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A summary of the drug CDK hydrophobic hydrogen bonding H
2019-07-23

A summary of the drug-CDK2/6/9 hydrophobic (Φ), hydrogen-bonding (H), and polar-bonding (P) interactions based upon the KLIFS residue numbers is provided in Table 5. The KLIFS system gives comparable residues from different bombesin receptor the same value [77], which facilitates comparisons among d
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br Methods and materials br Cyclooxygenase
2019-07-23

Methods and materials Cyclooxygenase (COX) is the key enzyme required for the conversion of arachidonic C646 to prostaglandin, prostacyclins and thromboxanes., , , Two distinct isoforms of COX were initially discovered: COX-1 is a constitutive, housekeeping enzyme that is expressed in many tiss
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In the particular case of metals
2019-07-23

In the particular case of metals, several authors showed that AChE inhibition is somewhat contradictory and even questionable (Frasco et al., 2005, Nunes et al., 2005, Sáenz et al., 2010). Uranium is a particular metal, and one that has been shown to complex with several biologically important prote
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SKF38393 HCl Recently we have created CRISPR Cas mediated
2019-07-23

Recently, we have created CRISPR/Cas9-mediated col14a1a knockout fish to interrogate the function of col14a1a during regeneration using the caudal fin model. Using AFM, we showed that collagen XIV-A transiently acts as a molecular spacer responsible for BM biomechanics possibly by helping laminins i
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Previously published data showed an interaction
2019-07-23

Previously published data showed an interaction of α-tubulin and CK1δ [15] that was validated in the present study using SPR (Fig. 1A). The dominant motifs involved in the CK1δ/α-tubulin interface were defined using a peptide library of peptides covering the CK1δ amino niclosamide solubility sequen
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The ADME profile of AAT was very promising
2019-07-23

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 . A
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In principle in vitro techniques for
2019-07-23

In principle, in vitro techniques for assessing enzyme induction might include the use of cultured hepatocytes, precision-cut liver slices, immortalized filipin lines (such as those derived from hepatomas) and reporter gene constructs (where appropriate cells are transfected with recombinant DNA en
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br Introduction Epidermal growth factor receptor EGFR activa
2019-07-23

Introduction Epidermal growth factor receptor (EGFR)-activating-mutant non-small cell lung cancer (NSCLC) often initially responds well to EGFR tyrosine kinase inhibitors (TKIs) (Haber et al., 2011); however, the disease almost always recurs about 10–13 months of therapy. Analysis of clinical spe
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br Cytokine impact on ILC
2019-07-23

Cytokine impact on ILC fate Increasing evidence shows that ILC2 and ILC3 may convert into ILC1-like L-745,870 trihydrochloride by downregulating either GATA3 or RORγt, respectively, upregulating T-bet and gaining the capacity for IFN-γ production [60,61]. This process, often referred to as ‘ILC p
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br Substoichiometric substrate modification E ligases
2019-07-23

Substoichiometric substrate modification E3 ligases catalyze the rapid transfer of the SUMOD from the E2 enzyme to the substrate. By definition, enzymes are recycled in the reaction, allowing multiple rounds of substrate modification by a single enzyme. Thus, enzymes function at substoichiometric
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Our recent QTL mapping study revealed that
2019-07-22

Our recent QTL mapping study revealed that the adaptor genes, including the NCK genes and the ABI genes, are located within the genomic regions harboring the most significant QTL (Zhou et al., 2017), suggesting that these genes could be involved in the determination of resistance, and possibly throu
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Key molecules in the EP second messenger signaling cascade t
2019-07-22

Key molecules in the EP1 second messenger signaling cascade that are necessary for potentiation of GluK2/GluK5 were identified. We also identified three GluK5 serines located in a membrane-proximal C-terminal domain that, when mutated to the phosphomimetic aspartate and expressed with GluK2, rendere
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Our approach including the characterization of histone
2019-07-22

Our approach, including the characterization of histone modifications in scarce NK subsets, allowed us to identify super-enhancers, which associate with genes endowing a given cell type with its unique identity (Hnisz et al., 2013). Especially intriguing were SEs with distinct activities in NK subse
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br Expression data suggest involvement of additional TRIMs
2019-07-22

Expression data suggest involvement of additional TRIMs in heart function Given the complexity of the cardiac function, involved molecular pathways and processes, and the fact that only a few of the TRIMs have thus far been shown to have a cardiac role, we hypothesized that there would be more TR
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br Patients and Methods Patients who had been
2019-07-22

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)
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