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br Material and methods br
2022-05-07

Material and methods Results Discussion Neurosteroids capable of blocking the NMDAR channel attract a lot of attention as possible therapeutic agents for the treatment of neurodegenerative diseases. A large number of new RG108 with different structures have been synthesized in order to crea
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br NMDA receptor LBDs The
2022-05-07

NMDA receptor LBDs The study of GluA2 was later expanded to include NMDA receptors [22]. NMDA receptors are obligate heterotetramers that are composed of two glutamate-binding subunits and two glycine-, or d-serine-, binding subunits. In this study, crystal structures of the NMDA receptor glycine
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In summary this study demonstrated
2022-05-07

In summary, this study demonstrated the cDNA cloning and characterization of the galanin type II receptor (GalR2) and a novel GalR2-like receptor (GalR2-L) in chickens, in which these two receptors are possibly originated from a gene Metaphit mg event that occurred in the early vertebrate lineage.
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Moreover intestinal chronic inflammation is
2022-05-07

Moreover, intestinal chronic inflammation is a promoting factor in the development of CRC in patients affected by inflammatory bowel disease (IBD), such as Crohn's disease and ulcerative colitis. We have previously shown that pharmacological FXR activation via its ligand obeticolic ER 27319 maleate
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To investigate an involvement of GPR and GPR
2022-05-07

To investigate an involvement of GPR120 and GPR40 in the enhancement of cell motile activity of MG-63 cells, highly migratory (MG63-R7) Fmoc-D-Phe(4-Cl)-OH synthesis were established from MG-63 cells (Fig. 2A). The expression level of GPR120 gene was significantly higher in MG63-R7 cells than in MG-
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Several transgenic and knockout congenic
2022-05-07

Several transgenic and knockout/congenic mouse models have been generated in order to assess the role of FFAR1 for proper insulin secretion and maintenance of glucose homeostasis. The results obtained with three different receptor knockout mouse models were not consistent. The protection against hig
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ATN Ac PHSCN NH is a small
2022-05-07

ATN-161 (Ac-PHSCN-NH2) is a small peptide antagonist of integrin α5β1, a recently developed anticancer drug that interacts with the N-terminus of the β1 region of integrin α5β1 to lock integrin α5β1 in its non-activated conformation (Wang et al., 2016). The drug has been tested in Phase 2 clinical t
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br What are the local exocytotic protein targets of
2022-05-06

What are the local exocytotic protein targets of PKC? A direct method for PKC to potentiate insulin release would be to phosphorylate and activate components of the exocytotic machinery. Bulk measurements show that potentiation occurs by enhancement of the calcium sensitivity of exocytosis [56],
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Over the last decade intense efforts
2022-05-06

Over the last decade, intense efforts have been devoted toward identifying IN inhibitors as potential drugs against HIV. Raltegravir and elvitegravir are integrase strand transfer inhibitors (INSTIs) that have been approved for therapy and dolutegravir is another INSTI that is currently in advanced
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It is well known that histamine functions not
2022-05-06

It is well known that histamine functions not only as an inflammation mediator but also as an aminergic neurotransmitter or neuromodulator. Histaminergic neurons [27], [28] and histamine receptor subtypes (H1R [29] and H3R [30]) are widely existed in mammalian central olfactory system. Histamine reg
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To date several studies have suggested that
2022-05-06

To date, several studies have suggested that serum HER2 could be used as a biomarker for monitoring the disease course and the patient's response to therapy [110], [111]. However, the clinical usefulness of serum HER2 has not been fully validated because of conflicting data [31]. The enzyme-linked i
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Based on pharmacophore modeling a
2022-05-06

Based on pharmacophore modeling, a good HDAC inhibitor has at least three sides/regions: the attachment side of the Zn2+ cofactor/HDAC active site (Zn2+ binding group/ZBG), hydrophobic cap (CAP) and linker containing connecting unit (CU) with electronegative groups (Mohan et al., 2011, Rossi et al.,
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Analysis of the thermosensory responses
2022-05-06

Analysis of the thermosensory responses conferred by chimeric proteins suggests that both the ECD and ICD of AFD-rGCs contribute to their thermoresponsive properties. The presence of the GCY-18 or GCY-23 ICD and TMD in chimeric protein combinations generally corresponds to a higher or lower , respec
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One important aspect about GSK
2022-05-06

One important aspect about GSK-3 inhibitors is their effect on pluripotency of NU 9056 [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 events preserve
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br Introduction Human immunodeficiency virus HIV is a retrov
2022-05-06

Introduction Human immunodeficiency virus-1 (HIV-1) is a retrovirus that primarily infects components of the human immune system, such as CD4+ T cells, macrophages and dendritic hippo signaling pathway (Clapham and McKnight, 2001). HIV directly and indirectly destroys CD4+ T cells, which leads t
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