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In order to evaluate the in vivo pharmacology associated
2020-11-14

In order to evaluate the in vivo pharmacology associated with EP receptor antagonism, we wished to discover antagonists presenting a higher degree of selectivity over the other prostanoid receptors. We also wanted to increase the brain–blood ratio since it is probable that centrally mediated EP agon
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The optimization of the lead compound
2020-11-14

The optimization of the lead compound () was initiated and the initial key SAR and the results of the structural modifications of lead compound are summarized in . Replacement of the carboxylic pitavastatin moiety with other functional groups led to loss of functional activity against EP4 receptor
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Exposure to UV instead of DMBA also produced
2020-11-14

Exposure to UV instead of DMBA also produced a sloughing and angiogenic response in transgenic, but not WT, mice, indicating that the epidermis of the BK5.EP4 mice has a much lower apoptosis threshold than WT mice, as suggested by others (Chun and Langenbach, 2007). Overall, these studies suggest th
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The synthetic route chosen for the preparation of
2020-11-14

The synthetic route chosen for the preparation of the substrates 18 is shown in Scheme 3. Commercially available 4-aminobenzyl alcohol 13 was found to be relatively unstable to storage and hence it was prepared immediately before use by reduction of the readily available and inexpensive 4-nitrobenzy
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ap5 br Conflict of Interest br Statement of Authorship br In
2020-11-13

Conflict of Interest Statement of Authorship Introduction Plant endopeptidases are involved in many important biological processes. Recent developments in molecular biological techniques have revealed trace amounts of endopeptidases play essential roles in plant development, turnover of pho
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Concholepas concholepas our model species for
2020-11-13

Concholepas concholepas, our model species for this study, is a marine gastropod found along the Chilean coast that has become commercially important [25], [26], [27]. Until now, the main focus of immunology related to C. concholepas is the production of a novel hemocyanin that has been useful for t
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Currently two approaches can be used
2020-11-13

Currently, two approaches can be used individually or combinedly to overcome weak immunogenicity of subunit Brefeldin A receptor (Bookstaver et al., 2018; Moyle, 2017; Vartak and Sucheck, 2016). The first is to design particulate antigens. Virus-like particles (VLPs), for example—mainly derived fro
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Additionally we analysed the features of apomict
2020-11-13

Additionally, we analysed the features of apomict and sexual Boechera species DNMT proteins. All DNMT proteins showed highly similar theoretical pI, molecular weight and predicted sub-cellular localization (Table 2). Discussion Identification of the structure and expression levels of DNMTs durin
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br Funding br Conflict of interests br Introduction DAG
2020-11-13

Funding Conflict of interests Introduction DAG is generated by the hydrolysis of phosphatidylinositol-4,5-bisphosphate (PtdIns(4,5)P2) by PtdIns-specific phospholipase C (PLC) enzymes [1]. Remaining in the membrane, it binds proteins with cysteine-rich, C1 domains, and activates several of
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This hydrophobic biphenyl tail gave
2020-11-13

This hydrophobic biphenyl tail gave good binding affinity for human DHODH enzyme (IC Posaconazole was found to be the main metabolite in human microsomes and it was 100-fold less active against hDHODH than the ester. In an attempt to identify the specific non-covalent binding interactions which we
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Effect of a C C
2020-11-13

Effect of a C4-C5 double bond — The presence of a double bond at the substrate’s C4-C5 position affects the reactivity of Δ1-KSTDs to varying extent, depending on the enzyme. Most 3-ketosteroids that are converted by Δ1- KSTDs have this double bond. For some Δ1-KSTDs this double bond is even require
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br Introduction Cardiovascular disease continues to be
2020-11-13

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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Although DAPK has been implicated in neuronal death in ische
2020-11-13

Although DAPK has been implicated in neuronal death in ischemic stroke and neurodegenerative diseases, such as Alzheimer’s disease (Shamloo et al., 2005, Duan et al., 2013), the mechanisms about how DAPK regulates cell death are still elusive. In the present study, we investigated the signal transdu
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br Discussion Cytomegalovirus CMV is a herpes virus
2020-11-12

Discussion Cytomegalovirus (CMV) is a herpes virus that causes primary infection in normal hosts and re-activation infection in compromised hosts with impaired CMI, e.g., organ transplants. Following primary infection, which may be severe, CMV becomes latent in lymphocytes. Reactivation may occur
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It should be noted that the long lifetime binding responsive
2020-11-12

It should be noted that the long-lifetime binding-responsive luminescence of ARC-1528 and ARC-1530 becomes evident only upon illumination with radiation at near-UV range where the excitation of ATB or ASB moiety is possible. At higher wavelength range (visible light), the fluorophore (5-TAMRA) can b
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