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In the course of our
2019-09-19
In the course of our program, which was aimed at developing CRTH2 antagonists for the treatment of allergic diseases, we have been pursuing a new class of potent and selective CRTH2 antagonist lead based on the structures of CRTH2 antagonists known to date (, , ). Using a fused 6–6-membered ring sys
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To assess which export pathway is used by
2019-09-19
To assess which export pathway is used by the iNOS mRNA, we inhibited CRM1 activity by incubation of DLD-1 tezacaftor with LMB. Since LMB covalently and exclusively binds to CRM1, it represents a potent and specific inhibitor of the CRM1 transport activity [38]. Inhibition of CRM1 activity as well a
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Recent studies have reported that miR plays
2019-09-19
Recent studies have reported that miR-454 plays an important role in various cellular processes and diseases, such as inflammation, infection, osteogenic differentiation, and cancers [25,27,29,30]. Multiple evidence has documented that miR-454 promotes the proliferation, migration and invasion, and
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Our observation that nuclear but not cytoplasmic EP expressi
2019-09-19
Our observation that nuclear, but not cytoplasmic EP4 expression is associated with different outcomes is interesting. In breast cancer, using the same methods, we did not detect EP4 in the nucleus of malignant GGsTop kinase whereas cytoplasmic EP4 was commonly observed [13]. While G protein-couple
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br O GlcNAc transferase OGT belongs
2019-09-19
O-GlcNAc transferase OGT belongs to the metal-independent GT-B superfamily of glycosyltransferases, which has been well-reviewed previously [14,15]. OGT is an essential gene encoded on the X-chromosome, and it has two main regions: a long N-terminal tetratricopeptide repeat (TPR) region and a C-t
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At baseline mutant allele frequency of EGFR in tissue and
2019-09-19
At baseline, mutant allele frequency of EGFR in tissue and plasma samples did not correlated with anti-tumor response (Supplementary Fig. 1). Among 35 patients who were positive for cell-free DNA (cfDNA) at baseline, changes of cfDNA during treatment were analyzed. Negative conversion (NC) of cfDNA
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Expression of both CH H
2019-09-19
Expression of both CH25H and CYP7B1 by lymphoid stromal PSI-7977 is required for the synthesis of 7α,25-OHC in lymphoid tissues and the correct positioning of B cells. Production of EBI2 ligand by hematopoietically derived cells appears limited [24] but may occur under some circumstances, given tha
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br Results and Discussion br Experimental Procedures br Ackn
2019-09-19
Results and Discussion Experimental Procedures Acknowledgments The ubiquitin–proteasome system (UPS) is important for biological processes such as protein degradation and protein function regulation. In general, poly-ubiquitinated proteins are degraded by proteasomes, and some proteins ac
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Dysfunction of the ubiquitin proteasome system causes abnorm
2019-09-19
Dysfunction of the ubiquitin-proteasome system causes abnormal organelle morphology and impairs sperm formation and maturation steps resulting in male infertility [[7], [8], [9]]; this indicates that ubiquitination is essential for spermatogenesis and sperm function during fertilization. β-catenin i
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In anticipation of an approach based on modification of
2019-09-19
In anticipation of an approach based on modification of the cyclohexylacetic Sildenafil Citrate subunit of 1 as a means of improving permeability, a set of analogs were prepared to map out the optimum display of the acidic functionality. Homologated acids 25 and 26 were found to be equipotent to 1,
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The requisite extended benzyl alcohols and and final potenti
2019-09-19
The requisite extended benzyl alcohols –, , and and final potential DFG-out binding hybrid inhibitors – and – were prepared as shown in , . Benzaldehyde was alkylated with -methoxybenzyl chloride and then reduced with sodium borohydride to give benzyl alcohol . Pyridine derivative was prepared by
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Programmed cellular death or apoptosis is a process genetica
2019-09-18
Programmed cellular death or apoptosis is a process genetically controlled that plays an important role in cellular homeostasis, being an important defense mechanism to remove cells that have been infected, damaged or mutated (Smith and Smith, 2012, Wlodkowic et al., 2011). Nevertheless, apoptosis s
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The aniline R group was extensively explored and
2019-09-18
The aniline R2 group was extensively explored and a large variety of substitution was tolerated at several positions on the aryl ring (). Notably, substitution at the 3-position often gave increased potency. Increasing lipophilic bulk at this position gave increasing potency within an ether series (
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Voriconazole An increasing body of evidence demonstrates tha
2019-09-18
An increasing body of evidence demonstrates that MXC can cause neurobehavioral and neuropathological alterations [7]. In the brain, there are several steroidogenic enzymes, which are responsible for neurosteroid production. Neurosteroids are subsets of steroids that rapidly change neuronal excitabil
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It is well known that
2019-09-18
It is well known that CysLTs exert potent contractile action on human bronchial smooth muscles through activation of CysLT1 receptors. Indeed, in vitro antigen-induced contraction of passively sensitized human bronchial tissue is markedly suppressed by a pre-treatment with CysLT1 receptor antagonist
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