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Another mechanism underlying on the toxicity of dopaminergic
2019-08-19

Another mechanism underlying on the toxicity of dopaminergic neurons might be related to dopamine-dependent initial oxidative stress [60]. Dopamine glycosylase inhibitor mediated by monoamine oxidase (MAO) can produce hydrogen peroxide as a by-product, and excess dopamine can undergo auto-oxidation
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Diacylglycerol kinases DGK and are lipid kinases
2019-08-19

Diacylglycerol kinases (DGK) α and ζ are lipid kinases that limit diacylglycerol (DAG)-dependent activation pathways downstream of the TCR (Merida et al., 2015). Their upregulation in tumor infiltrating lymphocytes (TIL) has been linked to generation of hyporesponsive states that contribute to immun
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Keratin K has been identified as
2019-08-19

Keratin 8 (K8) has been identified as the first intermediate filament expressed during development in amphibians and mammals. In zebrafish, a type II cytokeratin 8 (zf-K8) cDNA has been cloned. zf-K8 gene was maternally inherited and expressed in all surface cells throughout the embryonic stages old
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Among the CYP enzymes CYP D has been considered
2019-08-19

Among the CYP450 enzymes, CYP2D has been considered a crucial protein that involves in the metabolism of xenobiotics and drugs (Zanger and Schwab, 2013). Some isoforms of the CYP2D subfamily have been well characterized, such as CYP2D6 due to its clinical importance and CYP2D14 in black cattle (Hama
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br Target enzyme attributes and
2019-08-17

Target enzyme attributes and substrate peptide selection Protein kinases catalyze the phosphorylation of serine, threonine, and tyrosine residues in both proteins and peptides using ATP as the phosphoryl donor. The human kinome is comprised of 518 protein kinases and 40 lipid kinases. The vast ma
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In conclusion we provide convincing
2019-08-17

In conclusion, we provide convincing evidence that the PRRSV-induced SGs are indeed bona fide SGs. While we determined that mRNA is present in the PRRSV-induced SGs, we did not distinguish its origin. Future studies will need to determine whether the mRNA stored in PRRSV-induced SGs is of cellular o
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For statistical analysis the Statistical Package for Social
2019-08-17

For statistical analysis, the Statistical Package for Social Sciences (SPSS) was used (version 21.0; SPSSInc., Chicago, IL). Chi-square (x2) exact test was used for the comparison of categorical data, whereas Wilcoxon and Mann–Whitney U tests were used for the analysis of nonparametric variables bas
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Prostaglandin E receptor subtype EP is a transmembrane
2019-08-17

Prostaglandin E receptor subtype 4 (EP4) is a transmembrane G-coupled protein receptor activated by prostaglandin E2 (PGE2). EP4 activation exerts anti-inflammatory effects in adipose tissue by dampening the levels of inflammatory chemokines [12]. In the mouse, EP4 deficiency aggravates fragmentatio
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The growth inhibitory effect of PGE has
2019-08-17

The growth inhibitory effect of PGE2 has been linked to the ability of Gs coupled PGE2 receptors EP2 and EP4 to mediate elevation of cAMP [22], [23]. Evidence suggests that this mechanism may not be the key cause of growth inhibition [24]. In various cell types, EP4 receptor has been shown to utiliz
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Emergence of antibiotic resistant strains of Mtb alongwith t
2019-08-17

Emergence of antibiotic resistant strains of Mtb alongwith the inefficacy of widely used Bacillus Calmette-Guerin (BCG) vaccine in adults are major challenges in the treatment and prevention of TB. Elucidation and characterization of new vaccine and drug candidates are therefore required in order to
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Our finding that activating DDR variants are a cause
2019-08-17

Our finding that activating DDR2 variants are a cause of this disease suggested that the ABL inhibitor dasatinib, a leukemia drug that also inhibits DDR2, could be used for treatment of affected individuals.10, 11 To examine the effect of dasatinib on p.Leu610Pro- and p.Tyr740Cys-induced autophospho
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Three kinase inhibitors dasatinib type I imatinib type II
2019-08-17

Three kinase inhibitors dasatinib (type I), imatinib (type II) and nilotinib (type II), identified initially as inhibitors of tyrosine kinase BCR-ABL, were found to target DDRs in a chemical proteomic profiling study (Bantscheff et al., 2007, Hantschel et al., 2008). These tyrosine kinase inhibitors
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A prominent example of such enzyme
2019-08-17

A prominent example of such enzyme is the proteasome, a highly promising target not only in cancer, but also in inflammatory and autoimmune diseases. Circulating proteasomes and respective anti-proteasome autoantibodies were detected in serum samples from patients with autoimmune diseases such as mu
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Structural homology modelling Intensive Phyre modelling was
2019-08-17

Structural homology modelling. Intensive Phyre2 modelling [44] was performed using the primary amino Tanshinone I sequence of A1S_0222 as input to generate an atomistic 3D-homology model of A1S_0222. The fit to the SAXS data of the homology model as well as the fit to the data of the E. coli adenin
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Preparation of the regioisomeric pyridooxazepinones
2019-08-17

Preparation of the regioisomeric pyridooxazepinones 10 and 11 was accomplished utilizing the synthetic sequence depicted in Scheme 3. Amide coupling of 63 and fruquintinib in chloride 64 afforded amide 65. Removal of the alcohol protecting group, followed by base catalyzed cyclization afforded a 1:2
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