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In conclusion this is the first description
2021-11-30

In conclusion, this is the first description of a GPR81 agonist with an ability to exert in vivo efficacy without causing flushing. These results demonstrate that GPR81 small-molecule agonists may be effective for treating dyslipidemia. In addition, targeting GPR81 could prevent the unwanted side ef
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br Results br Discussion br Materials and Methods
2021-11-29

Results Discussion Materials and Methods Introduction Deoxyribonucleic Histamine Phosphate (DNA) is among the most important biopolymers in living organisms alongside carbohydrates and proteins. DNA is a linear polymer consisting of four types of nucleobases, deoxyribose, and phosphate.
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Active compounds and were further tested and EC and pEC
2021-11-29

Active compounds , , and were further tested and EC and pEC values were determined as shown in . Compound showed EC of 0.97μM (pEC 6.01) with 84.5% maximal response, which suggests that introduction of alkyl chain on aromatic nucleus of , resulted in improved GPR40 agonistic activity than that of
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br Materials and methods br Results br Discussion In
2021-11-29

Materials and methods Results Discussion In this study, we discover that Sufu stabilizes Gli1 protein levels by antagonizing Numb/Itch-mediated protein degradation. Together with previous work that demonstrates control of Gli2/3 protein levels by Sufu (Chen et al., 2009, Jia et al., 2009, W
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br Materials and methods br Results br
2021-11-29

Materials and methods Results Discussion Defective regulation and inappropriate activation of the HH signaling pathway is implicated in many cancers. SMO targeting inhibitors were the first to enter clinical trials, however complications with acquired resistance and toxicity, also exemplifi
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Herein we describe the development of second generation GSM
2021-11-29

Herein, we describe the development of second generation GSM compounds aimed at improving critical physicochemical properties while maintaining the potent activity of the parent AGSM. Ligand design focused on identifying heterocyclic replacements for the hydrophobic D-ring as a means to improve ADME
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The active site of PS is located at the
2021-11-29

The active site of PS1 is located at the interior of its TM horseshoe-like fold (29) (Fig. 1). TM2 and TM6 serve as “doors” for substrate entry (30), as also observed in recent molecular dynamics (MD) simulations of the PS1 subunit (31). Recent coarse-grained (CG) and atomic simulations also showed
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br Materials and Methods br
2021-11-29

Materials and Methods Results Discussion In the present study, we investigated the postnatal expression of the two GABA receptor subunits, GABAAα1 and GABAB1, in order to determine the differential expression and regional distribution pattern of them between right and left hippocampi in the
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br Drugs approved or in
2021-11-29

Drugs approved or in development To date, three drugs: RAL (MK-0518), EVG (GS-9137) and DTG (GSK1349572) [104], have been approved by the FDA. Their structures are shown in Fig. 5. DTG is under development by GlaxoSmithKline (GSK), and studies have shown DTG to be effective in patients with resis
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Dibutyryl-cAMP, sodium salt mg In conclusion re evaluation o
2021-11-29

In conclusion, re-evaluation of HER2 status is necessary to determine the appropriate use of anti-HER2–targeted therapy beyond disease progression. EGFR and c-met amplification, as well as PIK3CA mutation, are rarely associated with acquired resistance. Our results highlight the importance of formal
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br Introduction The airway epithelium is the first
2021-11-29

Introduction The airway epithelium is the first barrier against inhaled insults and the final barrier against internal forces (hydrostatic, inflammatory, and ischemic) that disrupt water and solute movement across the epithelium. This barrier is formed by adhesion of airway and alveolar epithelia
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Corollary and Lemma Finally Corollary and Lemma show that
2021-11-29

(Corollary 3 and Lemma 9). Finally, Corollary 5 and Lemma 10 show that if then the support of is wide enough and so must contain the points of maximum of the attached. However, the support of is too narrow and so does not contain the points of maximum of the remote. Hence, the remote has at most
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NGS substitution linkage analysis and haplotype reconstructi
2021-11-29

NGS substitution linkage analysis and haplotype reconstruction was previously only used for short genome segments and not in the context of antiviral resistance. We optimized this approach to cover a complete viral protein and major DAA target, enabling us to investigate resistance associated NS3P h
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br Funding This work was partially supported by
2021-11-29

Funding This work was partially supported by the National Institute on Alcohol Abuse and Alcoholism, award R00AA021264, startup funds from the Department of Immunology, Herbert Wertheim College of Medicine, and the Office of Research and Economic Development at FIU, and pilot funds from Dr. Werth
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Firstly the impact on activity and selectivity was made by
2021-11-29

Firstly, the impact on activity and selectivity was made by replacing the 2, 3-di-F substitution of ring A with 2,3-OCHO- () and 2-NO () substitutions, and replacing the 3, 5-di-F substitution of ring B with 3,5-di-OMe () and 3,5-di-Me () substitutions. Compound kept moderate activity (EC = 220 nM)
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