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We have previously designed an azobenzene based molecule
2021-09-28
We have previously designed an azobenzene-based molecule, Razo, which could switch the conformations of G-quadruplex structures by photoregulation. 12, 13, 14, 15 However, it lacks selectivity to different G-quadruplexes. Therefore, we want to find a way to modify this molecule so that it could be u
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MG 149 australia The suboptimal trypsin selectivity profile
2021-09-28
The suboptimal trypsin selectivity profile of DPC423 prompted us to investigate additional P moieties for potency and selectivity. Glycinamide P () showed low nanomolar binding affinity against fXa which suggested that this P moiety sits deeper into the S pocket of fXa. To further elaborate on this
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br Acknowledgment br Introduction Non
2021-09-28
Acknowledgment Introduction Non-steroidal anti-inflammatory drugs (NSAIDs) are widely utilized to treat pain and inflammation [1], but their chronic use is hindered by a variety of potentially serious adverse events that include gastrointestinal (GI) mucosal lesions, bleeding and perforations
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Thus from this preliminary study a working model
2021-09-28
Thus from this preliminary study, a working model of HIV-1 integrase was developed from which a selective inhibitor of the strand-transfer reaction displaying whole-cell activity and negligible cytotoxicity was produced. Compound 9 provides a promising scaffold for further elaboration, and current i
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The H R antagonist JNJ developed
2021-09-28
The H3R antagonist JNJ-17216498, developed by Johnson & Johnson, has entered clinical trial studies, but no information regarding its structure has been publicized to date. A phase II study of JNJ-17216498 monotherapy has been completed for patients with narcolepsy, but the results are not publicall
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Dynasore synthesis Introduction Hedgehog HH signaling regula
2021-09-28
Introduction Hedgehog (HH) signaling regulates development, cell proliferation, and tissue repair [1], [2], [3]. In mammals, HH signaling is activated by 3 ligands: Sonic hedgehog (SHH), Indian hedgehog (IHH), or Desert hedgehog; SHH is the most widely expressed in adult tissues [3]. The primary re
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These to date remain the only
2021-09-28
These to date remain the only two reports of mutations in GC-C found in humans. Perhaps this once again emphasized the critical requirement of the presence of an optimally functional GC-C in the intestine, since neither its loss, nor its hyperactivity, can be tolerated in humans without severe conse
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fluoxetine hydrochloride Moreover we have demonstrated that
2021-09-28
Moreover, we have demonstrated that internalization and subcellular trafficking of NPRA, using IF staining (IFS) and co-IP of plasma membrane, endosomal, lysosomal, and recycling endosome markers to follow intracellular trafficking and signaling by confocal IF microscopy (CIF) and immunoblotting (IB
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br Introduction The replacement of
2021-09-28
Introduction The replacement of a regular intake of healthy oils and fibres for a diet based substantially on high fat- and high sugar-content foods has had profound consequences for public health. These changes in the way that the populations of high income, particularly Western countries, manag
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Docetaxel We recently reported that the human
2021-09-28
We recently reported that the human-derived PancCa cell line PANC-1 and the human-derived hepatocellular HepG2 cell line express GPR55 mRNA and protein [21]. In PANC-1 and HepG2 cells, knockdown of GPR55 with specific siRNAs abrogates cellular uptake of Tocrifluor 1117, a selective GPR55 ligand [21]
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br Materials and methods br
2021-09-28
Materials and methods Results and discussion Conflict of interest Introduction In the presence of continuous and excessive levels of nutrients, adipocytes become hypertrophic and release several pro-inflammatory adipocytokines such as interleukin-6 (IL-6), monocyte chemoattractant protei
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To overcome these limitations investigators have
2021-09-28
To overcome these limitations, investigators have developed novel strategies for identifying and purifying gonadotropes from transgenic mouse models. For example, FSH-producing gonadotropes have been tagged in vivo with a transgenic cell surface antigen (H-2Kk) so that they can be purified in vitro
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br Introduction Edible bird s nest EBN known
2021-09-28
Introduction Edible bird's nest (EBN), known as the health and precious food, is produced from the saliva secretion of several different swiftlet species. Researches have shown the nutritional value of the EBN with the containing of glycoproteins, carbohydrates, essential amino acids, minerals an
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A general synthesis of the tetrazole is shown in
2021-09-28
A general synthesis of the tetrazole is shown in . First, a magnesium-halogen exchange reaction quenched with DMF afforded benzo[]thiophene-5-carbaldehyde , which was further decorated with a bromine at the 3-position (). A Suzuki reaction with -tolylboronic 5-fluorocytosine followed by reduction
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Gap junction intercellular communication GJIC facilitates th
2021-09-27
Gap junction intercellular communication (GJIC) facilitates the exchange of ions, metabolites, Ca2+, inositol phosphates, and/or cyclic nucleotides of up to 1.8 kD in size between Cy3-dCTP through contact-dependent mechanisms [3,4]. Oocyte growth and development (as depicted in Fig. 1) depends, at l
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