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br Introduction G protein coupled receptors GPCRs represent
2021-12-02
Introduction G-protein coupled receptors (GPCRs) represent one of the largest family of receptors involved in cell membrane signal transduction and have become one of the leading therapeutic targets worldwide (Chakraborty and Chattopadhyay, 2015; Bouvier, 2001; Sriram and Insel, 2018). GPCRs sign
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br Ghrelin Ghrelin was purified from rat stomach about
2021-12-02
Ghrelin Ghrelin was purified from rat stomach about twenty years ago as a 28-amino fludarabine octanoylated peptide and shown to be the endogenous ligand of the growth hormone (GH) secretagogue receptor (now termed GHSR1a, Howard et al., 1996, Kojima et al., 1999). GHSR1a is a 7-transmembrane re
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Our own search towards aryl
2021-12-02
Our own search towards aryl-imidazole derived GSMs led to the discovery of the benzimidazole derivative (). It is one of the most potent GSMs to date, suffering however from sub-optimal drug-like properties. More recently, we have described the design and synthesis of bicyclic triazolo-derivatives,
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Encouraged by the observation obtained from region A
2021-12-02
Encouraged by the observation obtained from region A, we selected the structure of 1 as the next template to successively pursue the SAR on regions B-D of 1 (lower side of Fig. 2). Next, we turned attention to the external aromatic ring of 1 to verify the impact on the antagonistic activity and prep
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LPCs have been previously described as potential anti diabet
2021-12-02
LPCs have been previously described as potential anti-diabetic factors due to stimulation of secretory activity from the isolated rodent pancreas, L-type cells, ands insulin-producing cell lines, with LPC 18:1 as the main structure of interest (Soga et al., 2005, Sakamoto et al., 2006, Overton et al
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Finally the optimized leads and were
2021-12-02
Finally, the optimized leads (−)- and (−)- were tested in rat model of CIPN (3 and 30 mg/kg, po, qd, administered for 7 days) and the results have been shown in . Under acute set up, after single oral administration at 30 mg/kg, both the compounds exerted significant improvement of the NP condition
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br Materials and methods br Results br Discussion I have
2021-12-02
Materials and methods Results Discussion I have identified an alternative transcript of the integrin αE gene that is abundantly expressed in testis. In humans, this transcript (hAED) includes part of intron 26 and exons 27, 29, 30, and 31 of the conventional αE gene and Northern analysis in
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Ertapenem sodium salt br Brief overview of GSK
2021-12-02
Brief overview of GSK-3 inhibitors We will briefly summarize some of the key aspects about GSK-3 inhibitors. Additional details of GSK-3 inhibitors in clinical trials have been recently reviewed [5]. GSK-3 is a complicated target as it is involved in many biological processes from neurology, diab
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While the specific set of
2021-12-02
While the specific set of challenges associated with deorphanization and transforming each poorly characterized GPCR into a useful drug target will be unique, much can be learned by considering how these issues have been addressed for other receptors. One group of poorly characterized GPCRs that hav
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The top concern for the clinical use of CRISPR
2021-12-02
The top concern for the clinical use of CRISPR-Cas9 technology is safety. Off-target alterations must be avoided to ensure genome integrity and proper cellular function. WGS found no off-target effects among the top 49 predicted off-target sites. WGS did find 4,658 indels and 1,891 SNVs in sgRNA1/2-
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Injury to oligodendrocyte progenitors caused in part by glut
2021-12-01
Injury to oligodendrocyte progenitors caused in part by glutamate contributes to the pathogenesis of myelination disturbances in PVL [5]. In the immature human brain, the susceptibility of developing oligodendrocytes to hypoxia-ischemia correlates with their expression of glutamate receptors of the
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N Cadherin facilitated gap junction formation
2021-12-01
N-Cadherin facilitated gap junction formation between embryonic lens Cabazitaxel sale by stabilizing membrane appositions (Frenzel and Johnson, 1996). Cx43 has been found to be delivered to N-Cadherin-positive membrane HeLa cells (Shaw et al., 2007), and N-Cadherin determine the localization of Cx4
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br Materials and methods br Results br Discussion Although
2021-12-01
Materials and methods Results Discussion Although homologues of the β-galactosidase gene were known to exist in the Xenopus genome, and SA-β-gal activity has been detected in whole-mount Xenopus embryos by histochemical staining (Davaapil et al., 2017), no reports have been presented so far
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WT associated protein WTAP a nuclear
2021-12-01
WT1 associated protein (WTAP), a nuclear protein, is first identified by Little [6] who noticed its specific interaction with WT1. Besides several essential physiological processes, such as mRNA stabilization [7], eye development [8], m6A methylation [9], mRNA alternative splicing [10] and LFM-A13
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DLS only provides a Z average size based
2021-12-01
DLS only provides a Z-average size based on spherical model, hence the size of nanorods was determined as 300 nm by DLS measurement. However, the size of length is nearly 400 nm while width is about 100 nm, which was clearly observed by transmission electron microscopy (TEM) (D). Meanwhile, the TEM
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