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Based on these findings we set out to identify
2022-05-11

Based on these findings, we set out to identify GPR109A agonists capable of biasing the receptor's signaling towards the functional anti-lipolytic and presumed therapeutic response, and away from the flushing side-effect pathways. Indeed, using recombinantly expressed GPR109A, two classes of compoun
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Analogous to all GPCRs the GLP R transduces
2022-05-11

Analogous to all GPCRs, the GLP-1R transduces signals from the outside of the cell to the inside by allosterically converting a ligand-binding event to activation of intracellular effectors. The GLP-1R couples to several intracellular effectors and this pleiotropic coupling is physiologically releva
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All models used here rely
2022-05-11

All models used here rely on WT FGFR3, which is activated by exogenous FGF ligand to alter chondrocyte proliferation and differentiation. This approach toward modeling the aberrant FGFR signaling in cartilage differs from the actual situation in ACH or TD, where the chondrocytes are exposed to long-
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Interestingly the subcellular localization of FBPase
2022-05-11

Interestingly, the subcellular localization of FBPase in hepatocytes and proximal tubule XMD17-109 sale reveals that FBPase is also able to translocate to the nucleus in these cell types. The nuclear localization of muscle-FBPase was recently reported [35]. This data corroborate our results on the
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Cyclophosphamide monohydrate br Nanoscale Cortical Actin Rem
2022-05-11

Nanoscale Cortical Actin Remodeling in Regulated Exocytosis The network of cortical Cyclophosphamide monohydrate is formed by numerous fine actin filaments, which are only about 10nm in diameter [52]. Although the microscale role of the cortical actin network in vesicle exocytosis is well establ
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br Hh Proteins at a Glance Hh family
2022-05-10

Hh Proteins at a Glance Hh family proteins are evolutionarily conserved morphogens that provide cells with positional information and fate instruction during early embryonic development. After development, Hh ligands contribute to tissue homeostasis and wound healing 1., 2.. Consistent with these
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br Concluding Remarks and Future Perspectives Our understand
2022-05-10

Concluding Remarks and Future Perspectives Our understanding of substrate targeting mechanisms utilized by kinases has grown tremendously in the past few years, but challenges still remain in relating these mechanisms to the organization of complex signaling networks. Substrate prediction based o
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PBIT In summary we obtained and type of linaclotide by
2022-05-10

In summary, we obtained - and -type of linaclotide by protein chemical synthesis and acquired the X-ray crystal structure of linaclotide for the first time through racemic crystallization technique. The structure of linaclotide forms a compact spatial structure containing three- turns through three
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Atovaquone receptor TRAPP Transport Protein Particle complex
2022-05-10

TRAPP (Transport Protein Particle) complexes share a common core architecture and function in Atovaquone receptor and autophagy (Kim et al., 2016). In yeast, the core complex has GEF activity for the Rab1 ortholog Ypt1. The larger TRAPPII and III complexes include regulatory subunits implicated in
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It has been indicated that chemicals induced mammalian cell
2022-05-10

It has been indicated that chemicals-induced mammalian cell death is mediated by GSK-3 activation (by downregulated of GSK-3 phosphorylation) leading to apoptosis (Huang et al., 2014, Li et al., 2014, Tanabe et al., 2011, Yun et al., 2009). In contrast, accumulating evidences have reported that the
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It has been proposed that
2022-05-10

It has been proposed that HCA1 may be a better target than HCA2 to treat dyslipidemia and to prevent progression of atherosclerosis, because HCA1 is less widely expressed, and HCA1 activation does not result in flushing. However, since the antilipolytic effects mediated by HCA2 appear to be not the
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T L cells can be induced to differentiate
2022-05-10

3T3-L1 cells can be induced to differentiate into adipocytes by the appropriate hormonal treatment and they offer a useful in vitro model system for adipogenesis. GPR120 mRNA was detected in differentiated mature adipocytes but not in confluent preadipocytes (Fig. 3A). The level of GPR120 mRNA incre
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In conclusion GPR inhibits and GPR enhances the cell motile
2022-05-10

In conclusion, GPR120 inhibits and GPR40 enhances the cell motile activity stimulated by TPA in melanoma cells, while MMP-9 activation was reduced by GPR40. In contrast, GPR40 negatively regulated cellular functions of fibrosarcoma GSK1016790A [11]. Taken together, it is suggested that opposite eff
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For some agonists these stable GPR responses
2022-05-10

For some agonists, these stable GPR119 responses were resistant to washing. Thus, sustained activation could continue, for at least a number of hours, even after removal of free agonist. These data are consistent with reports for other GPCR systems that do not desensitize (Calebiro et al., 2009, Fer
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GW was also the starting point
2022-05-10

GW4064 was also the starting point for a study by an independent research group. The co-crystal structure of GW4064 with FXR suggested the potential for favorable hydrogen bond interactions between the isoxazole 3-aryl group and several receptor residues such as Tyr373 and Ser336. Replacing the 2,6-
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