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Given that dimethylamine substitution was tolerated as in
2019-07-04
Given that dimethylamine substitution was tolerated as in SR106447 (), we investigated na inhibitor amine substitutions as replacements for the -butyl group (). Cyclic amines (SR19880, 19882) or simple mono-substituted anilines (SR20037) were not active, nor was an acetylated version (SR20039). The
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A major open question in the field
2019-07-04
A major open question in the field of lipid mediators is the molecular nature of the PLA2 enzyme involved in the release of DHA and related omega-3 fatty acids from phospholipids as a first committed step for the generation of SPMs. Although by analogy with AA it is often assumed that cPLA2α may ser
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It is believed that emphysema in smokers is
2019-07-04
It is believed that emphysema in smokers is mediated by proteases released from inflammatory sigma receptor that cause destruction of the extracellular matrix in alveolar septa [1]. Metalloprotease-12 is mainly released by macrophages and is considered the enzyme responsible for emphysematous lesio
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The discovery of proteases that are active in organic
2019-07-04
The discovery of proteases that are active in organic solvent media has greatly extended their ability in the synthesis of useful products. Microbial proteases which are able be catalyse in non-aqueous solvents present new expectation in enzyme applications. This kind of enzymes gives a major contri
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It is particularly notable that CYP D appears to be
2019-07-04
It is particularly notable that CYP2D6 appears to be the most stable of the major CYP450 rosmarinic acid in its expression over time in vitro and appears to be least affected by culture conditions and sample to sample variability (i.e., CYP2D6 expression is remarkably consistent over time and betwe
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br Acknowledgements This work was
2019-07-04
Acknowledgements This work was supported by grants from Agence Nationale de la Recherche (ANR CAPHE) and from Ligue contre le Cancer. We acknowledge the continuous support of CNRS and the University of Strasbourg. We thank the technical assistance of the “Plateforme de Chimie Intégrative de Stras
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br Acknowledgement This research was
2019-07-04
Acknowledgement This research was supported by a grant from the National Research Foundation of Korea (NRF-2013R1A1A2011238) funded to Young-Mi Lee. Introduction Stroke is considered a serious disease with high morbidity and high mortality. More than 6 million deaths are reported each year wo
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LY-411575 of cGAS has a central role in
2019-07-04
cGAS has a central role in STING activation after DNA sensing, but it is unknown if most of the DNA sensors act independently or in cooperation with the cGAS-cGAMP pathway. This was addressed for IFI16 (Almine et al., 2017, Jønsson et al., 2017) and PQBP1 (Yoh et al., 2015) but remains to be tested
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Introduction Mycobacterium leprae the causative agent of lep
2019-07-04
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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We recently reported that the information about the
2019-07-04
We recently reported that the information about the electronic density obtained from a QTAIM analysis is useful to describe the molecular interactions that stabilize and destabilize the different complexes L-R [13], [14], [15]. Specifically in our previous work reported for DHFR inhibitors, the QTAI
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br Activatable optical imaging probes
2019-07-04
Activatable optical imaging probes Optical fluorescence imaging, which directly detects photons emitted from fluorescent probes, has become as a powerful analytical method to study biological processes both in vitro and in vivo. It is characterized by high sensitivity, is free of radioactive irra
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br Introduction Our understanding of
2019-07-04
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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br Prospect of DDR antagonist DDR a receptor of tyrosine
2019-07-04
Prospect of DDR2 antagonist DDR2, a receptor of tyrosine kinase has been found now to be reported to play a significant role in onset of osteoarthritis at the early stage of diseases progression. The DDR2 are the receptor for extracellular collagen and activated upon the binding of collagen resul
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For radiochemotherapy it is well known that mitotic
2019-07-04
For radiochemotherapy, it is well known that mitotic cell death and apoptosis present the major cell death modes. More recently, autophagy-dependent cell death has been described to occur upon radiochemotherapy (Daido et al., 2005, Song et al., 2017). This form of regulated cell death depends on com
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br Genotype phenotype correlations Genotype phenotype correl
2019-07-04
Genotype-phenotype correlations Genotype-phenotype correlations are limited. Compared with individuals with truncating variants, those with pathogenic missense variants in the adenosine triphosphate binding site had a milder disorder, some with ability to walk unaided, better hand use, and less r
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