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One strategy which is different from the above is
2020-10-28
One strategy which is different from the above is to isolate a similar enzyme to the one under study which will not be recognized by the antibody of the original protein. This approach will lead to prolonging an enzyme’s activity. For example, a novel variant of Carboxypeptidase G2 (CPG2), which has
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P H is a nonheme
2020-10-28
P4H is a nonheme iron(II) dioxygenase that uses O2 and α-ketoglutarate as co-substrates (Fig. 1A). The three-dimensional structure of mammalian P4H is unknown. We reasoned that an electrophilic analog of α-ketoglutarate could serve as an irreversible inhibitor of the enzyme and, hence, a useful prob
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Accumulated evidence indicates that apelin plays a protectiv
2020-10-28
Accumulated evidence indicates that apelin plays a protective role in ischemic stroke, contributing to post-stroke recovery (Yang et al., 2014; Chen et al., 2015; Xin et al., 2015; Yan et al., 2015). Apelin gene (APLN) encodes prepro-apelin with 77 amino acids, while the C-terminal 23 PF 04418948 a
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In recent years there has
2020-10-28
In recent years, there has been much interest within the endothelin community regarding the possibility that ETA and ETB receptors may form homo- and heterodimers. Heterodimerization of endothelin receptors may provide an explanation for the results mentioned in the previous paragraph and might also
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Adding MPA or NETA we found no impact
2020-10-28
Adding MPA or NETA we found no impact on the estradiol-induced downregulation of serum-stimulated endothelin synthesis in vitro [40]. Progesterone was also able to inhibit the angiotensin II-induced increase in endothelin production [41]. Several clinical studies on the effect of oral or transdermal
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Introduction Neuropathic pain occurs in approximately one th
2020-10-28
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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A number of chemical strategies have been developed to
2020-10-28
A number of chemical strategies have been developed to design activatable optical imaging probes and have been summarized in several excellent reviews 11., 12., 13., 14., 15.. Fluorogenic enzyme substrates are one of the most explored activatable probe types for enzyme detection. These probes contai
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SR 49059 synthesis To further define the importance
2020-10-28
To further define the importance of CYP3A for OSC metabolism in vivo, a strong CYP3A inhibitor ketoconazole was used to test whether CYP3A would affect its metabolism. As expected, the biotransformation of OSC to SC was significantly decreased by ketoconazole at all three substrate concentrations. H
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XL184 br RING dimerization RING type domains
2020-10-28
RING dimerization RING-type domains are found in many different structural contexts. While many exist as single-chain XL184 (Fig. 3A), a notable feature of RING-type E3s is their tendency to form homodimers and heterodimers (Fig. 3C–F). Homodimeric RING-type E3s include cIAP, RNF4, BIRC7 (shown
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However a two receptor model presents a mystery
2020-10-28
However, a two-receptor model presents a mystery of how MBns know whether they are receiving an acquisition or forgetting signal from the PPL1 DAns. The most attractive explanation for this is that the two receptors might have different signaling properties and mobilize distinct signaling cascades.
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br Acknowledgement This study was supported by Vetenskapsr d
2020-10-28
Acknowledgement This study was supported by Vetenskapsrådet, Sweden (Grant 2017-02918). Introduction Soybean is a major source of protein and oil used for food and feed, as well as for the production of industrial products like lubricants and hydraulic fluids (Choudhary and Tran, 2011; Hsien,
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BMH-21 The on target in vitro pharmacology
2020-10-27
The on target in vitro pharmacology of 18 was then further explored, first in respect of murine CRTh2 receptor activity (Table 5), where similar levels of activity were found in both a binding and functional assay compared with the human orthologue, consistent with our earlier observations in the su
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Magnified regions of the upregulated proteins identified by
2020-10-27
Magnified regions of the upregulated proteins identified by MALDI-TOF are shown in Fig. 2. The identified proteins were phosphoglycerate kinase, fructose-bisphosphate aldolase class II, alcohol dehydrogenase, phosphoglyceromutase, 6-phosphogluconolactonase, malate dehydrogenase, alkyl hydroperoxide
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Phenylbenzofurans are a very important molecule skeleton due
2020-10-27
Phenylbenzofurans are a very important molecule skeleton due to their synthetic versatility and their proved pharmacological properties [2]. They are synthetic compounds in which an additional phenyl ring is present in any position of the benzofuran nucleus. This could be easily obtained possible by
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Curcumin is a polyphenol extracted from turmeric which is co
2020-10-27
Curcumin is a polyphenol extracted from turmeric, which is commonly used as a spice and food-coloring agent in many cultures [9]. Curcumin possesses anti-inflammatory, antioxidant, and cancer-preventive properties [10], [11], [12]. In addition to these well-known effects, consuming curcumin may bene
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