• br Materials and methods br Results Artemis

  2020-06-09

  

  Materials and methods Results Artemis has been reported to possess 5′–3′ exonuclease activity in vitro on ssDNA, as well as DNA-PK-dependent endonuclease activity on single-strand overhang and hairpin DNA structures [11]. However, enzymes within the metallo-β-lactamase family typically contain

• Since the initial identification of DNA ligase inhibitors by

  2020-06-09

  

  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

• Regarding eicosanoid production iPLA VIA appears

  2020-06-09

  

  Regarding eicosanoid production, iPLA2-VIA appears, in general terms, not to play a major role in mediating this response in innate immunity and inflammation, as evidenced by the large number of studies highlighting the lack of effect of selective inhibition of the enzyme in stimulus-induced AA rele

• The discoidin domain receptors DDR and DDR are receptor tyro

  2020-06-09

  

  The discoidin domain receptors, DDR1 and DDR2, are receptor tyrosine kinases (RTKs) that are stimulated by collagen in the extracellular matrix (ECM). Unlike most other RTKs, they form ligand-independent stable dimers that are non-covalently linked. This ECM activation induces receptor phosphorylati

• We can think of two ways in which

  2020-06-09

  

  We can think of two ways in which collagen binding could activate DDR (Figure 8). A single collagen triple helix could interact with both DS domains in the DDR dimer (“composite binding site”) and thereby activate the receptor, similar to the situation exemplified by the growth hormone-growth hormon

• br Rationale and hypothesis To discover an allosteric inhibi

  2020-06-09

  

  Rationale and hypothesis To discover an allosteric inhibitor of EGFR, Jia et al. (2016) screened a library of 2.5 million compounds at 1 μM ATP concentration in opposition the purified EGFR L858R/T790M mutant enzyme. 1322 best hits were found from this round of screening. The pinnacle hits had be

• The ADME profile of AAT was very promising with

  2020-06-09

  

  The ADME profile of AAT-008 () was very promising, with high stability in HLM. The pre-clinical pharmacokinetic properties of AAT-008 were also assessed in rats (Sprague-Dawley, male), dogs (beagle, male), and monkeys (cynomolgus, male). The experimentally determined parameters are summarized in .

• To date little is known about

  2020-06-08

  

  To date, little is known about mode of action or the underlying genetic basis of DEET repellency for human-biting ticks. To begin to unveil these mechanisms, we carried out behavioral assays to confirm the effectiveness of DEET as a deterrent for D. variabilis. RNA sequencing was then used to build

• br Materials and methods br Results br Discussion

  2020-06-08

  

  Materials and methods Results Discussion In this study, we first showed that fluxametamide, a novel isoxazoline insecticide, inhibits agonist responses in two types of LGCCs, the M. domestica GABACl and GluCl, with higher potency in the former channel versus the latter one (Fig. 3). In addi

• rusty Although in vitro and in vivo immunosuppressive

  2020-06-08

  

  Although, in vitro and in vivo immunosuppressive effects of female steroids have been described in fish (Yamaguchi et al., 2001, Law et al., 2001), their mode of action was not evaluated in detail. Consequently, it is of considerable interest to investigate the intracellular pathways that regulate t

• It is known that cigarette smoke increases the

  2020-06-08

  

  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 HPF in several mouse m

• Lymphocyte mobility and homing is modulated by

  2020-06-08

  

  Lymphocyte mobility and homing is modulated by the chemoattractant receptor subfamily of G protein-coupled receptors (GPCRs) (Campbell et al., 2003, Rot and von Andrian, 2004). B cell migration and position are controlled to a large extent by the lymphoid chemokines CXCL13, CXCL12, CCL19, and CCL21

• br Acknowledgements The research leading to

  2020-06-08

  

  Acknowledgements The research leading to these results has received funding from the European Union Seventh Framework Programme (FP7-PEOPLE-2013-COFUND) under grant agreement no 609020 − Scientia Fellows (JB) and the Research Council of Norway (NFR-grant 221444) (JB, JPM, OB). Introduction Hu

• br Patients and Methods Patients who had been initiated

  2020-06-08

  

  Patients and Methods Patients who had been initiated on a DPP-4 inhibitor (see in the online version at doi:10.1016/j.clinthera.2018.06.002) between April 2012 and June 2017, when the common threshold for dose adjustment for all non-linagliptin DPP-4 inhibitors was a creatinine clearance (CrCl) l

• GLP also showed cardioprotective effects i e infarct size

  2020-06-08

  

  GLP-1 also showed cardioprotective effects (i.e., infarct size reduction and ejection fraction improvement) in experimental models of myocardial ischemia-reperfusion injury by suppressing caspase-3 activation and preventing apoptosis of cardiomyocytes [[50], [51]]. Of note, such a cardioprotection w

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