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br Conformational properties of DGK br Interaction of DGK
2020-12-23

Conformational properties of DGKϵ Interaction of DGKϵ with its lipid substrate A major component of the interaction between DGKϵ and lipid bilayers is the insertion of the hydrophobic segment comprising residues 20–42 into the membrane, as discussed above. However, this is not the only interac
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Inhibition of DHODH is reflected by
2020-12-23

Inhibition of DHODH is reflected by an antiproliferative effect on peripheral blood mononuclear thymidine phosphorylase (PBMCs), which can be measured by the inhibitory effect on their phytohemagglutinin (PHA) stimulated growth. The test was performed as described in the reference. Data for few sel
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Our finding that activating DDR
2020-12-23

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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We report here that DAPK signaling pathways play significant
2020-12-23

We report here that DAPK signaling pathways play significant roles in OGD-induced neuronal death. Exposure of the melanocortin receptor to OGD led to DAPK activation, which then promoted cell death through BimEL overexpression. Furthermore, DAPK-induced BimEL overexpression was mediated by inactiva
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br Fragment based drug discovery FBDD is a powerful
2020-12-23

Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical palmitoylethanolamide reviews space with libraries which are smaller in size, producing drug leads with high ligand-bindi
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Oral antipsychotics are substrates of CYP enzymes which
2020-12-23

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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Drug drug interactions are frequently attributed to function
2020-12-23

Drug-drug interactions are frequently attributed to functional alterations in CYP enzymes, including inhibition and induction (Chen et al., 2014, Wang et al., 2013). Mechanism-based inhibition is an irreversible form of enzyme inhibition and could form a stable inhibitor-enzyme complex, which is th
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van Linden et al developed a comprehensive guide
2020-12-23

van Linden et al. developed a comprehensive guide that describes drug and ligand binding to more than 1200 human and mouse protein kinase domains [77]. Their KLIFS (kinase–ligand interaction fingerprint and structure) directory includes an alignment of 85 potential ligand binding-site residues occur
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Beside the previously reported Topo I
2020-12-23

Beside the previously reported Topo I inhibition, time and concentration dependent CRM1 inhibitory properties of klavuzon derivatives have been shown as a second mechanism of action in this work. Especially, compounds 3 and 20 are the most effective derivatives and they completely inhibit CRM1 activ
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Fermentation process for growth of E coli BL
2020-12-23

Fermentation process for growth of E. coli BL2(DE3)/pBMS–P3Hcys was carried out in 25- and 380-L fermentors containing 15- and 250-L medium, respectively. Cell yield of about 100g/L (wet cells) was achieved by feeding glycerol and Hy-yest during fermentation. Typical fermentation parameters are show
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br Results br Discussion This
2020-12-23

Results Discussion This study assesses impacts of HLA-DPB1 and CMV reactivation on GVHD, relapse, and OS after allo-HSCT. Here we demonstrate that HLA-DPB1 and CMV reactivation both increase aGVHD risk independently. Consistent with reported data, we show that HLA-DPB1 mismatching is associate
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It was reported that IVM modulates
2020-12-22

It was reported that IVM modulates various ion channels, such as type-A GABACls, α7 acetylcholine-gated cation channels, P2X4 ATP-gated cation channels, and glycine-gated chloride 822 in vertebrates (Adelsberger et al., 2000, Khakh et al., 1999, Krause et al., 1998, Krůšek and Zemková, 1994, Shan e
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To avoid the difficulty of the nonsmooth
2020-12-22

To avoid the difficulty of the nonsmooth constraints, a sequence of smooth problems by using smoothing functions have been progressively approximated this nonsmooth problem. To date, there have been many smoothing functions, such as perturbed Fischer–Burmeister (FB), Chen–Harker–Kanzow–Smale (CHKS),
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In this contribution herein we report our newly devised
2020-12-22

In this contribution, herein we report our newly devised molecular probes with a triazole linked benzimidazole-indole-thiazolium mixed heterocyclic framework as depicted in Scheme 1. Their architecture was designed to achieve the advancement in selectivity and specificity toward DNA matrix over RNA
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The larger eukaryotic ligases such
2020-12-22

The larger eukaryotic ligases, such as LigI and LigIV, also possess an additional N-terminal DNA-binding domain (DBD) that is required for efficient ligation (Fig. 1c) and enables these ligases to encircle DNA [17]. An equivalent helix–hairpin–helix domain is also present in the bacterial NAD-depend
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