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br Materials and methods br
2019-07-23
Materials and methods Results Discussion For many years, oral PDE5-Is have been prescribed as an on-demand regimen for treating ED. Several studies have reported on the efficacy and safety of such a regimen, with an overall efficacy rate of 60–70% [21]. However, many patients complain of a
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Perturbations in cell cycle are known to induce apoptosis Ou
2019-07-23
Perturbations in Obeticholic Acid for are known to induce apoptosis. Our results show that a fraction of the DT40YB-1b+/− cells, in addition to becoming tetraploids, undergo apoptotic cell death. Similar observations linking polyploidy and apoptosis have been made in the past [23], [30], [31], [32]
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8-CPT-2Me-cAMP, sodium salt br Halogenases Enzymatic C H act
2019-07-23
Halogenases Enzymatic C–H activation leading to halogenation is another emerging area in biocatalysis [55,56]. Incorporation of halogen atoms during medicinal chemistry eff ;orts is a well-established practice, presenting an effective means to control the molecule’s bioactivity and physicochemical
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The discoidin domain receptors DDR and DDR are receptor tyro
2019-07-23
The discoidin domain receptors, DDR1 and DDR2, are receptor tyrosine kinases that are activated by different types of collagen (Shrivastava et al., 1997, Vogel et al., 1997). Both receptors interact with a number of fibrillar collagens, and DDR1, but not DDR2, is also activated by the network-formin
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Several studies have demonstrated that Syn
2019-07-23
Several studies have demonstrated that αSyn specifically associates with lipid rafts (Cole et al., 2002), raising the possibility that the perturbation of rafts can affect the aggregation and phosphorylation of αSyn (Fortin et al., 2004). Schneider et al. (2010) described the potential involvement o
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Given its high frequency it
2019-07-23
Given its high frequency, it is not surprising that different strategies have been developed to restore the sensitivity of EGFR T790M-mutant sorafenib tosylate to EGFR inhibition. To date, several different strategies have been evaluated in both preclinical and clinical models, but only few have be
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Among the Ub interactions observed in the HOIP structure is
2019-07-23
Among the ~Ub interactions observed in the HOIP structure is one that involves a RING2 domain (from the non-cognate HOIP) [47]. A similar binding interaction was defined between HHARI RING2 and the hydrophobic patch on Ub by NMR [54]. HHARI RING2 mutations that ablate the interaction inhibit formati
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FOX proteins constitute a large class of transcription
2019-07-23
FOX proteins constitute a large class of transcription factors with multiple functions, from development and organogenesis to regulation of metabolic and immune functions. The Fox transcription factor is characterized by a 100-amino-acid wing helix or forkhead DNA-binding domain. In addition, the FO
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br Discussion The N terminal domain of DDRs has long
2019-07-22
Discussion The N-terminal domain of DDRs has long been recognized as a member of the DS superfamily (Johnson et al., 1993, Karn et al., 1993), and its role in collagen binding is understood in atomic detail (Carafoli et al., 2009, Ichikawa et al., 2007). Our crystal structure shows that the secon
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Until recently the first line
2019-07-22
Until recently, the first line treatment of RLS was the administration of low dose of three dopaminergic drugs, which has been approved by the US Food and Drug Administration and the European Medicines Agency for the treatment of moderate to severe RLS. These compounds are pramipexole (Mirapex), rop
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In the past few years DNA templated fluorescent
2019-07-22
In the past few years, DNA-templated fluorescent metal nanoparticles have been developed as ideal alternatives to organic dyes due to their facile synthetic process, outstanding optical properties, ultrafine size, and fine biological compatibility. Since the first successful demonstration of DNA-tem
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High throughput screening HTS of the AstraZeneca compound co
2019-07-22
High throughput screening (HTS) of the AstraZeneca pgds inhibitor 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
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Given the importance of cysteine cathepsin
2019-07-22
Given the importance of cysteine cathepsin inhibitors as putative therapeutic molecules and microbial virulence factors, we chose to investigate whether Yersinia enterocolitica may be a potent producer of such inhibitors. Y. enterocolitica is the most heterogeneous species within the genus Yersinia.
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Because aspirin and ibuprofen are NSAIDs both
2019-07-22
Because aspirin and ibuprofen are NSAIDs, both cause a variety of adverse effects, including stomach ulcers, stomach bleeding, coagulation disorders, Erlotinib Hydrochloride and cerebral microbleeds [13]. Moreover, both cause liver damage [10]. Laster [14] reported a patient with pericarditis treate
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Employing distinct genetic and pharmacological approaches Di
2019-07-22
Employing distinct genetic and pharmacological approaches, Divakaruni et al. now demonstrate that macrophages still acquire their IL-4-elicited phenotype in the absence of CPT1a (considered the main isoform in leukocytes) or CPT2, and highlight that the increased LC-FAO in M(IL-4) cells is less cruc
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