapy. Chemotherapy, when initiated, is generally e
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In a recent study a CMV
2020-02-24
In a recent study, a CMV DNA load cut-off of 500 IU/ml in BAL fluid was found to have a positive predictive value of ∼50% for the presence of probable CMV pneumonia (considering a prevalence of this event of 10% among patients at risk and undergoing BAL testing). Tan et al., in contrast, found CMV D
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The binding pattern of was analysed by flexible molecular do
2020-02-24
The binding pattern of 1 was analysed by flexible molecular docking. The NS 1738 inserted into the narrow ATP binding site of CK2 (Fig. 2). As shown the aliphatic chain of 1 was located at the edge of the pocket and established van der Waals interactions with the side chains residues of Ile95, Met1
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To develop novel EPAC inhibitors Zhou and
2020-02-24
To develop novel EPAC inhibitors, Zhou and co-workers optimized the HTS hit as the chemical lead. After modifications of the substituents on the phenyl ring or C6-position of compound , compound () was identified to be the more potent compound in this series with an IC value of 4.0µM (EPAC2). Dock
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br Conclusions br Acknowledgements Implantable Microsystems
2020-02-22
Conclusions Acknowledgements Implantable Microsystems for Personalised Anti-Cancer Therapy is a EPSRC (Engineering and Physical Sciences Research Council, UK) funded grant (Ref. EP/K034510/1) Introduction Flemingia philippinensis, belonging to the legume family, is a polyphenol rich plant
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