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It appears that different agonists for GPR activate differen
2022-07-08
It appears that different agonists for GPR55 activate different signalling pathways [25]. GPR55 activation through LPI has been shown to trigger ERK 1/2 phosphorylation 22, 23, 25, 33. Conversely, endogenous cannabinoid compounds AEA and 2-AG have been shown to have no effect on ERK 1/2 signalling 2
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MG 149 ATP as a transmitter can be
2022-07-08
ATP as a transmitter can be released from injured MG 149 and sensory nerve endings (Sperlágh et al., 1995, Sperlágh et al., 1997, Sperlágh et al., 1998, Burnstock, 2013, Burnstock, 2014). ATP can activate the P2X3 receptor in the DRG neurons (Gao et al., 2011a; Xu et al., 2012). In DRG neurons cult
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We first investigated the influence
2022-07-08
We first investigated the influence of the -acyl group of the glycine amide side chain and found that shorter linkers lead to better activities (–); simple -benzoyl substituents were always superior to the 3-arylpropanoyl group present in the high-throughput hit (). Electron withdrawing substituents
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Fmoc-Phe-OH A general synthesis of the
2022-07-08
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 Fmoc-Phe-OH followed by reduction of th
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Until now various reports have
2022-07-07
Until now, various reports have demonstrated the therapeutic potential of enzyme-resistant forms of GIP in experimental diabetic animal models , , . In essence, structural modifications performed at the Tyr residue in GIP generate analogues that are completely resistant to the actions of DPP-IV and
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br Acknowledgements This work was supported
2022-07-07
Acknowledgements This work was supported by grants of the Argentine National Research Council (CONICET, PIP 0662). The authors express their appreciation to the Transmission Electron Microscopy Service (MET) of the Faculty of Veterinary Medicine of the National University of La Plata (Argentina)
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In addition to attenuating joint inflammation via T cells
2022-07-07
In addition to attenuating joint Cinchonidine via T cells, Cpd43 could also decrease the severity of CIA/AIA by suppressing the function of innate leukocytes such as neutrophils and macrophages via FPRs, as has been shown in other acute inflammatory models including neutrophil/macrophage-mediated K
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It is considered that activations of MMP
2022-07-07
It is considered that activations of MMP-2 and MMP-9 are closely related to progression process of cancer cells, such as invasion and metastasis [22], [23]. In fibrosarcoma cells, GPR40 suppressed not only MMP-2 and MMP-9 activations, but also cell motile and invasive activities, suggesting GPR40 ne
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Through the analysis of various synthetic
2022-07-07
Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic BOP reagent sale motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of discover
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Sumoylation is involved in regulating protein protein
2022-07-07
Sumoylation is involved in regulating protein-protein interactions, subcellular protein localization, protein stability, and transcriptional factor activity (reviewed in [29]). The small ubiquitin-like modifier (SUMO) protein is covalently attached to a lysine residue in a Ψ-K-X-D/E consensus sequen
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Evidence suggests that phosphorylation increases synaptotagm
2022-07-06
Evidence suggests that phosphorylation increases synaptotagmin affinity for the SNARE complex [15], [128]. It is, however, unclear how this might affect release. Synaptotagmin has been identified as part of the minimal vesicle docking machinery in chromaffin TTNPB [129]. Thus, phosphorylation of sy
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The finding that a peptide consisting of d amino acids
2022-07-06
The finding that a peptide consisting of d-amino acids binds to LSD1-CoREST1 with equal affinity as the l-amino tolbutamide mg ligand indicates that the assays detect a generally non-specific association between two highly charged molecules. Nonetheless, p53-CTD is an effective inhibitor of LSD1 an
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br Methods br Involvement of HO in rheumatic diseases br
2022-07-06
Methods Involvement of HO-1 in rheumatic diseases Therapeutic strategy targeted HO-1 Based on the researches focusing on the effect of HO-1 in rheumatic diseases, amount of approaches targeting regulation of HO-1 have been arising (See Table 1 for summary). It has been shown that different
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It would also be interesting to understand the
2022-07-06
It would also be interesting to understand the potential connection between asymmetric histone inheritance and another phenomenon reported by several investigators: selective DNA strand segregation (reviewed by Evano and Tajbakhsh, 2013, Rando, 2007, Tajbakhsh and Gonzalez, 2009). Recent development
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Protein structures determined in high resolution
2022-07-06
Protein structures determined in high resolution by X-ray crystallography and NMR techniques provide wealth of structural information on intra-domain and inter-domain protein interactions of small sized proteins. In addition, cryo-EM often provides low resolution structures of multi-component protei
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