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Carbamate and OP insecticides are still among the most widel
2019-09-20

Carbamate and OP insecticides are still among the most widely used pesticides in the world [151]. In 2012, the OP insecticides chlorpyrifos and acephate were ranked 14th and 22nd overall in estimated amounts of agricultural pesticides used in the US. The carbamate insecticide carbaryl and the OP ins
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We have previously reported the characterization
2019-09-20

We have previously reported the characterization of A-127722, a novel, non-peptide endothelin antagonist that displays very high affinity binding (K=69 pM) with a more than 1000-fold greater affinity for human endothelin ETA than ETB receptor. Although A-127722 is >1000-fold more selective for endot
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The ADME profile of AAT was
2019-09-20

The ADME profile of AAT-008 () was very promising, with high stability in HLM. The pre-clinical pharmacokinetic properties of AAT-008 were also assessed in rats (Sprague-Dawley, male), dogs (beagle, male), and monkeys (cynomolgus, male). The experimentally determined parameters are summarized in . A
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br Materials and methods br Results discussion br Conclusion
2019-09-20

Materials and methods Results + discussion Conclusions We have demonstrated the systematic optimization of the functional folding of a CF synthesized GPCR. The approach addresses central issues relevant for many membrane proteins such as disulfide bridge formation, proper hydrophobic enviro
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br Materials and methods br Results br
2019-09-19

Materials and methods Results Discussion The present work demonstrates the functional role of DGAT2 in elevating the neutral lipid accumulation in engineered N. oceanica, which have aroused a great deal of interest in industrial scale biofuel production. Recently, there have been increasing
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Besides degrading cholesterol the cholesterol
2019-09-19

Besides degrading cholesterol, the cholesterol degradation pathway also offers a route to obtain useful starting materials for the production of steroid drugs and hormones. Indeed, steroids are among the most marketed pharmaceuticals with about 300 approved steroid drugs [15] and a worldwide market
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Investigations of mice lacking up to
2019-09-19

Investigations of mice lacking up to three CDKs identified the mitosis-regulating kinase CDK1 as the main essential component for the cell cycle, whereas ablation of other Z-DQMD-FMK mass regulators such as CDK2, CDK4, or CDK6 did not result in defective proliferation 12, 13. Mouse models and speci
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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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