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From an industrial perspective the
2021-02-24

From an industrial perspective, the low turnover numbers and limited substrate scope of α-KG halogenases still represents a significant challenge. However, in light of the fact that currently no chemical processes are available for the selective halogenation of aliphatic carbon centers in complex mo
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This study showed that ER redox disturbance associated ER
2021-02-24

This study showed that ER-redox disturbance-associated ER stress is linked to cytoplasmic chaperone signaling, including HSP90 stability and its client protein, eNOS. The highly increased PERK and IRE-1α lead to dissociation with the chaperone protein, thereby decreasing HSP90 stability (Fig. 5B). S
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This study showed that ER redox disturbance associated ER
2021-02-24

This study showed that ER-redox disturbance-associated ER stress is linked to cytoplasmic chaperone signaling, including HSP90 stability and its client protein, eNOS. The highly increased PERK and IRE-1α lead to dissociation with the chaperone protein, thereby decreasing HSP90 stability (Fig. 5B). S
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Most remarkably an essentially identical collagen binding
2021-02-24

Most remarkably, an essentially identical collagen-binding mode to DDR2 is employed by SPARC, an α-helical matricellular protein unrelated to DDR2 that also recognizes the GVMGFO motif in collagen (Giudici et al., 2008, Hohenester et al., 2008). The convergence of binding mechanisms suggests that th
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Herbal products may alter the metabolism of certain
2021-02-24

Herbal products may alter the metabolism of certain drugs and, likewise, the metabolism of components of herbal products may be altered by some drugs, specifically those that affect cytochrome P450 RO4929097 (CYP). These can bring about an alteration of the pharmacokinetics and pharmacological acti
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Against this backdrop we set out to
2021-02-24

Against this backdrop, we set out to identify synthetic and endogenous ligands that bind directly to and regulate the activity of Nurr1. Owing to the pivotal role Nurr1 plays in producing and processing dopamine, and the need for neurons to tightly regulate dopamine levels, we postulated that the re
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Against this backdrop we set out to
2021-02-24

Against this backdrop, we set out to identify synthetic and endogenous ligands that bind directly to and regulate the activity of Nurr1. Owing to the pivotal role Nurr1 plays in producing and processing dopamine, and the need for neurons to tightly regulate dopamine levels, we postulated that the re
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As part of a program to explore the
2021-02-24

As part of a program to explore the key binding interactions between the core of 1 and DGAT-1 a systematic analysis of the aminopyrimidine subunit was initiated. A potential approach to improving passive permeability within this series would be to increase lipophilicity via incorporation of substitu
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Two are the sigma receptors identified to date the
2021-02-23

Two are the sigma receptors identified to date: the non-opioid receptor, σ1R, and σ2R, whose identity with the Progesterone Receptor Membrane Component 1 (PGRMC-1) protein is in doubt (Chu et al., 2015). Despite endogenous ligands have not been yet identified, drugs of abuse may interact with these
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p and p which are downstream of pAkt and
2021-02-23

p21 and p16, which are downstream of pAkt and pERK1/2, are tumor suppressors which induce cell senescence and NG,NG-dimethyl-L-Arginine hydrochloride synthesis arrest [[56], [57], [58]]. Inhibitors of pAkt or pERK1/2 can activate p21 and p16 and promote cell senescence and cell cycle arrest [11,12,[
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EphB promotes tumor growth by stimulating angiogenesis throu
2021-02-23

EphB4 promotes tumor growth by stimulating angiogenesis through EphrinB2 [18]. However, the distinct and specifically involvement of LY2874455 sale and veins in the tumor angiogenesis of all tumor grades is unclear. Our results indicate that the relation between EphrinB2 and EphB4 stained blood ves
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br Disclosure statement br Acknowledgment This work was
2021-02-23

Disclosure statement Acknowledgment This work was supported by the National Natural Science Foundation of China (81270704, 81330018). Background Over-expression of cyclooxygenase-2 (COX-2) is common in many malignancies including non-small cell lung cancer (NSCLC) and is associated with po
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Another enzyme class that has emerged
2021-02-23

Another enzyme class that has emerged as a potential alternative to P450s are the so-called ‘unspecific peroxygenases’ (UPOs). They also contain a heme but are extracellularly expressed fungal enzymes that are often more stable than P450 monooxygenases. Importantly, UPOs use H2O2 instead of O2 as th
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br Results and discussion The effects
2021-02-23

Results and discussion The effects of hypoxia, a combination of shear stress and hyperoxia, and a combination of shear stress and hypoxia in BAECs were assessed at 0, 15, 30, 60, 120, and 180 min. Changes in phosphorylation levels of eNOS at Ser635 were investigated using immunoblotting, and repr
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br Molecular characterization of LEI L DNase II LEI like
2021-02-23

Molecular characterization of LEI/L-DNase II LEI, like most serpins, is a metastable protein and its anti-protease activity is related to its “stressed to relaxed transition”. So that, the inhibition of elastase by the well described suicide mechanism generates the cleaved form of LEI (see Padron
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