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The AURA trial was a phase I
2021-06-25

The AURA trial was a phase I/II study evaluating the safety, tolerability and activity of Osimertinib in patients with EGFR-mutated NSCLC progressing after a previous EGFR TKI. The phase I component of the study included a dose escalation part (Osimertinib 20mg to 240mg), using a rolling six design,
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br Results and Discussion br Experimental Procedures br Ackn
2021-06-25

Results and Discussion Experimental Procedures Acknowledgments The ubiquitin–proteasome system (UPS) is important for biological processes such as protein degradation and protein function regulation. In general, poly-ubiquitinated proteins are degraded by proteasomes, and some proteins ac
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In addition to cleaving ubiquitins off
2021-06-25

In addition to cleaving ubiquitins off modified proteins, DUBs can also cleave between ubiquitin moieties within a polyubiquitin chain to edit the ubiquitin signal. DUBs employ different strategies to recognize polyubiquitin (Figure 1). DUBs that rely only on interactions on the S1 site tend to be
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The activity of chromenones bearing heteroaryl groups
2021-06-25

The activity of chromenones bearing heteroaryl groups at the 8-position is summarised in . Replacement of the 8-phenyl substituent of by a thiophen-2-yl group ( and ) did not improve DNA-PK inhibitory activity, although the 4-phenylthiophen-2-yl derivative (), together with the bithiophene analogue
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N1-Methylguanosine-5'-Triphosphate br Materials and meth
2021-06-24

Materials and methods Results Discussion CDK4 has been identified recently as a potential therapeutic target in human breast cancer, liposarcoma, melanoma, and glioblastoma [[37], [38], [39]]. Due to the importance of CDK4 activity in cancer cells, CDK4 inhibitors have emerged as promising
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br Acknowledgments This work was supported by Natural Scienc
2021-06-24

Acknowledgments This work was supported by Natural Science Foundation of China (No: 81501485). We are particularly grateful to Dr. Dan Yang and Dr. Yi Zhang for their assistance and facilities in helping this experiment and manuscript. Oral squamous cell carcinoma (OSCC), the most common malig
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T cell infiltration is an important predictive biomarker for
2021-06-24

T cell infiltration is an important predictive biomarker for the PD-1 blockade, and it is closely associated with a good prognosis. In our study, we found that T cells were low and exhausted within the tumor microenvironment and were distributed in the tumor margin. Anti-PD-1 treatment reduced PD-1
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br Material and methods br Results br
2021-06-24

Material and methods Results Discussion In vitro evidence indicates that LAS191859 is a potent CRTh2 antagonist as demonstrated in GTPγS binding studies with potency in the low nanomolar range and in addition it demonstrates a long receptor residence time. This potency is also maintained in
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Medroxyprogesterone acetate To assess which export pathway i
2021-06-24

To assess which export pathway is used by the iNOS mRNA, we inhibited CRM1 activity by incubation of DLD-1 Medroxyprogesterone acetate with LMB. Since LMB covalently and exclusively binds to CRM1, it represents a potent and specific inhibitor of the CRM1 transport activity [38]. Inhibition of CRM1
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Unexpectedly CRF receptor agonist and antagonist
2021-06-24

Unexpectedly, CRF2 receptor agonist and antagonist evoked similar effects in the fall in tail skin temperature caused by restraint. However, Ucn3 reduced basal values of tail skin temperature, thus indicating that some degree of basal vasoconstriction caused by BNST treatment with Ucn3 may have cont
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In general up to date
2021-06-24

In general, up to date, no study has considered thermodynamic modeling to estimate the amprolium receptor of SO2 by different DESs. Since experimental measurements are time consuming and expensive, general and accurate theoretical models are vital to estimate SO2 solubilities in different DESs over
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5959 From our array results Supplemental
2021-06-24

From our array results (Supplemental Fig. S2), we found that differential lncRNA profiling exhibited much greater disparity compared to differential gene profiling in CD28nullCD8+ T cells, indicating that differentially expressed lncRNA(s) would serve as ideal hallmarks. Moreover, we were fortunate
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br Materials and methods br Results Recently
2021-06-24

Materials and methods Results Recently, a quantitative proteomic analysis of C2C12 mouse myoblasts cell line totally deprived of protein kinase CK2 catalytic subunits (CK2α/CK2α′(−/−)), suggested that the cellular expression of HSP27, a chaperone with multiple functions related to proteostasis
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Other membrane currents are affected
2021-06-24

Other membrane currents are affected as well. Some studies have provided evidence that sulfonylureas, in addition to blocking KATP channels, also inhibit chloride and calcium channels. GLYB has been shown to almost inhibit the current generated by Na+–K+ pumps in a concentration-dependent manner (wi
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The estrogenic activity of steroids with a C
2021-06-24

The estrogenic activity of steroids with a C19 methyl group may provide a selective advantage in estrogen physiology that is not provided by E2. In this regard, 5α-androstanediol has been proposed to be a second physiological estrogen in fetal mouse Kifunensine based on the timing of ERβ synthesis
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