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br Criteria for ER targeted fluorescent probes br Survey of
2021-05-14
Criteria for ER-targeted fluorescent probes Survey of fluorescent probes Proposed approach to high affinity fluorescent steroidal ER probes Our proposed approach to the development of a new generation of fluorescent estrogen receptor imaging agents employs many of the elements present in th
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On the opposite side sPLA
2021-05-14
On the opposite side, sPLA2-X has also been implicated in the pathology of cancer [167,168]. Human sPLA2-X induces lipid droplet formation in Ras-driven MDA-MB-231 triple-negative breast cancer pitavastatin synthesis and promotes their survival during nutrient stress. It acts through the products o
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We recently described the benzoxazin one
2021-05-13
We recently described the 1,3-benzoxazin-4-one analogue of LY294002 and showed it to have pan-PI3K and DNA-PK activity [2]. We have also reported on the activity of other family members, such as 3 which causes sensitization of lung cancer and colon cancer cells to radiation [11] and 4 (LTUSI122) as
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There is literature precedence for
2021-05-13
There is literature precedence for the metabolic activation of the methylene carbons adjacent to the ring oxygen(s) of dioxanes and benzopyrans resulting in ring-opened electrophilic carbonyl species. Based on the potential for this metabolic pathway being operative with , a steric block approach wa
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Our finding that activating DDR
2021-05-13
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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glutamate receptor antagonist br Results br Discussion The m
2021-05-13
Results Discussion The most relevant overall finding was that DDR1 is present in myelin and is probably synthesized by oligodendrocytes. This result was supported by three different approaches. First, we detected presence of DDR1 mRNA in myelin by ISH. Second, the pattern of DDR1 immunostainin
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To be a qualified non specific CYP inhibitor
2021-05-13
To be a qualified non-specific CYP inhibitor used as an in vitro or in vivo screening tool to distinguish CYP involvement in the overall metabolism, a complete inhibition of the entire metabolism catalyzed by CYPs in a simple experiment is desired. Based on our results, 100 μM atipamezole can comple
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Our results implicate a critical role for
2021-05-13
Our results implicate a critical role for CXCR-1 in promoting the migration of colonic tumor cells. Expression of this receptor, but not CXCR-2, increased significantly because of the EMT (Fig. 3). Moreover, although Clone A VO-Ohpic trihydrate express comparable levels of both IL-8 receptors, only
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br Clinical trials of CRM inhibitors KPT clinical trials hav
2021-05-13
Clinical trials of CRM1 inhibitors KPT-330 clinical trials have been initiated with promising very early results. One trial includes patients with advanced solid tumors whose disease has progressed after at least one prior therapy for metastatic disease (NCT01607905). Another trial includes patie
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Under conditions of energy scarcity or nutritional restricti
2021-05-13
Under conditions of energy scarcity or nutritional restriction, AMPK, a critical energy sensor, is activated in response to the increased ratio of AMP to ATP. Various kinases may phosphorylate AMPK, leading to its activation. For example, AMPK phosphorylation by liver kinase B 1 (LKB1) at Thr172 res
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The CPA EoS was presented
2021-05-13
The CPA EoS was presented by Kontogeorgis et al., in 1996 [23]. The proposed equation is composed of two parts (SRK EOS + association term) such that it can well predict the thermodynamic behavior of hydrogen bonding materials as a result of considering the association term. Yakoumis et al. (1997) e
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br Method br Results br Discussion In this cross
2021-05-13
Method Results Discussion In this cross-sectional study, we investigated the relationship between the COMT ValMet polymorphism and age on regional cortical thickness in healthy adults across the lifespan. The mesocortical pathway was of primary interest because of its projections from the v
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In this clinical context measures of cell mediated immune re
2021-05-13
In this clinical context, measures of cell-mediated immune response to CMV have been evaluated. The QuantiFERON-CMV assay (QFN-CMV; Qiagen, Germany) which measures predominantly CD8+ T-cell responses to CMV by an in-tube IFN-gamma release technique is commercially available in some regions.1, 2 Cons
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The contradictory effects exerted by metals
2021-05-13
The contradictory effects exerted by metals were reviewed by Nunes (2011) that stated that the concentration and the species of metal can cause specific effects in ChE activity. Being environmentally exposed, the organism can accumulate metals in tissues, increasing their concentrations. Some author
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A 350619 hydrochloride Research done thus far supports the
2021-05-13
Research done thus far supports the hypothesis that MPA has detrimental effects on cognition, alone and in combination with estrogen; there are other FDA-approved progestogens that satisfy the uterus opposing effects that have not been cognitively profiled. An important goal to aid women's health is
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