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We have compared the potency of a series
2020-09-03
We have compared the potency of a series of DNA-directed alkylating agents, including N-mustard-acridine, N-mustard-quinoline, and N-mustard-quinazoline conjugates previously synthesized in our laboratory [7], [13], and currently used drugs (oxaliplatin, cisplatin, or 5-FU) for the treatment of CRC
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ELUXA HM EMSI is an ongoing pivotal Phase
2020-09-02
ELUXA 1 (HM-EMSI-202) is an ongoing pivotal Phase II global clinical trial, designed to further investigate the efficacy and safety of Olmutinib in patients T790M-positive NSCLC with acquired resistance after first-line EGFR TKIs. Primary endpoint is ORR according to RECIST 1.1, while secondary endp
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br EBV BILF A Virus
2020-09-02
EBV-BILF1—A Virus-Encoded 7TM Receptor with Immune Evasive Functions The EBV-encoded BILF1 receptor (EBV-BILF1) is thought to be implicated in the immune evasion strategy of EBV.56, 61, 62 This orphan 7TM receptor is expressed at significant levels during the early lytic phase of the virus infect
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br DUBs in regulation of critical steps in
2020-09-02
DUBs in regulation of critical steps in tumor metastasis Tumor metastasis comprises a complicated series of biological processes in terms of the invasion-metastasis cascade that requires cancer butein sale to (1) migrate and invade from the origin sites through the extracellular matrix (ECM) to
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DGK is not the only DGK isoform
2020-09-02
DGKε is not the only DGK isoform that has been associated with p53. It has been shown that DGKζ binds to p53 and modulates its activity in both the cytoplasm and the nucleus [39]. In the cytosol DGKζ promotes the degradation of p53 through the ubiquitin-proteosome system [39], also a likely mechanis
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DDR was originally cloned by the group of Michele de
2020-09-02
DDR1 was originally cloned by the group of Michele de Luca, at the time named TrkE. The Genoa-based research team identified the skin, and the keratinocytes in particular, as a major site of DDR1-binding activity [20]. DDR1 is also expressed in kidney, liver and lung (Fig. 2). The functional role of
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Conversely to the reduction in
2020-09-02
Conversely to the reduction in restraint-evoked HR increase following the blockade of CRF receptors, Nijsen et al. [28] demonstrated that BNST treatment with a nonselective CRF MG 149 synthesis antagonist enhanced the tachycardia evoked by contextual fear conditioning. Taken together, these results
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BTL-105 Rambabu et al reported A series
2020-09-02
Rambabu et al. reported A series of novel N-substituted 2-(2-oxo-2H-chromen-4-yloxy)propanamide derivatives synthesized from readily available 4-hydroxy coumarin to the corresponding ethyl 2-(2-oxo-2H-chromen-4-yloxy)propanoate followed by hydrolysis and further reacted with different substituted am
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br Method Detailed study protocol was
2020-09-02
Method Detailed study protocol was reported previously. The ULTIMATE- HFrEF trial was approved by the Institutional Review Board of our hospital, and the study drug, udenafil, was approved as Investigational New Drug for treatment in patients with chronic HFrEF by Ministry of Food and Drug Safety
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Several large scale clinical studies
2020-09-02
Several large-scale clinical studies have set out with the common goal to further understand the cognitive impact of menopause and hormone therapies taken by women (Gleason et al., 2015, Greendale et al., 2011, Karlamangla et al., 2017, Rapp et al., 2003, Shumaker et al., 2003). Only one human study
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br Conflict of interest statement br References and
2020-09-02
Conflict of interest statement References and recommended reading Papers of particular interest, published within the period of review, have been highlighted as: Acknowledgements We acknowledge financial support by the Swiss State Secretariat for Education, Research and Innovation (Federa
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br Oxysterols as Key Players in Metabolic Syndrome
2020-09-02
Oxysterols as Key Players in Metabolic Syndrome? Obesity and sedentary lifestyle are on the rise and pose serious threats to people\'s health and wellbeing. Obesity is often associated with other pathologies and is one of the criteria included in the definition of metabolic syndrome (MetS) (see G
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br Results and discussion br
2020-09-01
Results and discussion Conclusions In conclusion, we have developed rational strategies that allowed us to successfully identify a series of novel analogs structurally related to to modulate the activity of estrogen-related receptors (ERRγ and ERRβ), which are constitutively active. All of th
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Compounds were prepared via the
2020-09-01
Compounds were prepared via the routes shown in , varying the sequence of reactions to install the thiazole or the phenyl ring at the end of the synthesis (pyridyl examples were prepared using similar chemistry). The aminothiazole building blocks were prepared as shown in . 5-Aminothiazole was prep
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Numerous small molecule CRF receptor antagonists
2020-09-01
Numerous small molecule CRF receptor antagonists have been reported in the literature. Some representative examples are shown in . In preclinical studies (DMP696), , was found to be efficacious in preclinical behavioral models for anxiety and depression. In an open label clinical trial with (R12191
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