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In light of the overall loss
2021-07-15

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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The following is the supplementary data related to this
2021-07-15

The following is the supplementary data related to this article. Introduction Diacylglycerol kinase (DGK) phosphorylates diacylglycerol (DG) to produce phosphatidic CX-5461 (PA) (Baldanzi, 2014, Goto et al., 2006, Merida et al., 2008, Sakane et al., 2007, Topham and Epand, 2009). To date, ten m
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The data from drug screening
2021-07-15

The data from drug screening in P. berghei (Fig. 3D) provide proof of concept that chemogenomic profiling can be accomplished in P. berghei in the same manner as P. falciparum, in that significant increases in the EC50 ratio were found only for antifolate drugs in the parasite with attenuated TgDHFR
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Dehydrogenation by a KSTD is also a
2021-07-15

— 1(2)-Dehydrogenation by a Δ1-KSTD is also a crucial step during Pridinol Methanesulfonate receptor degradation of the steroid core. Several Δ1-KSTDs were shown to be active under either aerobic or anaerobic conditions [27,29,47,50,66]. Furthermore, the last common intermediate of both aerobic an
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The discoidin domain receptors DDR and
2021-07-15

The discoidin domain receptors, DDR1 and DDR2, are receptor tyrosine kinases (RTKs) that are stimulated by collagen in the extracellular matrix (ECM). Unlike most other RTKs, they form ligand-independent stable dimers that are non-covalently linked. This ECM activation induces receptor phosphorylati
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In conclusion our work provides
2021-07-14

In conclusion, our work provides the preclinical evidence showing the potent in vivo efficacy of AT7519 on chemoresistant cancer L-Carnitine inner salt receptor and its underlying mechanisms of action. Our work supports the biological rationale behind the clinical trials initiated with AT7519, part
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br Materials and Methods br Results br Discussion Even
2021-07-14

Materials and Methods Results Discussion Even though T cell checkpoint inhibitors alone have achieved impressive clinical benefit in some cancers, their application as single agents has had limited efficacy (Hamid et al., 2013; Wolchok et al., 2013). The resistance to immunotherapy is in pa
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It is important to note
2021-07-14

It is important to note that CRF1 may be activated during acute stress and early phases of anxiety disorders (Coric et al., 2010, Ising et al., 2007), as well the administration of Astressin 2B into the lateral septum did not have an effect on anxiety-like behavior in low-stress conditions but had a
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Here we examined whether Intracellular
2021-07-14

Here, we examined whether Intracellular ER may mediate Cd-induced ovarian cancer proliferation. To determine this relationship, we used ICI 182,780 as a general inhibitor of ERα and ERβ. The results suggest a metalloestrogenic effect of Cd in ovarian cancer cell lines. Inconsistency with our results
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Our previous studies have shown that in a preimplantation mo
2021-07-14

Our previous studies have shown that in a preimplantation mouse embryo the proportion of inner to outer cells (i.e. precursors of ICM and TE, respectively) is regulated by a different frequency of differentiative cell divisions at the 8- and 16-cell stages. Low number of inner blastomeres generated
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We then analyzed Ki proliferation index as a categorical
2021-07-14

We then analyzed Ki-67 proliferation index as a categorical variable by using 15%, essentially the median Ki-67 value in the entire study group (see above), to delineate low and high proliferation subgroups. By Fisher's exact test, both the type 1 versus non-type 1 EWS-FLI1 comparison (P = 0.047; Ta
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br Structure and function of EPAC isoforms EPACs are
2021-07-14

Structure and function of EPAC isoforms EPACs are guanine nucleotide exchange factors (GEFs) for the Ras-like GTPases Rap1 and Rap2 [9]. There are two mammalian EPAC isoforms, EPAC1 and EPAC2 1, 2 (Figure 1). Whereas EPAC1 displays a wide tissue distribution, the expression of EPAC2 is more restr
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In addition to vasoconstrictor actions acute effects ET
2021-07-14

In addition to vasoconstrictor actions (acute effects), ET-1 exerts potent mitogenic actions on vascular smooth muscle cells and cardiac myocytes (chronic effects), hence causing vascular and cardiac hypertrophy [19,24,25]. These effects are mediated via stimulation of either ETA or ETB receptors, a
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To get an indication whether GBM derived OHC could act
2021-07-14

To get an indication whether GBM-derived 25-OHC could act as a chemotactic signal for monocytes, lipid extracts of GM133 media were used in THP-1 migration assays. Although an indirect approach, these experiments revealed that medium lipid extracts induced monocyte migration in a quantitatively comp
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Downregulation of tumor suppressors is a major factor
2021-07-14

Downregulation of tumor suppressors is a major factor that leads to tumorigenesis. Phosphatase and tensin homolog deleted on chromosome 10 (PTEN), a common tumor suppressor, the S/GSK1265744 of which is often downregulated or even absent in the majority of human cancers, functions as a phosphatase
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