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It was then found that TAZ
2022-07-20
It was then found that TAZ, a YAP holomog, binds heteromeric SMAD2/3–4 complexes in a TGF-ß-dependent fashion, and is recruited to TGFβ response elements (Varelas et al., 2008). Knockdown experiments identified TAZ as critical for nuclear accumulation of SMAD2/3/4 complexes in response to TGF-ß, and
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One of the possibilities of HO targeting is gene therapy
2022-07-20
One of the possibilities of HO-1 targeting is gene therapy. So far, the majority of preclinical studies have focused on recombinant adeno-associated viral (rAAV) vectors as DNA carriers. They not only provide stable, long-term transgene expression in non-dividing lfm but also have very limited immu
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However a direct effect of ROS on
2022-07-19
However, a direct effect of ROS on GSNOR has also been described. Inhibition of GSNOR by ROS has been demonstrated for yeast [44], Arabidopsis[36], and Baccaurea ramiflora (Burmese grape) [45] suggesting that this could be a general mechanism of crosstalk between ROS and ·No signaling. Interestingly
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One important aspect about GSK inhibitors is
2022-07-19
One important aspect about GSK-3 inhibitors is their effect on pluripotency of Ramiprilat receptor [4]. Many GSK-3 inhibitors are ATP-competitive and suppress both GSK-3alpha and GSK-3beta [476]. BIO was shown to suppress GSK-3 activity and promote Wnt/beta-catenin signaling. This combination of ev
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As part of our discovery efforts searching for
2022-07-19
As part of our discovery efforts searching for small molecule GPR119 agonists, we analyzed active pharmacophores of known agonists from the literature, and found that -methylsulfonylphenyl and substituted 4-hydroxyl piperidine are common fragments. In our initial efforts, we linked these two fragme
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Boc-D-FMK Several investigators including ourselves have
2022-07-19
Several investigators including ourselves have previously shown, that allogeneic HLA-DPB1 class II-alleles are powerful leukemia rejection Boc-D-FMK for CD4 T-cell therapy following allogeneic hematopoietic stem cell transplantation (Herr et al., 2017, Rutten et al., 2008, Stevanovic et al., 2012)
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In summary we have developed an efficient
2022-07-19
In summary, we have developed an efficient synthetic route to the required urea-isostere containing hydroxamic acid-based inhibitor . The target molecule, , was found to retain the inhibitory potency of the corresponding carbo-analog against glyoxalase-I while possessing resistance to cleavage by γ
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Petrat et al could show
2022-07-19
Petrat et al. could show, that even a low dosage of 10-mg/kg glycine (133 μmol/kg) has a beneficial effect on the small intestine after I/R. In regard to glycine, β-alanine has a clearly higher EC50 to the GlyR and activates the receptor with an efficiency of only 34.6%.16, 17 Therefore, it can be c
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br Transporter based brain targeting nano DDS Drug delivery
2022-07-19
Transporter-based brain-targeting nano-DDS Drug delivery to the central nervous system (CNS) is still challenging due to the bloodbrain barrier (BBB)53., 54.. The BBB is a natural defense barrier protecting the interleukin 1 receptor antagonist from harmful substances. Since only selected, neutr
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factor xa inhibitors Tetrazole is one of the most
2022-07-19
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
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Because of the relationship between carbohydrate consumption
2022-07-19
Because of the relationship between carbohydrate consumption and chronic diseases such as obesity and type II diabetes (Hu, van Dam, & Liu, 2001), there is mounting interest to evaluate the quality of alk pathway through analysis by glycemic index (GI) and Englyst assay, for example (Englyst, Kingm
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Ghrelin is a brain gut peptide
2022-07-19
Ghrelin is a brain-gut peptide hormone secreted from the stomach to stimulate food intake by acting on its receptor, growth hormone secretagogue receptor (GHSR). GHSR is expressed throughout the brain and in NPY/AgRP neurons in the ARC (Cowley et al., 2003, Willesen et al., 1999). Ghrelin-expressing
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br Structures of human secretase Before the near
2022-07-19
Structures of human γ-secretase Before the near-atomic resolution structures, the highest resolutions achieved for γ-secretase were 15 and 12Å [19, 21]. The 15-Å structure revealed a AT13148 chamber in the transmembrane domain and two pores at the top and bottom of γ-secretase, which were specula
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br Acute host defense Inflammation the
2022-07-19
Acute host defense Inflammation, the host response to infection and tissue injury, is crucial for survival and restoration of tissue structure and function. This acute response is mediated and governed by a variety of pro-inflammatory circuits to ensure recognition of invading pathogens, coordina
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The second patient had a
2022-07-18
The second patient had a homozygous substitution within exon 6 (c.538C>T). The parents were heterozygous and showed no clinical or immunological defect. The mutation has been predicted to alter a potential exonic splicing enhancer (ESE) site. Therefore, exon 6 skipping could be explained by the ESE-
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