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Further modifications on the position of compound led to com
2019-11-08
Further modifications on the 8-position of compound led to compound 4 (8-pCPT-2′--Me-cAMP, a.k.a. 007, ), which is a potent (half-maximal activation of EPAC1 at 2.2µM) and selective (about 100-fold EPAC/PKA selectivity) EPAC agonist. Since the discovery of compound , it has been widely used as a pow
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In the horse oviduct the EP receptor was most strongly
2019-11-08
In the horse oviduct, the EP2 receptor was most strongly expressed in epithelial TAK-875 australia particularly in nonciliated (secretory) epithelial cells as evidenced by IHC. Furthermore, relative amount of EP2 mRNA was greater in the ampulla than in the isthmus, although this likely reflects diff
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br Acknowledgements This study is sponsored
2019-11-07
Acknowledgements This study is sponsored by the Natural Science Foundation of China (grant no. 51178161), 111 Project (grant no. B13024) and the Fundamental Research Funds for the Central Universities (grant no. 2017B00914) Introduction Highway and pavement engineers are facing concrete pavem
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ERRGO mice exhibited increased oxygen
2019-11-07
ERRGO mice exhibited increased oxygen consumption, decreased RER, high running endurance, and resistance to diet-induced weight gain. These changes are physiological hallmarks of increased aerobic capacity in mice and are a direct consequence of engineering highly oxidative and vascularized muscle b
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br Disclosure statement br Acknowledgment This work was supp
2019-11-07
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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PGE exerts its functions by binding to
2019-11-07
PGE2 exerts its functions by binding to different receptors. Four different subtypes of PGE2 receptors are found in mammals and are designated as EP1-4. These are G-protein coupled receptors that belong to a family of seven rhodopsin-like transmembrane spanning receptors. They are structurally diffe
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The potent estrogen EE induced a decrease in CYP C
2019-11-07
The potent PF-2341066 EE2 induced a decrease in CYP2C11 activity (reduction in 2α-OH and 16α-OH testosterone) and protein at the 200 ppb dose and in this respect was similar to nonylphenol and genistein. This result agrees qualitatively with the results of Hallstrom et al. (1996) who exposed male ra
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GNF 2 The only reported synthesis of the aminobicyclic
2019-11-07
The only reported synthesis of the aminobicyclic core of is based on bis-alkylation of a 4-amino-5,6-dihydroxypyrmidine with dibromoethane. The likelihood of poor regiocontrol/reactivity in utilizing such a transformation for the synthesis of compounds with a substituent on the dioxinyl ring led us
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fasudil receptor In this study a GMI
2019-11-07
In this study, a GMI of 1.0 was associated with high sensitivity above 90%, specificity below 30% and higher negative predictive value. However, this cut-off couldn\'t have been optimal because of the lower level of Youden J Index which was was low compared to that found in previous studies where t
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The four other mutations S T V I T
2019-11-07
The four other mutations (S281T, V317I, T328A and A329S) were not detected in the absence of the A286S. This could suggest that when all of them are present, there would be a tri-dimensional structural modification that would interfere with the binding of the insecticide and produce different levels
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br Materials and methods br Results and discussion br
2019-11-07
Materials and methods Results and discussion Conclusions The current research work deals with preparation of CES from RHA and comparative study of Ni (II) ion adsorption on CES and RHA. It was observed that carbon embedded silica shows more porous structure and more surface area as compared
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3CAI br Introduction Hematopoietic stem cells
2019-11-07
Introduction Hematopoietic stem 3CAI and leukemic stem cells (HSCs and LSCs, respectively) both have a capacity of self-renewal. Whereas HSCs give rise to all blood lineages during lifetime hematopoiesis, LSCs are responsible for the initiation and propagation of leukemia, as well as drug resista
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A number of chemical strategies have been developed
2019-11-07
A number of chemical strategies have been developed to design activatable optical imaging probes and have been summarized in several excellent reviews 11., 12., 13., 14., 15.. Fluorogenic enzyme substrates are one of the most explored activatable probe types for enzyme detection. These probes contai
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The prospects of the use of this novel
2019-11-06
The prospects of the use of this novel approach for the selective local thermo-activation of enzymes include biomedical and biotechnological applications. As NPs could be engineered to gain access to GSK1838705A through the endosomal compartment [47] or through non-endocytotic pathways [48], [49], [
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br Introduction Our understanding of how ligands interact
2019-11-06
Introduction Our understanding of how ligands interact with G protein coupled receptors is evolving, particularly the recognition that some have the ability to preferentially activate a subset of intracellular signalling cascades – so called pathway biased ligands [1]. Additionally, it is now acc
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