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Introduction Neuropathic pain occurs in approximately one
2020-10-16
Introduction Neuropathic pain occurs in approximately one-third of patients with diabetes and is refractory to currently available analgesic drugs (Abbott et al., 2011). This painful diabetic neuropathy (PDN) is associated with elevated levels of methylglyoxal (MG; a reactive glucose metabolite) an
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br Substrate Specificity Discrimination and Binding Energy I
2020-10-16
Substrate Specificity, Discrimination, and Binding Energy In Solasodine to catalytic efficiency, which can be gauged in reference to an absolute scale of ‘catalytic perfection’ 10, 11, specificity is a relative concept because it requires comparison between given alternative substrates. In fact,
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Several recent reviews have appeared covering different aspe
2020-10-16
Several recent reviews have appeared covering different aspects of the sPLA2 family of enzymes, including sPLA2-V, and the interested reader is kindly directed to these for specific details [34,[135], [136], [137]]. It is important to remark here, however, that recent studies on sPLA2-V suggest that
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The Acat gene was identified by functional complementation
2020-10-16
The Acat1 gene was identified by functional complementation of a Chinese hamster ovary cell mutant lacking ACAT activity [12]. Unlike most other genes, human Acat1 is located in two different chromosomes, enkephalin 1 and 7, with each site containing a distinct promoter: chromosome 1 contains exons
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br Materials and methods br Results br Discussion
2020-10-16
Materials and methods Results Discussion Endothelial cells are crucial for both vascular homeostasis and protecting the vasculature against atherogenic insults [3]. OxLDL-mediated injury to endothelial cells is crucial for endothelial dysfunction in the pathogenesis of atherosclerosis and a
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br Introduction Rheumatoid arthritis RA is a chronic systemi
2020-10-16
Introduction Rheumatoid arthritis (RA) is a chronic, systemic inflammatory disease that can be divided in at least two subsets based on the presence of antibodies to citrullinated proteins (ACPAs) [1]. Importantly, such ACPA target proteins [[2], [3], [4], [5]] also represent candidate autoantige
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The role of ETB clearing receptors has been
2020-10-16
The role of ETB clearing receptors has been studied in detail in endothelial cell–specific ETB knock-out mice. In these animals, clearance of an intravenous ARRY-380 of labeled ET-1 was reduced significantly compared with wild-type controls. Importantly, functioning ETB were retained on all other c
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In addition to EGFR other receptor tyrosine kinases
2020-10-16
In addition to EGFR, other receptor tyrosine kinases (RTKs) also play roles in the tumor progression under hypoxia, especially hepatocyte growth factor receptor (cMet) (Le et al., 2012). Our data suggested that unlike EGFR, hypoxia had no apparent effect on cMet Fmoc-Val-OPfp (data not shown), sugg
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Gliptins have become a part of
2020-10-15
Gliptins have become a part of various therapeutic regimens to treat type 2 diabetics in recent decades. Gliptins were developed to lower the blood glucose in type 2 diabetes patients and have been shown to be effective [4,5]. More than a dozen gliptins have been developed for the treatment of T2DM,
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The only reported synthesis of the aminobicyclic core
2020-10-15
The only reported synthesis of the aminobicyclic core of is based on bis-alkylation of a 4-amino-5,6-dihydroxypyrmidine with dibromoethane. The likelihood of poor regiocontrol/reactivity in utilizing such a transformation for the synthesis of compounds with a substituent on the dioxinyl ring led us
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br Introduction Cardiovascular disease continues to be the l
2020-10-15
Introduction Cardiovascular disease continues to be the leading cause of death in developed countries. Atherosclerosis, a chronic inflammatory cardiovascular disease, is characterized by the progressive buildup of oxidized low density lipoproteins in the arterial walls (Ross, 1999). In the develo
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CUDC-101 These evidence prompted us to
2020-10-14
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 CUDC-101 (Gu
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br Conclusions Enzyme can be
2020-10-14
Conclusions Enzyme can be delivered to the tumour by using humanised or fully human L-Stepholidine or even loaded into synthetic nanospheres produced from silica [64] or liposomally entrapped [65]. For any future ADEPT developments, a number of basic points need to be considered. As immunogenici
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The Ewing sarcoma breakpoint region gene EWSR is a
2020-10-14
The Ewing sarcoma breakpoint region 1 gene (EWSR1) is a partner in a large, diverse range of mesenchymal (and some nonmesenchymal) tumors (Tables 1 and 2). As the 5′ partner, EWSR1 is able to fuse with an array of genes. These fusions can generate genetically different but phenotypically identical n
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Nitrendipine The liposomes as a FDA approved drug delivery c
2020-10-13
The liposomes, as a FDA-approved drug delivery carrier, have been widely utilized for drug delivery [32], [33], [34]. Liposomes are defined as self-assembled vesicles, which are composed of one or multiple concentric lipid bilayers and enclose an aqueous core. The advantages of utilizing liposomes a
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