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α-mangostin It has long been known that native BChE is a
2019-10-10
It has long been known that native BChE is a major factor in the inactivation of cocaine, an ester-type drug of abuse [190]. But recently some researchers conceived the idea that BChE mutations could improve that function to a point that would favorably impact cocaine overdose. Rapid progress was ma
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br Results br Discussion Fetal development occurs under cond
2019-10-10
Results Discussion Fetal development occurs under conditions of low oxygen tension and steady maternal glucose such that physiologic systems including the pancreas are functionally poised in the prenatal state. Postnatally, oxidative metabolism becomes dominant and intermittent feeding exposes
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Both progesterone and the calcium ionophore A rely on the
2019-10-10
Both progesterone and the calcium ionophore A23187 rely on the synthesis of cAMP by sAC to elicit exocytosis in human sperm (Fig. 2E-H and [8], [60]). We had reported earlier that digestion of endogenous cAMP with recombinant cAMP-specific phosphodiesterase 4D [9] or inhibition of its synthesis with
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br Chemistry The test compounds listed in Table Table Table
2019-10-10
Chemistry The test compounds listed in Table 1, Table 2, Table 3, Table 4, Table 5, were synthesized as outlined in Scheme 1, Scheme 2, Scheme 3, Scheme 4, Scheme 5. Synthesis of 2–5 is described in Scheme 1. N-Sulfonylation of the aniline 26 with benzenesulfonyl chloride afforded the sulfonamide
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There has recently been some interest in Uba
2019-10-10
There has recently been some interest in Uba6, which is most similar to slime mold, with BLAST identities of 59% and positives 73% in the 400–600 ADD range. The 400–600 ADD correlation of the two profiles is a striking 87%, so functional differences probably arise outside the ADD binding domain. Hum
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Although the implication of DA and glutamate
2019-10-09
Although the implication of DA and glutamate signaling crosstalk in drug-evoked neuronal adaptations is well acknowledged, targeting the cognate receptors to alleviate symptoms is associated with a loss of efficacy over time and the appearance of severe sides effects, likely due to the involvement o
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Overall the DDR kinase domain has a
2019-10-09
Overall, the DDR1 kinase domain has a typical kinase domain structure and adequate sequence and/or structure similarity with other kinase domains, as shown in Fig. 2, which allow homology modeling of the active and inactive conformations. In addition to conformational changes to the activation loop
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Citrus comprising some of the most widely
2019-10-09
Citrus [29], comprising some of the most widely cultivated fruit crops worldwide, has been consumed as a food and dietary supplement. According to traditional Chinese medicine, dry pericarp of Citrus, as a Chinese herbal remedy, is capable of regulating Qi and expelling phlegm, and has been used to
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There are some limitations to our study First the small
2019-10-09
There are some limitations to our study. First, the small sample size, even if comparable or higher than most studies, did not offer the possibility to consider other variables, such as frequency of use or age of onset. Second, since most subjects did not report current use, we could not analyze sep
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rgs protein Another milestone in the field is
2019-10-09
Another milestone in the field is the de novo discovery of EPAC2 and EPAC1 specific inhibitors through fluorescence-based HTS assays. Due to the excellent EPAC/PKA selectivity of rgs protein , it has been widely applied as a useful chemical probe to discriminate EPAC related signaling pathways and
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The key difference between the membrane zymography and
2019-10-09
The key difference between the membrane zymography and classical measurements of enzyme activities in soil slurries is the enzyme-substrate accessibility. Classical enzyme assays maximize access of substrate to all potentially reactive enzyme sites by ensuring sample destruction and detachment follo
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br Funding br Disclosure of interest br Acknowledgments br I
2019-10-09
Funding Disclosure of interest Acknowledgments Introduction Pulmonary fibrosis (PF) is a chronic disease characterized by extensive deposits of the extracellular matrix (ECM) that can impair the architecture and function of the lungs (Cavazza et al., 2010). Imbalance between the prolifer
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br Conclusions br Acknowledgements This work was supported b
2019-10-09
Conclusions Acknowledgements This work was supported by the Science and Technology Planning Projects of Guangdong Province (2014A020210027); the Major Scientific Research Projects of Universities in Guangdong Province (2016KZDXM042); the Natural Science Foundation of Guangdong Province (2015A0
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Introduction Innate lymphoid cells ILCs are recently
2019-10-09
Introduction Innate lymphoid g protein coupled receptors (ILCs) are recently described immune cells of lymphoid origin and include cytotoxic natural killer (NK) cells and interleukin-7 receptor alpha (also known as CD127)+ subsets, which, similar to T helper (Th) lymphocytes, can be distinguished
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The authors identified inhibitors of SUMOylation using two a
2019-10-09
The authors identified inhibitors of SUMOylation using two assays to monitor the conjugation of SUMO1 to RanGAP1 by E1 and E2 enzymes: a fluorescence resonance energy transfer (FRET) primary screen that evaluated over 250,000 compounds and a chemiluminescence secondary screen. A counter screen was u
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