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The regulation of gap junction connexin
2022-03-17
The regulation of gap junction-connexin-mediated activities may be achieved through action on the channel gating properties (membrane voltage, pH, interaction with junctional and cytoskeletal proteins, Ca2+ and K+ concentrations, etc) or on the trafficking, turnover and localization of connexins. Sh
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br Learning from our ancestors As mentioned earlier homologu
2022-03-17
Learning from our ancestors As mentioned earlier, homologues of all γ-secretase components have been identified in plants and protozoans, some of which have emerged as model systems for the study of γ-secretase independent functions of the presenilins [27]. The moss P. patens was the first plant
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Herein exploiting several spectroscopic techniques i
2022-03-17
Herein, exploiting several spectroscopic techniques, i.e. CD, UV and NMR, along with gel electrophoresis, size exclusion chromatography and in silico prediction analysis, the conformational behaviour of R1.2 and R1.3 was studied in Na+- and K+-rich solutions, which mimic the extra- and intracellular
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Some malignant human tumors cells also express
2022-03-17
Some malignant human tumors olopatadine hcl also express FPRs and respond to bacterial or endogenous agonists by increased motility and growth. For instance, FPRs expressed by human gastric cancer cells, mediate epithelial–mesenchymal transition, cell proliferation, migration, and resistance to apo
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Akt mTOR signaling pathway is a major
2022-03-17
Akt/mTOR signaling pathway is a major negative regulator of autophagy, via modulating ULK1 complex. It is well established that Inhibition of mTOR by deprivation of nutrients or growth factors, led to dephosphorylation of ULK1, ULK2, and Atg13 in human cells, which is a key step for ULK1 complex ass
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br FREE FATTY ACID RECEPTOR GPR br G PROTEIN COUPLED
2022-03-17
FREE FATTY ACID RECEPTOR 1 (GPR40) G-PROTEIN-COUPLED RECEPTOR 120 CONCLUSION Free fatty gallamine receptors whose natural ligands are identified as FFAs having various lengths have been reported. They act as novel nutrient sensing receptors independent of PPARs and FABPs, and they are know
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The suboptimal trypsin selectivity profile
2022-03-17
The suboptimal trypsin selectivity profile of DPC423 prompted us to investigate additional P moieties for potency and selectivity. Glycinamide P () showed low nanomolar binding affinity against fXa which suggested that this P moiety sits deeper into the S pocket of fXa. To further elaborate on this
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In the course of an
2022-03-17
In the course of an internal FAAH, program,, , , , , , , , , , , , , many very similar compounds were profiled in vivo with particular interest paid to their ability to penetrate the BBB. The compounds profiled were heteroaryl piperazinyl and piperadinyl ureas; a class of compounds, reported on pr
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In spite of decades of research the mechanisms of SV
2022-03-17
In spite of decades of research the mechanisms of SV endocytosis and recycling remain controversial. Accumulating evidence suggests that SV endocytosis occurs by more than one mechanism (e.g. clathrin-independent endocytosis, clathrin-mediated endocytosis, bulk endocytosis; reviewed in (Dittman and
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H O induced astrocyte ATP release through lysosome exocytosi
2022-03-17
H2O2 induced astrocyte ATP release through lysosome exocytosis. The LDH assay and electric microscope results indicated that the increase of extracellular ATP concentration was not due to the cell rupture, but the alternations in cell activities. In addition, when lysosome exocytosis was blocked by
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Whether histamine receptor distribution is altered in canine
2022-03-17
Whether histamine receptor distribution is altered in canine GI diseases remains unknown, but human research has documented altered histamine receptor density in certain GI diseases (Sander et al., 2006, Deiteren et al., 2015, Von Rahden et al., 2011). Additionally, a novel H4 receptor antagonist, J
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The presence of the H
2022-03-17
The presence of the H3 receptor in humans was confirmed approximately 25 years ago, and the receptor was successfully cloned in 1999 (Thurmond, 2010). The H3 receptor is unique, as it controls feedback of histamine release, particularly in the central nervous system, where it modulates neurotransmit
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Dual H H receptor antagonists developed by GlaxoSmithKline
2022-03-17
Dual H1/H3 receptor antagonists developed by GlaxoSmithKline have also reached clinical trials at various stages. These candidates are useful for alleviating the symptoms associated with allergic rhinitis(Daley-Yates et al., 2012). GSK-1004723, 4-[(4-chlorophenyl)methyl]-2-( (2R)-1-[4-(4- [3-(hexahy
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br Prostaglandins meet Hippo The prostaglandins lie
2022-03-17
Prostaglandins meet Hippo The prostaglandins lie at the crossroads between inflammation, regeneration and tumorigenesis (Figure 3). Prostaglandins are synthesized from archidonic Fmoc-D-Phe(4-Cl)-OH mg by Cox1 and Cox2 enzymes [40, 41] and in the gut, prostaglandin E2 (PGE2) protects against DSS-
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In conclusion re evaluation of HER status
2022-03-17
In conclusion, re-evaluation of HER2 status is necessary to determine the appropriate use of anti-HER2–targeted therapy beyond disease progression. EGFR and c-met amplification, as well as PIK3CA mutation, are rarely associated with acquired resistance. Our results highlight the importance of forma
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