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Consistent with previous simulations on
2021-09-01

Consistent with previous simulations on the DFG-Asp-out/-in interconversion of Abl kinase, we only observe the DFG flip with protonated Asp747 (Shan et al., 2009). We showed previously that the pKa for the DFG-Asp in Abl is elevated at 6.5. Further “constant pH” simulations whereby protonation event
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br Materials and methods br Results and discussion In the
2021-09-01

Materials and methods Results and discussion In the present work, we have applied two methodologies, CoMFA and CoMSIA to build 3D-QSAR models. There is no crystal structure available; therefore, an indirect method i.e., a ligand-based approach is the method of choice. The highly active molecul
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In contrast to PEGylated proteins which tend to have reduced
2021-09-01

In contrast to PEGylated proteins which tend to have reduced SGI1776 synthesis in the body relative to their native counterparts, proteins conjugated to albumin tend to accumulate in certain locales in vivo. This means that albumin-based drug carrier systems have particular applications in the fiel
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To estimate the nonparametric regression we use a
2021-09-01

To estimate the nonparametric regression, we use a B-spline basis. Let be the space of polynomial splines of degree and denote a normalized B-spline basis with and , where is the supremum norm. For any and , we have for some coefficients . Here we allow to increase with and differ for differ
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The present study has shown
2021-09-01

The present study has shown that additional protein stability can be achieved (Fig. 6). The 0.6 to 1.0 °C increases that were observed were not large compared, for example, to the ∼5 °C increase that has been reported using sequence modifications [22]. This may reflect that the Hyp enters both the X
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br Acknowledgments br Casein kinases CK
2021-09-01

Acknowledgments Casein kinases (CK) are serine/threonine-specific enzymes and can be divided two subtypes: casein kinase 1 (CK1) and casein kinase 2 (CK2). CK1 contains at least seven isoforms (α, β, γ1, γ2, γ3, δ and ε) expressed in eukaryotic organisms, CK1 is involved in various cellular pro
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To develop antagonists selective for the mouse EP
2021-09-01

To develop antagonists selective for the mouse EP1 receptor, we started with compound (), synthesized as previously described (). Diethyl dipicolinic RVX-208 () was reduced with NaBH to . Parikh–Doering oxidation of with sulfur trioxide–pyridine complex and DMSO produced the unstable aldehyde . 4-C
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Apart from the ET system
2021-09-01

Apart from the ET system's role in regulating blood vessel tone, it is also involved in a variety of cellular processes that are relevant to DR. For example, the ET receptors influence the survival of retinal ganglion mk-801 (McGrady et al., 2017; Tonari et al., 2012), development of the retinal va
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The Rev protein is a crucial regulator of TLS
2021-09-01

The Rev1 protein is a crucial regulator of TLS activity because of its structural function [10]; therefore, we focused on Rev1 to investigate how Dot1/Rad53 function impinges on TLS-dependent mutagenic bypass of MMS-induced lesions. In particular, we examined Rev1 localization to chromatin by immuno
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According to our results germination of transgene dgks lines
2021-08-31

According to our results, germination of transgene dgks lines didn’t differ under optimal conditions and 50 mM NaCl, while 100 mM NaCl slightly affected germination rates of dgk mutants. Exogenous application of EBL even diminished the effect of 100 mM NaCl on dgk mutants. The critical effect on ger
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Besides by substrate and product KSTDs may
2021-08-31

Besides by substrate and product, Δ1-KSTDs may also be inhibited by other steroids. N. simplex ATCC 6946 Δ1-KSTD was strongly inhibited non-competitively by dicortinone (60), a steroidal dimer, and by bis-1-dehydrodicortinone, with values of 0.7 and 0.75 μM, respectively. This enzyme was also inhib
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IL is not expressed in tissues constitutively because of its
2021-08-31

IL-8 is not expressed in tissues constitutively because of its strong chemoattractant, proinflammatory, and angiogenic activities. Rather, it is an inducible factor, produced by a variety of cell types, including leukocytes, fibroblasts, endothelial and epithelial cells, in response to proinflammato
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Previously the N glycan in V of
2021-08-31

Previously, the N-glycan in V3 of HXB2, HXB10, LAI and BRU strains was reported to be dispensable for their infectivity to T cell lines, although detailed growth kinetics and experimental conditions were not described 4, 5, 6, 7, 8. The experiments appear to have been done by infection initiated wit
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Considering the protumoral functions of TAMs
2021-08-31

Considering the protumoral functions of TAMs, new therapies against TAMs have recently gained interest. Such treatments, particularly inhibitors of the colony stimulating factor 1 receptor (CSF-1R), are currently evaluated in several clinical trials [19]. CSF-1R inhibitors may also be of interest i
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Though limited to a large cohort
2021-08-31

Though limited to a large cohort of self-reported healthy individuals, associations between individual mglur have been identified which may be clinically significant. Though slight, there is a relationship between the CYP2D6-inferred metabolizer phenotype and the diplotype-predicted activities of U
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