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In light of the overall loss of activity and selectivity
2021-02-26

In light of the overall loss of activity and selectivity observed with this series of arylchromenone-4-ones bearing small -alkoxy substituents, we were pleased to identify a potent and relatively selective inhibitor , exhibiting IC values of 0.008μM and 0.07μM for DNA-PK and PI3Kα, respectively. The
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Pol is responsible for the bulk of
2021-02-26

Pol ε is responsible for the bulk of leading-strand synthesis in vivo (Daigaku et al., 2015, Nick McElhinny et al., 2008, Pursell et al., 2007) and physically associates with CMG (Langston et al., 2014, Sengupta et al., 2013, Sun et al., 2015, Zhou et al., 2017). Furthermore, leading-strand synthesi
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ornidazole synthesis A spectrum of therapies came in order t
2021-02-26

A spectrum of therapies came in order to counter this misfortune, some of them are discussed below. However, the common problem faced by most of these drugs is their emerging resistance after a span of time. Some of the important drugs reported so far are as: Quinine-based antimalarial drugs (Fig. 1
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While the mechanism of DHODH
2021-02-26

While the mechanism of DHODH inhibition-induced differentiation is not fully understood, this phenomenon may be caused by pyrimidine depletion. Pyrazofurin, an inhibitor of OMP decarboxylase, was able to induce differentiation and suggests pyrimidine depletion as a potential mechanism (Sykes et al.,
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br Materials and methods br Results br
2021-02-26

Materials and methods Results Discussion In this paper, we have demonstrated application of the glmS ribozyme reverse genetic tool for chemogenomic profiling in Plasmodium spp. This tool can provide robust attenuation of expression for different target genes, across different strains varyin
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Our data indicate that the ability of these
2021-02-26

Our data indicate that the ability of these promiscuous kinases to bind chemically diverse inhibitors is defined by the hydrophobic pocket formed by the activation loop, which is only accessible in the DFG-Asp-out conformation. Inhibitors do not artificially induce the DFG-Asp-out conformation as wa
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Recent pharmaceutical research in the field
2021-02-26

Recent pharmaceutical research in the field of respiratory diseases has sought to make available new agents that specifically and selectively antagonize the actions of cysteinyl–leukotrienes. Such an effort has resulted in the development of two classes of drugs, effective in counteracting Cys-LTs p
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br Results br Discussion GPCRs recognize a broad range
2021-02-26

Results Discussion GPCRs recognize a broad range of molecules with a vast chemical Spadin sale through different mechanisms. Our understanding of the recognition of lipid mediators by GPCRs primarily comes from the structural studies of receptors for lysophospholipids and endocannabinoids inc
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Acknowledgments br Introduction Steroidogenesis the process
2021-02-26

Acknowledgments Introduction Steroidogenesis, the process of testosterone synthesis, occurs in the adrenal cortex, testis and ovary, and it is controlled by luteinizing hormone (LH), which is synthesized and secreted from the pituitary (Hanukoglu, 1992, Payne and Youngblood, 1995). In the testis
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br Materials and methods br Results
2021-02-26

Materials and methods Results Discussion PKA and Epac are two principal effector proteins involved in cAMP signaling; they are expressed in a wide range of tissues and control diverse biological functions [10]. The existence of two cAMP effectors provides more precise regulation of cAMP sig
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To elucidate whether the impact of hypoxia
2021-02-26

To elucidate whether the impact of hypoxia on EGFR expression is cell context specific or culturing density dependent, we chose the following cancer PEG Virus Precipitation Kit mg driven by EGFR and evaluated the EGFR expression after hypoxia treatment at different culturing density: a highly aggre
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Apicidin With respect to bone metabolism and ossification re
2021-02-26

With respect to ‘bone metabolism and ossification’-related genes, treatment of SaOS-2 osteoblast-like Apicidin with MS-10 up-regulated IGFBP-4, TG2, and SOST. Up-regulation of IGFBP-4 in SaOS-2 cells inhibits DNA and protein synthesis induced by IGF-1 (Kudo et al., 1995, Kudo et al., 1996). In addit
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The structure of the HOIP RBR LDD module
2021-02-26

The structure of the HOIP RBR–LDD module bound to UbcH5~Ub reveals insights into an activated HOIP component [47]. Contacts between the E2~Ub and the non-cognate RBR module in the crystal suggest how a structure in which the active sites of the E2 and the E3 are in close proximity might look. In thi
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The present study is a genetic association study using the
2021-02-26

The present study is a genetic association study using the classic candidate gene approach. This method has been repeatedly criticized in the past to produce highly unreliably findings (e.g. Flint & Munafò, 2013). The alternative would be the conduction of a sorafenib tosylate wide association stud
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Several limitations of this study
2021-02-26

Several limitations of this study need to be acknowledged. First, although 200 patients were recruited into this study and completed assessments at baseline, only 89 patients completed the cognitive tests after 8weeks of treatment. The relatively long study period (8weeks) was the main reason for th
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