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An AXL decoy receptor with enhanced GAS binding
2024-09-19
An AXL decoy receptor with enhanced GAS6-binding properties, MYD1, was engineered as a therapeutic tool to disrupt GAS6/AXL signaling in vivo (Kariolis et al., 2014). MYD1 was shown to block metastasis of human ovarian cancer Phosphoramidon Disodium Salt and a murine breast cancer cell line in graf
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Matthew et al synthesized and carried out SAR studies
2024-09-19
Matthew et al. synthesized and carried out SAR studies of imidazo-[1,2-a]-pyrazine as Aurora kinase inhibitors with enhanced kinase selectivity and found that ABT-263 39 showed optimal potency on Aurora-A and Aurora-B with IC50 value of 4 nM and 13 nM while on phosphorylation histone H3 (pHH3), EC5
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and LO are members of the lipoxygenase family that convert
2024-09-19
5- and 12/15-LO are members of the lipoxygenase family that convert arachidonic colony stimulating factor 1 receptor into lipid mediators such as leukotriene B4 (LTB) and 12()-hydroxyeicosatetraenoic acid (HETE) and 15()-HETE, respectively. Evidence from several in vitro and in vivo studies has sho
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In previous years evidence emerged that
2024-09-19
In previous years, evidence emerged that inferred secondary metabolites in plants might exhibit a potential arginase inhibition [36]. In a recent study, Pham and co-workers showed the inhibitory activity of chlorogenic ABT 702 dihydrochloride (7) and piceatannol (8) (Fig. 3b) on mammalian arginase
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br Implications for cancer ROS have a long history
2024-09-19
Implications for cancer ROS have a long history of being involved in the development and progression of cancer and increased ROS level is considered as a hallmark of many tumors [76], [77]. Initially, it was thought that ROS would serve as chemical mutagens that would indiscriminately damage cell
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Various antiangiogenic drugs have been analyzed over
2024-09-19
Various antiangiogenic drugs have been analyzed over the last few years; noteworthy, bevacizumab, a monoclonal antibody against VEGF-A, alone or in combination with cytotoxic agents showed interesting results in terms of radiographic response rates and progression-free survival in initial phase 2 st
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Cellular detoxification is an important process that helps r
2024-09-19
Cellular detoxification is an important process that helps remove excess oxidants from the cellular environment through endogenous antioxidants or other molecules capable of reduction. One of the key regulators of antioxidant production is the transcription factor, nuclear factor (erythroid-derived
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Aconitase clusters are prone to oxidations and are among the
2024-09-19
Aconitase clusters are prone to oxidations and are among the first to undergo a change in transition state during stages of electrophilic stress rendering them inactive [31]. Aconitase activity in LETO and OLETF did not differ at T0 suggesting that the early onset of insulin resistance may not be at
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Flavonoids protein interactions studies play a substantial p
2024-09-18
Flavonoids-protein interactions studies play a substantial part in the hunt for novel molecules which are to interact with a selected disease-relevant target [35]. The mode of potential interaction gives information about the flavonoid effectiveness and selectivity. Lately, possible target molecules
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br The AHR functions in the
2024-09-18
The AHR functions in the immune system – a tsunami of exciting findings The research of recent years has convincingly established an important function of the AHR in linking chemical environmental cues to immune responses [21,22], and reviewed in [1,23]. As a side effect, a view of the AHR as “Th
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It is also possible that adrenoceptor activation may inhibit
2024-09-18
It is also possible that α2-adrenoceptor activation may inhibit glutamate accumulation by upregulating the glutamate-buffering activity of Müller SB743921 through EAAT1 or adjusting EAAT2 in bipolar cells, as well as the NMDA receptor. Therefore, we investigated whether topical administration of br
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The assay performance was estimated using
2024-09-18
The assay performance was estimated using Z′-factors (plotted in Fig. 2A) according to Zhang et al. calculated for each plate comparing positive (in the absence of an inhibitor) and negative controls (in the presence of an AdK inhibitor). The mean Z′-factor±SD was determined to be 0.7±0.1, indicativ
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To understand the kinase selectivity
2024-09-18
To understand the kinase selectivity profile of this series, deoxycorticosterone receptor , as a representative analog from this series, was profiled against 216 purified protein kinases representing the tyrosine and serine/threonine kinase families using an in-house Caliper EZ Reader mobility shift
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Whereas more research is needed to identify the
2024-09-18
Whereas more research is needed to identify the precise mechanism by which FIN exerts its antidyskinetic effect, the ar 165 1 mg that it can negatively modulate dopaminergic transmission is also supported by our previous findings. Indeed, we have previously shown that FIN completely reversed the be
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NSC697923 br Conclusions and future direction ER
2024-09-18
Conclusions and future direction ER(−)/PgR(+) breast cancers have a distinct clinical course, response to treatment, and molecular features when compared to other breast cancer types, however some of them are actually technical artifacts or consequences of too high definitions of positivity. Acco
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