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br Substrate characterization of candidate peptide reporters
2020-03-26
Substrate characterization of candidate peptide reporters in a library Measurement of resistance to intracellular proteases Use of capillary zone electrophoresis for assay readout Selection of lead peptide from small library screen Characterization of final reporter Additional modif
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SAR405 DDR is one of two
2020-03-26
DDR1 is one of two, non-integrin tyrosine kinase receptors activated by collagen. Although DDR1 has five isoforms (1a, 1b, 1c, 1d, 1e) generated by alternative splicing, only DDR1a and 1b have active kinase domains, whereas DDR2, encoded by a distinct gene, has one isoform (Vogel et al., 2006). Coll
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Our knowledge of DDR induced signaling pathways
2020-03-26
Our knowledge of DDR-induced signaling pathways is still fragmentary. In particular, we do not know which signaling effectors interact with the phosphorylated receptors and how different effectors are linked to the control of specific cellular functions. The DDRs are at the interface between RTKs an
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High throughput screening HTS of
2020-03-26
High throughput screening (HTS) of the AstraZeneca G-15 australia collection was conducted and identified oxadiazole amide () originating from a kinase directed screening library (although inactive against a panel of kinases). This compound had moderate potency as a DGAT-1 inhibitor (IC=0.52μM) and
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Not all of the biological activities exhibited by
2020-03-26
Not all of the biological activities exhibited by progestogens (Table 1) are mediated via binding to SRs. For example, the anti-estrogenic action of progestogens in the 3787 sale is due to the progestogen-bound PR suppressing ER gene expression, and consequently the ability of the cell to respond to
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Recently roflumilast has been approved as the first selectiv
2020-03-26
Recently, roflumilast has been approved as the first selective PDE4 inhibitor for the treatment of chronic obstructive pulmonary disease (COPD) [2]. Roflumilast has been suggested to target several different pathogenetic mechanisms, including inflammation, fibrotic, emphysematous and vascular remode
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Here we were able to show for the
2020-03-25
Here, we were able to show for the first time that stimulation of VSMCs with two different growth factors resulted in a dramatic decrease in gp130mRNA expression occurring four to six hours after stimulation with Ang II and PDGF-BB. The mRNA level remained extremely low within 12 hours after stimula
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Stressful life events are modulators of
2020-03-25
Stressful life events are modulators of mood and can trigger a variety of destructive behavior, including drug abuse and relapse in addicts (Association, 2013; Chen et al., 2012; Sinha, 2009). Likewise, drug-associated stimuli evoke a negative affective state in abstinent drug users. Compelling evid
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Materials and methods br Results br Discussion
2020-03-25
Materials and methods Results Discussion Hydroxylation of proline in bacterial amprolium is one of the oxygen-requiring metabolic reactions, which needs efficient oxygen. Oxygen supply is always a rate-limiting step for tyrosinase production even though pure oxygen is purged in a bioreactor
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Cholesterol Moreover as shown in Fig f while the
2020-03-25
Moreover, as shown in Fig. 5f, while the knockdown of SMURF2 in wild-type Cholesterol has no significant effect on HSP27, in CK2α/α′(−/−) cells it leads to an increase of HSP27 level. These results suggest that SMURF2 affects HSP27 protein stability only when overexpressed, at least in our cell mod
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The ACC receptor family appear to be attractive
2020-03-25
The ACC receptor family appear to be attractive targets for the development of novel anthelmintics. With this in mind we also tested the activity of the anthelmintics levamisole and pyrantel which activate the nematode nAChR (Martin and Robertson, 2007). We found both molecules were partial agonists
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Functional studies revealed that these ESR
2020-03-25
Functional studies revealed that these ESR1 mutations lead to constitutive activity of the ER, meaning that the receptor is active in absence of estrogen, conferring resistance against several endocrine agents. Recent studies reported that the occurrence of ESR1 mutations is rare in ER+ primary brea
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fty Even minor alterations in the surfactants
2020-03-25
Even minor alterations in the surfactants structure could have consequences on their physico-chemical characteristics; mono-RLs have less solubility, stronger surfaces sorb, and stronger cationic metals binding than homologue di-RLs (Zhang et al., 1997). The HPLC separation of RLs structure is base
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The objective of the present work is to
2020-03-25
The objective of the present work is to search for the optimum blend when 12.5–50% metakaolin is substituted by RHA and reacted with 10 M sodium hydroxide solution to produce geopolymers. It was hypothesized that the amorphous Meropenem from RHA will increase the Si/Al ratio of the mix and in situ r
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It is known that cigarette
2020-03-25
It is known that cigarette smoke increases the oxidative burden in the lungs of mice with emphysema, which leads to oxidative stress [[34], [35], [36]]. However, in addition to cigarette smoke, studies have shown that endogenous oxidative stress is associated with proteolytic Cy3 NHS ester (non-sulf
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