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In addition several other considerations were made for the o
2022-03-07

In addition, several other considerations were made for the optimization exercise. While the structural features of the endogenous ligands for long-chain fatty SL 0101-1 receptors suggest obtaining orthosteric agonists with drug-like properties may be challenging, the optimization efforts were com
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Tetrazole is one of the most commonly used bioisosteres
2022-03-07

1-Tetrazole is one of the most commonly used bioisosteres for carboxylic acids arising from their similarity in pKa (ca. 4.5–4.9 vs 4.2–4.4, respectively)., Metabolically, tetrazoles may exhibit an advantage over carboxylic acids because they form -glucuronides which are not as chemically reactive a
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A breakthrough in the understanding
2022-03-07

A breakthrough in the understanding of the unique properties of GPX4-downregulation-induced cell death was accomplished when Seiler et al. in 2008 demonstrated the role of 12/15-lipoxygenase (12/15-LOX), a polyunsaturated fatty Imipenem australia metabolizing enzyme [92], in the execution of GPX4-k
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Neuregulin/Heregulin-1β (NRG-1β/HRG-1β), human recombinant p
2022-03-07

Although ALPS type 0 is very rare with few published cases, we herein report the clinical and immunogenetic characteristics of two additional unrelated patients from highly inbred North African population. Both patients present two rare splicing defects mechanisms in FAS gene inducing the skipping o
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ADAM has two alternative splicing forms
2022-03-07

ADAM12 has two alternative splicing forms, a membrane-anchored long form (ADAM12-L) and a secreted short form (ADAM12-S). Both the long and short forms have metalloproteinase, disintegrin, cysteine-rich, and epidermal growth factor-like domains and can shed pro-heparin binding-epidermal growth facto
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A biochemical characterisation of this functionally crucial
2022-03-07

A biochemical characterisation of this functionally crucial LSD1-p53 interaction is the focus of this study. Using several complementary assays [29], [30], [31], [32], we find that a well-defined segment of p53-CTD is capable of binding to LSD1 active site, thereby inhibiting the enzymatic activity
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It is difficult however to assure that observed
2022-03-07

It is difficult, however, to assure that observed alterations of pro-oxidant/antioxidant levels within the studied organisms are related directly to heavy metal pollution, rather than to other accompanying environmental stressors. Environmental factors like oxygen partial pressure, temperature, sali
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Prolonged sGC oxidative inhibition occurs in
2022-03-07

Prolonged sGC oxidative inhibition occurs in many diseases [46,[86], [87], [88]]. Keeping sGC membrane-bound and functional under conditions of high oxidative stress requires a mechanism for restoring oxidized sGC (Fe3+) heme iron to its reduced (Fe2+) state. Without this redox regulation, the sGC e
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The beta catenin TCF complex
2022-03-07

The beta-catenin/TCF complex is an important target in the Wnt/beta-catenin pathway. This complex has proven challenging to target. However, natural inhibitors of this complex have been identified. One group of inhibitors is called the inhibitors of Wnt response (IWR-1/2). IWR-1/2 targets Axin and s
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A few research articles described that PLGA could alone impr
2022-03-07

A few research articles described that PLGA could alone improve physiological activities in certain illnesses by exerting therapeutic effects. These reported therapeutic activities of PLGA can be appended to the hydrolysis products of PLGA lactate, glycolate, and H+. We will recapitulate their respe
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AY 9944 dihydrochloride br Author contributions br Acknowled
2022-03-07

Author contributions Acknowledgements The work was financially supported by a grant from the Investigator-Initiated Studies Program (Ref. #38124) from Merck Sharp & Dohme, and, in part, from Research Grants Council of the Hong Kong Special Administrative Region, China (Ref. No.: 14110314), awa
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Adenosine triphosphatase ATP is a signaling molecule in
2022-03-07

Adenosine triphosphatase (ATP) is a signaling molecule in acute pain and chronic pain(Burnstock, 2009, Burnstock, 2013, Burnstock, 2014, Chizh and Illes, 2001). It is also known that presynaptic A1 receptors are involved in the inhibition of transmitter release (Vizi and Knoll, 1976). Extracellular
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Previously localization studies have been conducted
2022-03-04

Previously, localization studies have been conducted using antibody-based detection of Pgp protein in tissues of Clade V nematodes. In transgenic C. elegans, Cel-Pgp-3 and Cel-Pgp-1 proteins localized to the apical membranes of the excretory and intestinal cells and the anterior pharynx (Broeks et a
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In the present study Trichoderma viride glucosidase
2022-03-04

In the present study, Trichoderma viride β-glucosidase was screened in our laboratory and used for the synthesis of gentiooligosaccharides via reverse hydrolysis and transglycosylation. Material and methods Results and discussion Conclusions In the present study, the T. viride β-glucosidas
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Further we examined the degradation
2022-03-04

Further, we examined the degradation of Cx43. Autophagy and the proteasome system have previously been implicated in Cx43 degradation (Falk et al., 2014). DEX inhibited communication between Fenretinide by promoting the degradation of Cx43 through autophagy in osteocytes (Gao et al., 2016). In our
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