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A An optimized BEI SEIscore based on the
2020-12-01
(A) An “optimized BEI-SEIscore” based on the trends, emerged from the statistical analysis of several optimization studies in pharmaceutical industry (Abad-Zapatero, 2007, Abad-Zapatero and Blasi, 2011). This type of optimized scores has been used in many previous studies. Ki=1nM at 300° K, compare
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br Cysteine proteases as molecular targets for
2020-12-01
Cysteine proteases as molecular targets for trypanosomatid diseases Approaches relying on a molecular target, such as SBDD and target-based screening, have supported outstanding scientific developments in current pharmaceutical R&D. By integrating experimental and computational methods, these str
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One strategy which is different from the above is to
2020-12-01
One strategy which is different from the above is to isolate a similar enzyme to the one under study which will not be recognized by the antibody of the original protein. This approach will lead to prolonging an enzyme’s activity. For example, a novel variant of Carboxypeptidase G2 (CPG2), which has
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The COMT gene maps to
2020-12-01
The COMT gene maps to chromosome 22q11.2 (Grossman et al., 1992) and has two protein isoforms. The differences between S-COMT and longer MB-COMT are in the N-termini, which use alternative translation initiation sites and promoters. These two isoforms display different affinity and capacity for COMT
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Phenylbenzofurans are a very important molecule skeleton due
2020-12-01
Phenylbenzofurans are a very important molecule skeleton due to their synthetic versatility and their proved pharmacological properties [2]. They are synthetic compounds in which an additional phenyl ring is present in any position of the benzofuran nucleus. This could be easily obtained possible by
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Although it is well established that
2020-11-30
Although it is well established that estrogen and ESR1 mediate numerous reproductive processes, increasing evidence suggests that ESR2 also lays an integral role in reproduction. ESR2 is a mediator in folliculogenesis and may also act by stimulating ovulation and regulating luteinization (Su et al.,
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MoAbs targeting the tumourigenic pathways such as
2020-11-30
MoAbs targeting the tumourigenic pathways, such as IGF-1R may theoretically have a dual working mechanism. On the one hand they block pathways having an anti-tumour working mechanism, and on the other hand they may also stimulate an immunological response inducing a reaction of the patients own immu
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br Early developments Historically the advent
2020-11-30
Early developments Historically, the advent of SMEPT can be traced to the 1980′s, where the first example of localized prodrug conversion was achieved using a judiciously placed enzyme – in order to achieve a localized feed of 5-fluorouracil (5-FU). Immobilization of E. coli-derived cytosine deam
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Enhanced responses to varying concentrations of bronchoconst
2020-11-30
Enhanced responses to varying concentrations of bronchoconstrictors, such as MCh, and airway obstruction are characteristic of Sulforaphane and common to other clinical states, including chronic obstructive pulmonary disease, lung transplantation, and infection- or chemical agent-induced airway infl
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Methods br Results br Discussion In this study we
2020-11-30
Methods Results Discussion In this study we make the novel observation that villin-1 and gelsolin are down-regulated in response to diverse cellular stressors, including bacteria associated with the pathogenesis of CD. The high plasticity and dynamics of the Illumina 384 cytoskeleton are exp
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Even more unambiguous was the relative contribution of
2020-11-30
Even more unambiguous was the relative contribution of Gq/11 signaling in AngII-mediated transactivation as measured by the ERK1/2 and the BRET-based readout. Although Gq/11 was absolutely required for ERK1/2 phosphorylation following AngII-stimulation, in contrast, we observed a sustained EGFR-Grb2
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One of the most fundamental distinctions between Ub signals
2020-11-28
One of the most fundamental distinctions between Ub signals is substrate monoubiquitination versus polyubiquitination. With the exception of the E2, UBE2W, which represents a special case because it Propranolol HCl only ubiquitinates the flexible N-termini of substrates [5], [6], [20], most example
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br Conclusion From the series of
2020-11-28
Conclusion From the series of synthesized N-methylated and N-benzylated pyrimidinediones, it may be concluded that the presence of electron rich species with pyrimidinediones is vital for enhancing binding with target, although, incorporation of steric bulky group must be taken into consideration
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The thermal behavior of the UV sensitive nanocomposites was
2020-11-28
The thermal behavior of the UV-sensitive nanocomposites was investigated by DSC before and after irradiation in an extended temperature range (from −40 to 250 °C). Fig. 4a shows the thermograms of the non-irradiated GNP-DNA/PDMS nanocomposites in comparison with a neat PDMS sample. The filler-loaded
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br Introduction Malaria remains a
2020-11-28
Introduction Malaria remains a serious parasitic disease in tropical areas due to its high morbidity and mortality rates. It is estimated that 212 million cases occurred globally in 2015, leading to 429, 000 deaths, most of which were in children aged under 5 years in Africa [1,2]. The protozoans
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