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If overexpression of ADK is sufficient
2024-09-29
If overexpression of ADK is sufficient to induce spontaneous seizures, then reduction of ADK in engineered mice should prevent epileptogenesis. The generation of mice with moderately reduced levels of ADK in brain rather than complete ADK deficiency seems to be essential, since several lines of evid
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br Mechanisms of specific immunotherapy Several mechanisms m
2024-09-29
Mechanisms of specific immunotherapy Several mechanisms may be involved in specific immunotherapy of EAMG by active immunization with the therapeutic vaccine in IFA. During the therapy, the therapeutic benefits result from diversion of autoantibody specificities away from pathogenic extracellular
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All scientific data over the
2024-09-29
All scientific data over the years points that 5α-reductase inhibitors undoubtedly are an effective treatment for BPH and associated LUTS, having a favorable risk-benefit profile. In contrast, although some studies indicated positive results, there is still no consensus about their use in BPH or PC
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Regarding brain tumors AXL has been
2024-09-29
Regarding Protein A/G tumors, AXL has been implicated in gliomagenesis and chemoresistance [39]. Previous investigations found that AXL is constitutively phosphorylated in many glioma cell lines, murine xenograft tumors and primary patient tumor samples [40]. Immunohistochemical analysis of AXL and
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IC values were obtained for an expanded
2024-09-28
IC50 values were obtained for an expanded version of the fragment library using the previously described mobility shift assay. Subsequently, Ki values were estimated from IC50 values to allow better comparison of the activity against targets which were measured at different substrate concentrations
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Aurora A the polar kinase is located at the
2024-09-28
Aurora A the ’polar kinase’ is located at the centrosome and is required for its maturation, division, for the mitotic spindle assembly and entry into mitosis., Mutation or transcriptional silencing of Aurora A impairs centrosome maturation and separation, leads to mono/multipolar spindles, to dela
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The Type A series contains of
2024-09-28
The Type-A series contains 6 of the 11 confirmed hits, making it a highly attractive lead template. Seven (7) out of 8 Type-A series of 3-substituted-2-furoic acids are highly active (84–100% inhibition) at the high concentration of 100μM. We could deduce some interesting, albeit preliminary structu
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Many ruthenium complexes were tested as potential anticancer
2024-09-28
Many ruthenium complexes were tested as potential anticancer agents and two complexes, namely NAMI-A (trans-[imH] [RuCl4(dmso-S)(im)]; im, imidazole) and KP1019 (trans-[indH][RuCl4(ind)2]; ind, indazole) have successfully entered clinical trials [27], [28]. NAMI-A is selectively active against metas
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br Antibiotic drug discovery approaches Traditionally novel
2024-09-28
Antibiotic drug discovery approaches Traditionally, novel BCTC were largely discovered by phenotypic screening approaches of various sources of compounds, such as natural products isolated from extracts of soil microbes and semi-synthetic or fully synthetic compound libraries derived from known a
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br Results br Discussion By using an
2024-09-28
Results Discussion By using an unbiased proteomic screen for xCT binding partners, followed by functional validation, we have made the surprising discovery that mTORC2 regulates amino (+)-Aphidicolin metabolism in tumor cells by phosphorylating serine 26 of the cystine-glutamate antiporter xC
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ALK fusion positive NSCLC is clinically actionable because
2024-09-28
ALK fusion-positive NSCLC is clinically actionable because it can be targeted by several FDA-approved drugs, including the first generation TKI crizotinib, which is a dual inhibitor to MET and ALK [15], and the second generation inhibitors, alectinib and ceritinib, both of which are highly-selective
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SB 225002 The rank order of agonist potency in turkey cardia
2024-09-28
The rank order of agonist potency in turkey cardiac chambers demonstrated the predominant presence of the β-adrenergic receptor subtype, in line with the receptor classification by . However, a previous radioligand binding study in the left ventricles of 7-week old turkeys reported the existence of
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A high throughput small molecule ACK biochemical inhibition
2024-09-27
A high-throughput small molecule ACK1 biochemical inhibition screen was performed in-house and led to the identification of 1μM inhibitor furanopyrimidine (). Further binding studies found Iloperidone to be both ATP-competitive and reversible. Early structure-activity relationship (SAR) work was
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Although the mechanisms of APP secretion are well
2024-09-27
Although the mechanisms of APP secretion are well characterised (for review see Ref. [1]), production of soluble AChE species is less well understood although we have reported that a metalloproteinase can shed AChE similarly to APP [16], [17]. Recently it has also been demonstrated that cellular pre
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br Methods and results ACE
2024-09-27
Methods and results ACE is a Canadian satellite mission [7] that measures atmospheric T7 Tag Peptide mg spectra in the limb geometry using the Sun as a light source (solar occultation). The ACE orbit (74° inclination to the equator, 650 km altitude) concentrates measurements at high latitudes bu
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