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Shikonin represents naphtoquinonic compound isolated from th
2022-04-18

Shikonin represents naphtoquinonic compound isolated from the Chinese plant Lithospermum erythrorhizon[20]. Shikonin treatment inhibits AKT and ERK signaling pathways and induces apoptosis through FOXO transcription factors and mitochondrial pathway [21], [22]. Recent results suggest inhibition of l
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As we showed earlier a to min incubation with
2022-04-18

As we showed earlier [19], a 20- to 30-min incubation with 2mM t-BHP resulted in erythrocyte swelling, which was less in a Ca2+-containing medium. Given that this effect was abolished in the presence of the Gardos channel inhibitor CLT, as well as in media high in K+, we suggested the contribution f
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By using pharmacological treatment with CBX or transgenic an
2022-04-18

By using pharmacological treatment with CBX or transgenic animals lacking the two major astroglial Cxs, the Double KO mouse, we demonstrated that the gap-FRAP technique was able to detect the total inhibition of GJC with a reduction of about 39% and 38% compared to control, respectively. The residua
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While the apparent complexity of gap junction regulation pre
2022-04-18

While the apparent complexity of gap junction regulation presents challenges, new technologies continue to propel the field forward. Advances in microscopy are increasingly able to capture rapid dynamics at the plasma membrane (e.g., biosensors [67] and lattice light sheet microscopy [100]) and to d
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The ultimate success of multimodal probe in the inflammation
2022-04-18

The ultimate success of multimodal probe in the inflammation imaging will be dependent on simplicity in synthesis (combining various modules without protection/deprotection), ease of optimization of pharmacological properties (linker group with tunable PEG moiety), co-registration of macroscopic and
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Introduction Histone is the core component of chromatin
2022-04-16

Introduction Histone is the core component of chromatin and histone modification is one of the key mechanisms of epigenetic regulation (Bannister and Kouzarides, 2011). Amino epigenetics disease residues on histone tails can be modified under different mechanisms including acetylation, methylation
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Betahistine N methyl pyridyl ethylamine is a well known dual
2022-04-16

Betahistine (N-methyl-2-(2-pyridyl)ethylamine) is a well-known dual H1 Murine sale agonist/H3 receptor antagonist with structural resemblance to histamine. Though it has been approved long before the discovery of H3R to treat disorders of vestibular function as Menières-Disease, the evidence for th
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Previous studies have established that phosphorylation
2022-04-16

Previous studies have established that phosphorylation of GC-B is required for activation of GC-B. Conversion of all six chemically determined serine and threonine phosphorylation sites in GC-B to alanines produced a properly folded enzyme that retained GC activity under synthetic detergent activati
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br Conclusion The development discovery of compounds targeti
2022-04-16

Conclusion The development/discovery of compounds targeting small GTPases is challenging [43,44]. Our data point to RBC8 being efficient and potent as a Ral inhibitor in human and mouse platelets, but that it exhibits some activity beyond just Rals, particularly in mouse platelets. It is however
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br Materials and methods br Results Human adipocytes differe
2022-04-16

Materials and methods Results Human adipocytes, differentiated from fibroblastic preadipocytes in culture, were incubated with IL-33 for either 3 or 24 h to examine acute and prolonged responses to the cytokine. Low, medium and high concentrations of IL-33 were employed. IL-33 had no significa
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Several studies have found that GPR possesses a
2022-04-16

Several studies have found that GPR55 possesses a distinct pharmacology from that of CB1 and CB2, and that only certain cannabinoids act at this receptor. In transfected p 00 mg expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, SR141716A (Rimo
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C-type natriuretic peptide (1-22) (human, rat, swine) G prot
2022-04-16

G-protein-coupled receptor (GPCR) ligands can be classified as either orthosteric or allosteric modulators. Orthosteric and endogenous ligands bind to the same site, which is topologically distinct from the allosteric site. In general, the binding domains of different orthosteric ligands may not exa
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The mechanisms of action of
2022-04-16

The mechanisms of action of MMF and DMF are not well understood, but a growing body of evidence has demonstrated that DMF may act on both the neurodegenerative and inflammatory response of MS patients. The majority of the data related to the mechanism of action of DMF/MMF demonstrates the associatio
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The calculations for the R substrate showed that
2022-04-16

The calculations for the R substrate showed that, like the S substrate, the coordination shell of the Zn GSA 10 is more symmetric than in the HIC-SG crystal structure. This symmetry indicates that the enzyme could use the same reaction mechanisms as for the S substrate, but with exchanged roles of G
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The SLC A mutations identified
2022-04-15

The SLC45A1 mutations identified in both families appear to be hypomorphic given that they resulted in a reduction but not abolition of intracellular glucose transport by SLC45A1 in our in vitro assay. It is tempting to speculate that recessive mutations causing a more severe dysfunction of the tran
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