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Although exhibited high inhibitory activity was found to
2022-03-24

Although exhibited high inhibitory activity, was found to be metabolically unstable due to the hydrolysis of the phosphate group (data not shown), which prompted us to modify the phosphate moiety of . Comparison of the activities between three compounds bearing no or different spacer groups (, , a
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The membrane metalloendopeptidase MME gene is located at hum
2022-03-24

The membrane metalloendopeptidase (MME) gene is located at human chromosome 3q21-27. It encodes a 100-kD type II transmembrane glycoprotein, a widely expressed membrane metalloendopeptidase that degrades a number of substrates. The active site of the enzyme faces the extracellular space. MME is wide
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Subcellular domains where Rac is
2022-03-24

Subcellular domains where Rac is active show limited Rho activity and vice versa (Fig. 4). This distinctive patterning in Rho activity is achieved via the downstream Rac effector Par6, an important part of the so-called Par polarity complex. In primary epithelium, the cytoskeleton and associated Rho
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Lactate LA the end product
2022-03-24

Lactate (LA), the end product of aerobic glycolysis, has been long neglected and seen as a byproduct until recently the findings for its important role in global gene transcription, cancer progression, functional polarisation of immune transferases and the sustenance of stem cells [[7], [8], [9]].
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We first set out to
2022-03-24

We first set out to identify the minimum pharmacophore. Early structure activity relationships (SAR) indicated that the chloro substituents were not required and that the benzisoxazole moiety could be replaced by a number of other groups. A broad survey of “left-hand” hydrophobic moieties was conduc
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In recent large clinical studies AIM
2022-03-24

In recent large clinical studies, AIM-HIGH and HPS2-THRIVE, the additional treatment of nicotinic casein kinase 2 to statin-based LDL-C lowering therapy did not decrease the major vascular events on the patients who had atherosclerotic vascular diseases [43,44]. In the AIM-HIGH study, the secondary
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The global spread and ever increasing incidence of metabolic
2022-03-24

The global spread and ever-increasing incidence of metabolic syndrome over the past few decades has not only categorized it as an ‘epidemic’ but has also dramatically increased the risk of cardiovascular diseases and diabetes. The increase in prevalence of diabetes in the United States alone has bee
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Here we performed TEM and AFM
2022-03-24

Here, we performed TEM and AFM imaging to study APE1–DNA interactions. The results showed that APE1 can dynamically polymerize on DNA in an apparently sequence-independent manner. We propose that this protein polymerization allows for scanning of the structural properties of DNA with short residence
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AFB Fapy dG has been long recognized as a substrate
2022-03-24

AFB1-Fapy-dG has been long recognized as a substrate for nucleotide excision repair [24,25]. However, we recently demonstrated that this lesion is removed by HET0016 excision repair. We showed that DNA glycosylase NEIL1, a member of the Fpg/Nei glycosylase family, could excise AFB1-Fapy-dG from sit
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br Declaration of interest br Acknowledgments br This
2022-03-24

Declaration of interest Acknowledgments This work was supported by grants from the Polish National Science Centre (PRELUDIUM grant no. 2013/11/N/NZ5/00270) and the European Commission FP7 Project Beta-JUDO (grant number 279 153), European Union EIT Health project DeTecT2D, Swedish Diabetes A
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In addition this study also
2022-03-24

In addition, this study also showed no obvious increase in apoptosis but obvious increase in necrosis after WZB117 treatment. The possible reason is that apoptosis is an ATP-utilizing process which is an active and programmed form of cell death. In contrast, necrosis is an uncontrolled or pathologic
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br Acknowledgements This work was
2022-03-24

Acknowledgements This work was supported by the National Institutes of Health [grant number GM024417]. Introduction In mammals, glucose is the major energy substrate supporting conceptus development after Magnolol receptor formation [1,2]. While the equine morula uses similar amounts of pyru
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Medulloblastoma predominantly occurs in infants and
2022-03-24

Medulloblastoma predominantly occurs in infants and children, and is the most-common type of paediatric malignant Ac-DEVD-pNA tumour, accounting for about 20% of all childhood brain tumors [63]. According to cancer genomics, medulloblastoma consists of at least 4 distinct subgroups: Hh driven, Wnt
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br SMO antagonists pitfalls and
2022-03-24

SMO antagonists: pitfalls and limitations The first Hh inhibitor discovered was cyclopamine, a naturally occurring alkaloid isolated from Veratrum californicum[21], which inactivates SMO by directly binding to its hepathelical bundle. Nevertheless, cyclopamine has shown several limitations as a d
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Ertapenem sodium salt Introduction Parkinson s Disease PD is
2022-03-23

Introduction Parkinson's Disease (PD) is a neurodegenerative disease affecting approximately 5–6 million individuals worldwide [1]. This number is expected to escalate to ∼10 million by the year 2030 as the world's population rapidly ages [2]. In the United States, more than 1 million individuals h
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