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The ester moiety is a promising
2021-10-11

The ester moiety is a promising structural motif at the C-3 position for the development of drug-like molecules. However, the labile C-3 ester bond impels these derivate to be susceptible to plasmatic degradation by esterases and this is natural steroidal metabolic process [39,40]. Hence, the isoste
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br Discussion and concluding remarks FPR is
2021-10-09

Discussion and concluding remarks FPR1 is considered to be a promising drug target for treating inflammatory and immunological diseases. Thus, natural compounds that could block and/or regulate FPR1 activity may be an important source of novel therapeutics for modulating inflammatory processes. H
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Our data show that oxidative stress
2021-10-09

Our data show that oxidative stress (high levels of ROS) suppresses the process of lysosomal exocytosis, which would be predicted to impair the expulsion of toxic compounds from cells. Therefore, we propose that ROS have a biphasic effect on the lysosomal clearance: consistent with their role as a s
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Hexokinases HXKs are major regulatory
2021-10-09

Hexokinases (HXKs) are major regulatory enzymes in sugar metabolism and in sugar sensing in plants (Claeyssen and Rivoal, 2007, Granot et al., 2013, Sheen, 2014, Aguilera-Alvarado and Sánchez-Nieto, 2017). HXK can phosphorylate both glucose and fructose to respective hexose-6-phosphates as a first s
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Since we found miR b
2021-10-09

Since we found miR-15b-5p to be differentially expressed along the porcine intestine in 31 day old piglets in a former study [10], the entire miRNA family was analyzed in terms of interaction with potential target-genes. In silico analysis predicted miR-15 family members to target the hedgehog signa
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br Acknowledgments br Introduction Liver disease is one of t
2021-10-09

Acknowledgments Introduction Liver disease is one of the leading causes of death worldwide. Death from any type of acute or chronic liver injury results when sufficient healthy hepatic parenchyma cannot be regenerated to perform vital liver-specific functions. Although the regenerative capabil
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br Concluding remarks br Conflict of
2021-10-09

Concluding remarks Conflict of interest statement References and recommended reading Papers of particular interest, published within the period of review, have been highlighted as: Acknowledgements We thank all the present and former members in our laboratory for their contributions to
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br Material and methods br Results Consistent with our previ
2021-10-09

Material and methods Results Consistent with our previous study, SR-SIM and confocal microscopy showed a large number of IBA1-expressing melk inhibitor in all parts of the human cochleae (Fig. 1). IBA1, the microglial and macrophage-specific calcium-binding protein, is involved in the membrane
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So far GnRH receptors have been detected in the human
2021-10-09

So far, GnRH receptors have been detected in the human ovary, but their physiological importance is still unclear (). In particular, GnRH receptors as well as GnRH types I and II have been localized in the granulosa histamine-2 receptor antagonist of pre-ovulatory follicles, but not of follicles fr
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Reports of hyperlocomotion after administration of ALX coupl
2021-10-09

Reports of hyperlocomotion after administration of ALX-5407 [27] coupled with the lack of hyperlocomotion after administration of SSR504734, a non-sarcosine, long-residence time, competitive inhibitor [19], suggested that the GlyT1 inhibitor chemotype may impact OP. Furthermore, a compound with a co
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Deferasirox synthesis At the second step blind docking simul
2021-10-09

At the second step, blind docking simulation of 150 independent runs was performed with smaller grid box. Structures of open (1v4t.pdb), semi-closed (4dch.pdb) and two structures of closed configuration of GK (pdb codes are 1v4s and 3vev) were used for simulation (for detailed explanations on can se
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Current guidelines for thromboprophylaxis recommend the use
2021-10-08

Current guidelines for thromboprophylaxis recommend the use of vitamin K antagonists (eg, warfarin), low-molecular-weight heparin (LMWH), or indirect inhibitor of factor Xa . Aspirin is also used for thromboprophylaxis in patients undergoing orthopedic procedures , . The efficacy and safety of LMWH
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The results show that pimarane and strobane diterpenoids exe
2021-10-08

The results show that -pimarane and -strobane diterpenoids exert inhibitory effects on FXa suggesting that they may have potential as FXa inhibitor. However, it should be noted that some compounds such as compounds , , , and are poorly bioavailable. Thus, the current study indicates that the number
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Acknowledgments The authors would like
2021-10-08

Acknowledgments The authors would like to thank members of the Department of Discovery Synthesis (DDS) and Biocon-Bristol Myers Squibb Research Center (BBRC) for scaling up key intermediates, analytical team for analytical experiments, lead profiling group for evaluating compounds in an in vitro AD
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To identify genes with significant expression differences we
2021-10-08

To identify genes with significant Procainamide HCl differences, we performed differential gene expression analysis between the two individuals with TRRAP variants (combined as biological replicates) and two unaffected controls. Gene ontology (GO) enrichment analysis of these genes with the GOrilla
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