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Prostaglandin E receptor subtype EP is a transmembrane G cou
2021-04-27
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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br Acknowledgment We thank Professor Yuh Chang Sun
2021-04-27
Acknowledgment We thank Professor Yuh-Chang Sun for providing helpful advice and the Ministry of Science and Technology of the Republic of China for financial support (grants MOST ). Introduction Past century has witnessed a tremendous increase in life expectancy of the human population, achi
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br Results and discussion br Conclusion
2021-04-27
Results and discussion Conclusion In the current study, a series of novel ‘open-chain’ classes of E. coli PDHc E1 inhibitors, N-acylhydrazone pyrimidine derivatives A, B, and C were designed and synthesized. As novel ThDP analogs, all A displayed moderate to powerful inhibitory activity with I
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br Common features of TdT pol
2021-04-26
Common features of TdT, pol μ and pol λ TdT, pol μ and pol λ remain in a closed conformation throughout their catalytic cycle, contrary to pol β [24•, 53, 54•]. One possible explanation for this observation is that they have traded fidelity (which requires open-to-closed transition) for a very t
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A set of small molecule LigI inhibitors were
2021-04-26
A set of small molecule LigI inhibitors were identified through an in silico structure-based screen, using the atomic resolution structure of LigI complexed with nicked DNA [[18], [26]]. This screen yielded inhibitors that were selective for LigI (L82), inhibited both LigI and LigIII (L67) and inhib
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We then evaluated in vivo DHODH mRNA
2021-04-26
We then evaluated in vivo DHODH mRNA Cdk2/Cyclin Inhibitory Peptide I using data from TCGA (Lee, Palm, Grimes, & Ji, 2015). To perform a pan-disease comparison of DHODH expression, log2 TPM expression values were converted to z-scores calculated per patient. Fig. 6 shows that across all 34 diseases
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High throughput screening HTS of the AstraZeneca
2021-04-26
High throughput screening (HTS) of the AstraZeneca Cilnidipine collection was conducted and identified oxadiazole amide () originating from a kinase directed screening library (although inactive against a panel of kinases). This compound had moderate potency as a DGAT-1 inhibitor (IC=0.52μM) and w
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Pulmonary fibroblasts can regulate the
2021-04-26
Pulmonary fibroblasts can regulate the wound healing process by secreting and processing extracellular matrix (ECM), chemokines, and cytokines. However, persistent and atypical fibroblast proliferation can result in ECM accumulation and may trigger the onset or development of pulmonary fibrosis [[17
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One of the features of ROCO
2021-04-26
One of the features of ROCO proteins, controlled by their domain architecture is their oligomerization status. By size-exclusion chromatography and Western blot analysis, DAPK1 was proved to form homodimers via its GTPase and kinase domains [53]. Similarly, A 419259 trihydrochloride australia micros
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Cell lines which possess microglial or neuronal
2021-04-26
Cell lines which possess microglial or neuronal properties are uncomplicated and convenient in vitro models for studying Medetomidine HCl receptor injury at the cellular and molecular levels. Microglial BV-2 cells are derived from the immortalized mouse microglia and exhibit many of the morphologic
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Oral antipsychotics are substrates of CYP enzymes which are
2021-04-26
Oral antipsychotics are substrates of CYP450 enzymes, which are crucial to their metabolism and elimination (Fig. 1). The efficacy and toxicity of antipsychotic agents is affected by factors that induce or inhibit CYP450 expression and function, such as drug–drug interactions. Additionally, the mult
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br Acknowledgements We thank Jeffrey D Konowalchuk and
2021-04-26
Acknowledgements We thank Jeffrey D. Konowalchuk and John Sony Robbins for their technical assistance. This work was supported by Natural Sciences and Engineering Research Council of Canada (NSERC) grants to DRB (RGPIN-2013-355303) and MB (RGPIN-2014-96395). AMR was supported by NSERC Vanier Doct
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nucleoside analog The in vitro cytotoxicity of the prodrugs
2021-04-26
The in vitro cytotoxicity of the prodrugs was assessed in the LS174T human colon cell line (). The results were found to reflect the stability of the prodrugs, with the unstable urea compounds ( and ) giving relatively poor cytotoxicity differentials between prodrugs and parents (i.e., approximately
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Introduction The inflammation process involves sequential
2021-04-26
Introduction The inflammation process involves sequential activation of signaling molecules, pro-inflammatory mediators, such as prostaglandins, leukotrienes, and oxygen free radicals [1]. Two cyclooxygenases Tideglusib sale were responsible for activation of the production of prostaglandins (PG1s
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Asteroids can provide an abundant
2021-04-26
Asteroids can provide an abundant supply of other resources, such as carbon, nitrogen, or calcium compounds, but will only be useful once the space economy is sufficiently developed to provide economically interesting uses for them. Others, such as titanium or aluminium, also exist in asteroids, but
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