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A general synthetic pathway to these tricyclic structures is
2022-03-18
A general synthetic pathway to these tricyclic structures is described in (detailed procedures can be accessed in the patent application WO 2011/014520 A2). Benzylation of the appropriate ketoester using KHMDS, followed by treatment with DMF-dimethyl acetal yielded the racemic (dimethylamino)-methy
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LPC OMe LPC LPC and
2022-03-18
LPC 14:0, 2-OMe-LPC 14:0, LPC 16:0 and 2-OMe-LPC 16:0 were shown to be most potent stimulators of intracellular calcium flux in the β cell model, which is one of key processes leading to insulin exocytosis. Yet, species with myristoyl residue initiate calcium influx through voltage-gated CCG 203971
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Several investigators including ourselves have previously sh
2022-03-18
Several investigators including ourselves have previously shown, that allogeneic HLA-DPB1 class II-alleles are powerful leukemia rejection SAR405838 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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Mapping and separation of the anti
2022-03-18
Mapping and separation of the anti-GlyT1C epitopes allowed us to verify the existence of calpain cleavage sites in isolated mouse synaptosomes. In order to allow calcium to enter the intrasynaptosomal compartment and activate endogenous calpain, we incubated synaptosomes in hypoosmotic high (200μM)
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Uracil DNA glycosylase UDG is
2022-03-18
Uracil-DNA glycosylase (UDG) is a highly conserved damage repair enzyme which can specifically recognize and excise uracil residue within the DNA sequences and actuate the DNA fty720 excision repair (BER) pathway which keeps the maintenance of genomic integrity and stability [[21], [22], [23]]. How
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Previous studies have demonstrated that
2022-03-18
Previous studies have demonstrated that cannabinoid potentiation of GlyR α3 subunits contributes to cannabinoid-induced analgesia. For instance, Dehydroxylcannabidiol (DH-CBD), a chemically modified cannabinoid, can alleviate acute pain and chronic inflammatory pain by targeting spinal α3 GlyRs (Xio
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br Dysregulation of glutamate transporter expression and fun
2022-03-18
Dysregulation of glutamate transporter expression and function Aberrant glutamate transporter function and expression are associated with various neurological disorders. Therefore, understanding the underlying mechanisms of EAAT1/2 expression may provide therapeutic targets for treating neurologi
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To directly address whether pharmacological
2022-03-17
To directly address whether pharmacological attenuation of physiological GIP provides therapeutic benefits in obese mice, we pursued a selective long-acting antagonist to complement the work we report on GIPR agonism. We report a GIP analog of sufficient aqueous solubility that employs a shortened N
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There are additional implications of subunit alterations
2022-03-17
There are additional implications of α2-subunit alterations in the hippocampus. P has anticonvulsant activity (Herzog, 1995, Herzog et al., 1997, Herzog et al., 2012, Reddy et al., 2001, Reddy, 2010). These actions result from the metabolic conversion of P to GABA-A receptor-modulating, antiseizure
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Ru II complexes have been reported to be both duplex
2022-03-17
Ru(II) complexes have been reported to be both duplex and G-quadruplex structure stabilizers, and potent anticancer agents [[11], [12], [13], [14]]. Barton, Norden, as well as Ji groups have provided detailed information about recognition and reactions of classical duplex DNA by Ru complexes [[47],
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br Conclusions We concluded that the
2022-03-17
Conclusions We concluded that the inhibitory effects of propofol on fMMYALF-induced neutrophil activation are mediated by competition with FPR1, which inhibits receptor-mediated downstream signaling and inflammatory responses such as oxidative burst, elastase release, and chemotactic migration (F
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To further investigate if GPR was the
2022-03-17
To further investigate if GPR40 was the functional target of these phenylpropiolic e1 activating enzyme analogs, GW-1100, a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells with an IC50 value equal to 1 μM, was used to inhibit agonist-induced intracellular calcium flux [15]. H
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Several transgenic and knockout congenic mouse
2022-03-17
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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We conclude that a combination of GD specific
2022-03-17
We conclude that a combination of GD2-specific CAR T cell therapy with pharmacological EZH2 inhibition deserves investigation as a new therapeutic strategy in EwS and potentially other cancers with heterogeneous GD2 expression, including osteosarcoma, various soft tissue sarcomas, melanoma, lung can
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br Formation of secretory vesicles and trafficking toward
2022-03-17
Formation of secretory vesicles and trafficking toward plasma membrane Insulin and other components of the secretory granules are sorting and providing certain cues for Okadaic acid off the adjacent TGN membrane, forming immature secretory clathrin coated vesicles (Gehart and Ricci, 2013). Bin/A
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