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In our preliminary evaluation of this series
2020-03-17
In our preliminary evaluation of this series, we were surprised to discover that cholinesterase inhibitor was found to bind CSF-1R in a classical DFG-in binding mode (a). Dramatic conformational differences in the juxtamembrane domain and activation loops are apparent when this DFG-in structure is
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Leukotrienes themselves are implicated in the development
2020-03-17
Leukotrienes themselves are implicated in the development of gastrointestinal ulcers, asthmas, and different inflammatory processes [18], [19]. It is noteworthy that COX isozymes and LOX share the same substrate arachidonic acid; therefore, inhibition of prostaglandins production by cyclooxygenase p
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Introduction We have recently identified that caseinkinase C
2020-03-17
Introduction We have recently identified that caseinkinase 2 (CK2) inhibition protects white matter (WM) from ischemic injury. We focused our research on CK2 because upregulation of CK2 activity is associated with many diseases, including ischemic injury [1,[6], [7], [8]]. This review highlights an
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Since PTKs are involved in numerous aspects
2020-03-17
Since PTKs are involved in numerous aspects of cell function, their regulation is critical for cell survival and function. The carboxyl-terminal tyrosine of Src-family PTKs is a key site of regulation. Phosphorylation on this carboxyl-terminal tyrosine contributes to the induction of a conformationa
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In the context of E ligase drug
2020-03-17
In the context of E3 ligase drug discovery, it is critical to identify the appropriate E2/E3 substrate pairing to ensure the development and use of the most physiologically relevant screening assay. There have been many reports of limited E2/E3 activity profiling with a small number of E2 and E3 abi
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Haj Yahya et al applied native chemical ligation for the
2020-03-17
Haj-Yahya et al. [52] applied native chemical ligation for the construction of diubiquitin probes. They attached a cysteine residue to the lysine side chain of the proximal ubiquitin and ligated the distal module using the C-terminal thioester of ubiquitin. Elimination of the sulfur Caspase-9 Colori
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br Discussion Several DPP inhibitors are
2020-03-17
Discussion Several DPP-4 inhibitors are currently available for use in the treatment of type 2 diabetes mellitus. Due to the different chemical structures there are marked differences both in the binding kinetics on the target enzyme [10] and also different pathways of elimination [13] exist. In
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Introduction The number of patients with
2020-03-17
Introduction The number of patients with type 2 diabetes is increasing globally, and has become a serious public health problem. Type 2 diabetic patients exhibit a higher risk of bone fracture [1]. In addition, clinical studies have indicated that increased fracture risk is associated with long-ter
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br DDR receptor and MMP
2020-03-17
DDR2 receptor and MMP-13 expression Type II collagen protein in articular cartilage is highly stable structure as its half-life is 117 years [43]. The chondrocytes have limited ability to synthesis type II collagen protein in the matrix of mature articular cartilage once the collagen gets disrupt
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Amyloid Beta-peptide (25-35) Cell migration and invasion are
2020-03-17
Cell migration and invasion are central processes in the development and metastasis of cancer. The regulation of cell migration by DDR1 has been reported in many types of cancer cell lines; however, conflicting results have been reported regarding the inhibitory as well as promotive effects of DDR1
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br Materials and methods br Results Overexpression of KLF in
2020-03-16
Materials and methods Results Overexpression of KLF2 increased the cell viability and reduced the LDH leakage rate and O2•− and ONOO− generation in H/R HUVEC model. To evaluate the effect of KLF2 on H/R HUVEC injury, KLF2 was overexpressed in HUVECs. Cell viability and extracellular LDH level
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br Acknowledgements This work was supported by National Natu
2020-03-16
Acknowledgements This work was supported by National Natural Science Foundation of China (No. 81400241). Introduction Fluoride, as a member of the halogen group of elements, naturally existed in water, soil, animals, and plants around the world (Singh et al., 2018), and it is present in trace
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In the present study we have
2020-03-16
In the present study, we have examined, an alternative approach for introduction of Hyp into bacterial, non-animal collagens. Previously, Gruskin and colleagues [27] had shown that Hyp could be introduced into recombinant mammalian collagen sequences in E. coli through a mechanism of co-translationa
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Notochord is a transient structure differentiating at
2020-03-16
Notochord is a transient structure differentiating at early stage during embryogenesis that is at the origin of vertebral bodies in all vertebrates. In zebrafish, it is composed of vacuolated SB742457 surrounded by a unique ECM structure improperly called notochordal BM. As in chicken and amphibian
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br Conclusions In a former
2020-03-16
Conclusions In a former study we compared the modulating potential of halogenated 1H-benzimidazole derivatives towards CK2 catalytic subunits. Now we were interested if similar differences are also obtained using completely different substances. Some of these natural occurring compounds were alre
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