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Thus DGK active sites remain
2020-09-02

Thus, DGK-active sites remain ill-defined and, combined with the lack of crystal structures for mammalian DGKs, have limited our understanding of substrate and inhibitor binding. As a result, current DGK inhibitors consist of compounds with poor specificity within the DGK superfamily (de Chaffoy de
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One possible explanation for differences in the binding
2020-09-02

One possible explanation for differences in the binding ability of monomeric versus dimeric forms of DDR2 ECD to collagen could be that the monomeric form only binds to the primary GVMGFO site, whereas dimeric (and oligomeric) DDR2 ECD binds to additional sites on the collagen triple-helical molecul
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somatostatin receptor br Acknowledgements br This work was s
2020-09-02

Acknowledgements This work was supported by grants from the National Natural Science Foundation of China (Grant No.: 30260088) and the prophase research for National “973” Project of China (Grant No.: 2007CB116203). The DNA sequences of Hbvp1 and the Hbvp1 promoter were deposited in GenBank, an
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Beside the previously reported Topo I inhibition time and co
2020-09-02

Beside the previously reported Topo I inhibition, time and concentration dependent CRM1 inhibitory properties of klavuzon derivatives have been shown as a second mechanism of action in this work. Especially, compounds 3 and 20 are the most effective derivatives and they completely inhibit CRM1 activ
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CRF and urocortin I are not only
2020-09-02

CRF and urocortin I are not only readily found throughout the spinal cord (Korosi et al., 2007), CRF analogs are clearly able to alter nociceptive signals (Imbe et al., 2010; Lariviere and Melzack, 2000). However, it was unclear whether they are released endogenously and involved in the spinal modul
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To evaluate the new quadrupolar CPA qCPA
2020-09-02

To evaluate the new quadrupolar CPA (qCPA) the pure fluid properties of CO2 are predicted both in the critical region and in the compressed liquid region. The model is furthermore applied for the prediction and correlation of binary mixtures with CO2 and n-alkanes, water, alcohols and a few quadrupo
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The CYP D inferred metabolizer
2020-09-02

The CYP2D6-inferred metabolizer phenotype describes only one phase of the tramadol (T) ADME (absorption, distribution, metabolism, and excretion) and response process and does not explain all genotypic contribution of an individual’s phenotypic expression [11]. Numerous polymorphisms in the downstre
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Introduction Mycobacterium leprae the causative agent
2020-09-01

Introduction Mycobacterium leprae, the causative agent of leprosy, affects skin, peripheral nerves and upper respiratory tract [1]. Although leprosy has been eradicated from most of the countries, it still affects approximately a quarter of a million people from India [2]. Details of many bacteriol
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Materials and methods Cell culture and
2020-09-01

Materials and methods Cell culture and receptor gene transfection. PC12 gap-26 were purchased from the Institute of Cell Biology, Chinese Academy of Sciences, Shanghai, China. The cDNA for mouse CysLT1 or CysLT2 receptor (mCysLT1 and mCysLT2, subcloned into pcDNA3.0) was kindly gifted by Professor
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In recent years there has
2020-09-01

In recent years there has been a dramatic increase in identification and optimization of potent CRTh2 antagonists which may not only inhibit the recruitment and activation of Th2 cells but also accelerate apoptosis and clearance of these cells from inflamed tissue, thereby promoting the resolution o
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Abha et al reported Natural coumarinolignoids isolated from
2020-09-01

Abha et al. reported Natural coumarinolignoids isolated from the seeds of Cleome viscosa consist of a racemic mixture of cleomiscosins A 19, B 20 and C 21 and were screened for anti-inflammatory activity through mol. docking and QSAR studies by using reported in vivo activity of Swiss albino mice. B
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The CYP D inferred metabolizer phenotype describes
2020-08-31

The CYP2D6-inferred metabolizer phenotype describes only one phase of the tramadol (T) ADME (absorption, distribution, metabolism, and excretion) and response process and does not explain all genotypic contribution of an individual’s phenotypic expression [11]. Numerous polymorphisms in the downstre
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br Introduction Cancer related inflammation is associated wi
2020-08-31

Introduction Cancer related inflammation is associated with poor prognosis and reduced survival in numerous human malignancies. Expansion of myeloid derived immune Fungicidin in response to tumor-secreted factors largely contributes to the heightened systemic and intra-tumoral inflammatory milie
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Simulation methods In our study the TIP
2020-08-31

Simulation methods In our study, the TIP3P model is applied for water, AMBER99sb force field [24] is used to describe three types of EGFR, including the wild type (PDB: 2ITY) [25], its mutant G719S (PDB: 2ITO) [25] and mutant T790M (PDB: 3IKA) [26]. The force field of Tubemoside molecule is paramet
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G DH has gained interest because of its broad substrate
2020-08-31

G3DH has gained interest because of its broad substrate specificity and site-selective oxidation properties [9,10]. The conversion product, 3-ketoglycoside, possesses potential as a starting material for the chemical industry such as in polymer and surfactants because the keto group becomes a specif
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