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The phenolic hydroxyl group of ezetimibe
2020-05-15
The phenolic hydroxyl group of ezetimibe tolerated various structural modifications (disaccharide, carboxyalkyl and glucuronide) that retained inhibitory activity.13, 14, 15 We conjugated glycylglycine to phenolic hydroxyl group and synthesized ten 1H-pyrrole-2,5-dione derivatives 14a-j successfully
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Hepatocyte proliferation is accompanied by changing
2020-05-15
Hepatocyte proliferation is accompanied by changing gene expression [1,2]. as two of the three estrogen receptors are transcription factors: Estrogen Receptor alpha (ERα) and ERβ [[3], [4], [5]]. The most potent ligand estradiol, binds to ERα/ERβ and exerts changing cognate gene transcription [5]. O
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Sennoside C In mammals NETs contain DNA and antimicrobial pr
2020-05-15
In mammals, NETs contain DNA and antimicrobial proteins composed mainly of nuclear histones, granule-derived neutrophil elastase, myeloperoxidase, lactoferrin, pentraxin, and gelatinase among others [11], [46], [47], [48]. In fish, NETs-like structures have been observed, and DNA staining and immuno
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Apart from its high affinity the selection
2020-05-15
Apart from its high affinity, the selection of GW2580 as Alosetron lead in our radiotracer development program was motivated by its exceptional selectivity. The observed profound impact of small structural modifications on the selected panel of four kinases tested prompted us to conduct comprehensiv
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These evidence prompted us to investigate the
2020-05-15
These evidence prompted us to investigate the effectiveness of CT-133, a newly discovered, well-tolerated, selective and potent CRTH2 antagonist, as a treatment of ALI. CT-133 has shown a potential response in treating chronic obstructive pulmonary disease (COPD), allergic rhinitis and bupropion hyd
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Introduction Since the recognition of AIDS in more
2020-05-15
Introduction Since the recognition of AIDS in 1981 more than thirty-five years ago, nearly 70 million individuals have been infected with human immunodeficiency virus type 1 (HIV) and roughly half have died (http://www.unaids.org/en/resources/documents/2016/AIDS-by-the-numbers). Although the introd
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GSK1838705A Survival analysis has been widely
2020-05-15
Survival analysis has been widely used in medical science, economics, finance, and social science, among others. In many studies, survival data have primary outcomes or responses that are subject to censoring. The Cox model [7], [8] is the most commonly used regression model for survival data, and t
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br Results and discussion br Conclusions We have
2020-05-15
Results and discussion Conclusions We have developed a method to produce wildtype and mutant Ric-8A proteins from E. coli that can be phosphorylated at the regulatory protein kinase CK2 phosphosites to near homogeneity. The phosphorylation status and activity of the purified Ric-8A proteins wa
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Case report The patient was referred to the oral
2020-05-15
Case report The patient was referred to the oral and maxillofacial department at the authors’ institution for further evaluation and treatment. The patient underwent tumor resection with left hemi-mandibulectomy with wide bony margins (Fig. 1A), and mandible reconstruction with fibula free flap and
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Despite many studies having demonstrated the importance of
2020-05-15
Despite many studies having demonstrated the importance of connexin43 (Cx43), the most abundant connexin in bone cells, for bone development and turnover during the last decade [27], little is currently known about GJIC and Cx43 in primary bone tumors. In this report, we analyzed the specific role o
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To date methods for the simultaneous analysis
2020-05-14
To date, methods for the simultaneous analysis of multiple probe drugs in the plasma have been described by using HPLC-DAD or LC–MS/MS. Although previous cocktail methods have used combinations of those four or other probe drugs with LC–MS/MS methods, most of those studies focused on only the analys
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Almost of drugs in the market undergo deactivation though
2020-05-14
Almost 75% of drugs in the market undergo deactivation though oxidation, reduction or hydrolysis by cytochrome P450 (CYP) enzymes, and then, either directly or by facilitated excretion from the body (Guengerich, 2008). The CYP3A subfamily is of particular interest because of its broad substrate spec
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br Thermodynamic modeling br Selection of
2020-05-14
Thermodynamic modeling Selection of data The solutes were selected based on the set of data needed to evaluate the CPA-EoS for prediction of their solubility in CO2 + cosolvent, as shown in Fig. 1. Critical temperatures, melting temperatures and enthalpies of fusion of the solutes are required
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C PHNO has been described as
2020-05-14
[11C]-(+)-PHNO has been described as a full agonist at both D2 and D3 receptors [54,55]. [11C]-(+)-PHNO was initially developed as a PET radiotracer for imaging the high affinity state of the D2 receptor (i.e., highD2) as a means of measuring synaptic dopamine changes in response to pharmacologic ch
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Within the Class II receptors the Type I
2020-05-14
Within the Class II receptors, the Type I IFN receptor subunit, IFNAR-1, is exceptional in having four tandem FNIII domains, denoted here D1–D4. This structure appears to have arisen as a tandem Dryocrassin ABBA receptor of the basic D1/D2 structure; thus, D1 and D3 of IFNAR-1 are more closely relat
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