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Conventional aromatic radiofluorination via nucleophilic sub
2020-09-23
Conventional aromatic radiofluorination via nucleophilic substitution requires electron-withdrawing activating group(s) at the ortho or para position to achieve good radiolabeling yield. In the case of CJ-042794 (), the phenoxy substitution para to the fluoro group is considered an electro-donating
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On the opposite side sPLA X has
2020-09-23
On the opposite side, sPLA2-X has also been implicated in the pathology of cancer [167,168]. Human sPLA2-X induces lipid droplet formation in Ras-driven MDA-MB-231 triple-negative breast cancer AEBSF and promotes their survival during nutrient stress. It acts through the products of its enzymatic a
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Introduction Obesity constitutes a global healthcare
2020-09-23
Introduction Obesity constitutes a global healthcare problem and has many adverse effects on the cardiovascular function [1,2]. Recently, the perivascular adipose tissue (PVAT) has emerged as a relevant fat depot for cardiovascular risk and as a potential trigger in vascular dysfunction. Indeed, PV
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Elastase belongs to chymotrypsin family of proteases and it
2020-09-23
Elastase belongs to chymotrypsin family of proteases and it is responsible for the breakdown of elastin and other proteins, such as collagen and fibronectin, which are fundamental for the ECM elastic properties (Imokawa and Ishida, 2015). Misregulations of this enzyme are involved in skin ageing pro
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br Results br Discussion CCA is a fatal tumor
2020-09-23
Results Discussion CCA is a fatal tumor originating from the intrahepatic bile duct and the prognosis is very poor (Hoyos et al., 2018). CCA is one of the most dangerous primary liver malignant tumors and the most common malignant tumor of the biliary tract worldwide. However, the underlying m
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MuRF interacts with four and a half LIM
2020-09-23
MuRF3 interacts with four-and-a-half LIM domain (FHL2) and γ-filamin leading to their degradation via UPS [64]. Conversely, abnormal aggregation of these proteins was observed in mice lacking MuRF3. Moreover, MuRF3-/- mice were found more prone to cardiac rupture after acute myocardial infarction (
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ikk br Acknowledgements This work was supported by
2020-09-22
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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Midazolam oral clearance is used for characterization
2020-09-22
Midazolam oral clearance is used for characterization of both intestinal and hepatic CYP3A activity. However, the identification and subsequent use of metabolic markers of CYP3A activity can eliminate the need for unnecessary administration of probe drugs such as midazolam. Such metabolic markers wo
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Finally unilateral microinjection of CP Astressin B
2020-09-22
Finally, unilateral microinjection of CP-376395, Astressin 2B, CP-376395 + CRF or ASTR 2B + CRF into the BLA (Fig. 3A) or CeA (Fig. 3B) did not significantly alter spontaneous motor activity in the open field test (F4,24 = 0.148, P > 0.05; F4,29 = 0.290, P > 0.05 in the BLA and CeA, respectively, AN
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br Conclusions Enzyme can be delivered to
2020-09-22
Conclusions Enzyme can be delivered to the tumour by using humanised or fully human doxycycline hcl or even loaded into synthetic nanospheres produced from silica [64] or liposomally entrapped [65]. For any future ADEPT developments, a number of basic points need to be considered. As immunogenic
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In these tables the AAD for
2020-09-22
In these tables, the AAD for most of the alcohols in 2B and 3B schemes is less than 1%. It should also be said that for ethanol, AAD in 2B scheme is (0.36%) and for 3B scheme it is (0.02%), which indicates superior prediction of 3B scheme compared to 2B in CPA ƒ-theory model. Table 8a, Table 9 show
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The P H activity and the large
2020-09-22
The P4H activity and the large number of 4-Hyp residues that are formed, amounting to half of all the Pro residues or 10% of all residues, have been identified as having a clear role in the structure and chemistry of the triple helix [3]. The role of the rare 3-Hyp residues is less clear and is stil
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An ideal CHK inhibitor would be minimally
2020-09-22
An ideal CHK-1 inhibitor would be minimally cytotoxic, while enhancing the anti-tumor effect of a real cytotoxic agent that would be used in combination with the inhibitor. Our CHK-1 inhibitors have shown excellent selectivity over a panel of kinases including those regulating the cell cycle, but th
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br ANTITHROMBOTIC TREATMENTS br VOLUME OUTCOME RELATIONSHIP
2020-09-22
ANTITHROMBOTIC TREATMENTS VOLUME-OUTCOME RELATIONSHIP FOR REVASCULARIZATION PROCEDURES The guidelines also maintain the recommendations for training in PCI, both for ACS (≥ 75 procedures per operator in centers with at least 400 PCI procedures per year and a 24-hour on-call service) and for s
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br Signaling of DDR receptor and its
2020-09-21
Signaling of DDR2 receptor and its regulation Being the tyrosine kinase receptor, downstream signaling of DDR2 receptor is initiated by phosphorylation of cytoplasmic tyrosine residue upon ligand binding (Type II collagen) but the authentic facts or detail information of tyrosine phosphorylation
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