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Introduction The annual global market of industrial enzymes
2021-05-06
Introduction The annual global market of industrial ALW-II-41-27 synthesis is reported to be billions of USD [1], [2], [3], [4], [5], [6], [7], and impacts commercial sectors that include energy, animal feed, household products, food processing and pharmaceuticals [1], [2], [5], [6]. Enzymatic pro
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The synthetic routes to the substrates based on the
2021-05-06
The synthetic routes to the substrates based on the 2,3-dihydroxynaphthalene and 6,7-dibromo-2,3-dihydroxynaphthalene cores are depicted in Scheme 3. A Michael-type glycosylation of 2,3-dihydroxynaphthalene 16a gave the acetylated sugar 17a which was deprotected giving the required β-glucosidase sub
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A key inciting event in atherosclerosis is the deposition
2021-05-06
A key inciting event in atherosclerosis is the deposition of circulating low-density lipoprotein (LDL) in the subendothelial space of major arteries. In the subendothelium, native LDL is no longer protected by circulating antioxidants and is oxidatively modified to oxidized LDL (OxLDL) [5]. OxLDL is
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Compounds and were synthesized according to Reductive
2021-05-05
Compounds and () were synthesized according to . Reductive amination of ethyl acetoacetate with aniline afforded ester . Saponification of followed by intramolecular Friedel–Crafts acylation afforded ketone . Amide formation with benzoyl chloride followed by a reductive amination yielded compound
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The importance of mitochondria as site of aerobic
2021-05-05
The importance of mitochondria as site of aerobic oxidation of metabolic fuels, such as FA, has been recognized for a long time. It has been observed that the number of mitochondria may vary in response to cellular metabolic requirements and hormonal environment (Gao et al., 2014). In order to susta
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br Conclusions CK inhibition protects young and aging
2021-05-05
Conclusions CK2 inhibition protects young and aging WM function against an ischemic episode by preserving oligodendrocytes and axonal structure by maintaining mitochondrial integrity. CK2 recruits CDK5 and AKT/GSK3ß signaling to mediate WM ischemic injury in a differential spatiotemporal manner s
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It is common for plants
2021-05-05
It is common for plants that are deficient in P to invest in their roots in order to maximise P uptake from the soil. Here, plants grown in soil amended with OA had a higher root biomass:shoot meclofenamate ratio compared with plants in the INORG-P treatment. Additionally, greater allocation of C t
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As proof of principle the
2021-05-05
As proof of principle, the effect of selective blockade was measured using TAK-044, a peptide antagonist with approximately 250-fold selectivity for the ETA subtype over ETB as measured by ligand binding in the human heart. A 30-mg infusion over 15 minutes of TAK-044 (providing a serum concentration
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Introduction Protein ubiquitination is a posttranslational m
2021-05-05
Introduction Protein ubiquitination is a posttranslational modification that plays a major role in almost all cellular processes in eukaryotes (Hochstrasser, 2009; Komander & Rape, 2012). It involves the covalent attachment of ubiquitin (Ub) via its C-terminal glycine carboxylate to a primary amine
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Dipeptidyl peptidase inhibitors DPP is or gliptins stimulate
2021-05-05
Dipeptidyl peptidase-4 inhibitors (DPP-4is or gliptins) stimulate both post-meal insulin secretion and inhibit DMOG secretion in a glucose-dependent manner, rendering the risk of hypoglycaemia minimal [10]. They are weight-neutral or may even induce slight weight loss. Their good efficacy has been d
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The human serotonin hydroxytryptamine HT receptor
2021-05-05
The human serotonin (5-hydroxytryptamine; 5-HT) receptor family consists of 14 receptor subtypes to date, which are primarily G protein-coupled receptors (GPCRs) with 5-HT3 being the sole ligand-gated ion channel (Alexander et al., 2017). These receptors are widely distributed in the central and per
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Most of the amino acid residues contacting the substrate are
2021-05-05
Most of the amino dpp-4 inhibitor residues contacting the substrate are within the nucleotide-recognition lid (mauve or magenta in Fig. 4A). Two particularly important residues, W69 and Y76, are conserved in eubacteria and in some but not all of eight human AlkB homologs [52], [76] (Fig. 4B). The tr
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In the course of our program which was aimed
2021-05-05
In the course of our program, which was aimed at developing CRTH2 antagonists for the treatment of allergic diseases, we have been pursuing a new class of potent and selective CRTH2 antagonist lead based on the structures of CRTH2 antagonists known to date (, , ). Using a fused 6–6-membered ring sys
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Data from our in vitro studies using BEAS
2021-05-05
Data from our in vitro studies using BEAS-2B cells showed a biphasic response of cells to NNK. The initial phase of decrease in CRM1 expression in NNK-exposed cells was observed in our previous study. In this study, we further showed that p-p53 (Thr55) expression was also decreased during this initi
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br Clinical trials of CRM inhibitors KPT clinical
2021-05-05
Clinical trials of CRM1 inhibitors KPT-330 clinical trials have been initiated with promising very early results. One trial includes patients with advanced solid tumors whose disease has progressed after at least one prior therapy for metastatic disease (NCT01607905). Another trial includes patie
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