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Although domain organization had been clearly delineated by
2022-07-07
Although domain organization had been clearly delineated by the 4.3-Å structure of T4-γ-secretase [], atomic modeling of the side chains had to wait for the 3.4-Å structure []. In total, 598 residues in the transmembrane region and 632 residues in the ECD were modeled for the four components of huma
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The structural similarity software vROCS OpenEye has been ut
2022-07-07
The structural similarity software vROCS (OpenEye) [45] has been utilized by Musumeci et al. [46] to screen the Maybridge [47] HitFinder database (∼14,400 compounds) using Distamycin A (Fig. 3B) as a query. Using the Tanimoto coefficient (Section 6.4) and vROCS's colour scoring (atom/feature similar
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The suboptimal trypsin selectivity profile of DPC
2022-07-07
The suboptimal trypsin selectivity profile of DPC423 prompted us to investigate additional P moieties for potency and selectivity. Glycinamide P () showed low nanomolar binding affinity against fXa which suggested that this P moiety sits deeper into the S pocket of fXa. To further elaborate on this
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br Place in Therapy In the case of
2022-07-07
Place in Therapy In the case of minor bleeding, the anticoagulant effects of all FXa inhibitors except betrixaban, which has a longer half-life, will diminish within 24-48 hours of discontinuation of the drug provided the patient has normal renal function. In these cases stopping the FXa inhibito
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Potential platelet related mechanisms that
2022-07-07
Potential platelet-related mechanisms that might explain an augmented risk of MI in dabigatran treated patients have been investigated: Enhanced platelet reactivity is known to be associated with the risk of MI (Mangiacapra et al., 2018) and catalytically active thrombin is a potent stimulus to indu
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In NAFLD models the first
2022-07-06
In NAFLD models, the “first hit” is liver fat accumulation, which causes insulin resistance, whereas the interplay of inflammatory cytokines, which causes inflammation, acts as the representative “second hit” [9]. However, recently, the “multiple hit” hypothesis has taken into consideration that mul
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br Family A Receptors as
2022-07-06
Family A Receptors as Promiscuous Sensors for Peptone and Free Fatty Acids (FFAs) In addition to the family C 7TM receptors, several family A 7TM receptors are promiscuous in their ligand preferences, and several respond to organic nutrients from food, notably protein degradation products and FFA
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br Experimental br Acknowledgments The authors
2022-07-06
Experimental Acknowledgments The authors are grateful to Fundamental Scientific Research Fund of Chinese Academy of Medical Sciences (No. 2016ZX350030) for financial support. Introduction 2-Lysophosphatidylcholines (1-acyl-glycero-3-phosphocholines, 2-LPC) are blood derived factors involve
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Overall our results indicated the involvement of
2022-07-06
Overall, our results indicated the involvement of GABAAR in controlling GnRH/LH release through mechanism which included GABA action on molecular processes leading to GnRH biosynthesis. This is consistent with previous in vivo [14,54] and in vitro [55] studies in ewes suggesting that GABA inhibits G
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Additionally increased GLO gene expression protein expressio
2022-07-06
Additionally, increased GLO1 gene expression, protein expression, and activity have been reported in a variety of cancers, including breast,22, 23, 24 pancreatic, melanoma, and prostate.27, 28, 29 Vince and Daluge proposed that inhibitors of GLO1 could serve as anti-tumor agents, by increasing conce
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C http www apexbt com
2022-07-06
C136 is present in the joining region of two domains of NEIL1 and plays a critical role in the stability and dynamics of enzyme (Roy et al., 2007, Prakash et al., 2014). E181 resides in the conserved H2TH motif that binds to DNA and is very essential for enzyme activity. C136 is present in the near
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br Glycoengineering br The Omics perspective The publication
2022-07-06
Glycoengineering The « Omics » perspective The publication of the CHO-K1 genome sequence in 2011, followed by the publication of two Chinese hamster and six CHO cell line genomes in 2013, bring new opportunities in developing and engineering CHO paf receptor for improved glycoprotein producti
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br Experimental procedure br Acknowledgments This research w
2022-07-06
Experimental procedure Acknowledgments This research was supported by funds provided by NIH/NIAAA grant P01 AA020683 and the Waggoner Center for Alcohol and Addiction Research. Introduction Acute mesenteric ischemia (AMI) is still associated with a high mortality rate, and currently, an ea
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Recent studies suggested that non
2022-07-06
Recent studies suggested that non-coding RNAs participate in the modulation of Glut1 expression. For instance, the lncRNA NBR2-Glut1 axis was suggested to modulate cancer cell sensitivity to phenformin [37]. In renal carcinoma, miR-1291 is involved in the regulation of Glut1 Magnolol receptor [38].
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In early a collaborative effort between the
2022-07-05
In early 2017, a collaborative effort between the group that pioneered the above described evidence of platinum-induced PUFA chemotherapy resistance and a group that has contributed to much of the known molecular pharmacology of FFA4, revealed that the molecular target of 16:4(n-3), which affords ch
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