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Targeting the MAPK pathway has attracted significant interes
2020-06-28
Targeting the MAPK pathway has attracted significant interest in cancer therapy. Efforts directly targeting RAS protein are believed to be very challenging in spite of the promise shown by a few RAS inhibitors in the early development stage. Clinical benefits achieved by BRAF and MEK inhibitors have
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br Introduction Breast cancer is the most
2020-06-28
Introduction Breast cancer is the most common malignant tumor in women and the second leading cause of female death [1]. In recent years, with the improvement of early detection and the emergence of new treatment methods, the mortality rate of breast cancer has been greatly reduced. However, the
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ret pathway br Activatable photoacoustic probes Photoacousti
2020-06-28
Activatable photoacoustic probes Photoacoustic (PA) imaging is a recently developed technique [47]. The imaging approach uses probes that absorb a pulsed laser beam and convert light energy into acoustic signals. It combines the advantages of the high sensitivity offered by optical imaging and th
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Docking experiments showed that Me MeGlcA Xyl and
2020-06-28
Docking experiments showed that Me-MeGlcA3Xyl4 and MeGlc3Xyl4 were bound to EcXyn30A and the R293A variant in the same way as MeGlcA3Xyl4, having MeGlcA or its modified forms accommodated in the -2b subsite. All ligands were coordinated by the same Emodin and no new interactions were observed. The o
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Our finding that activating DDR variants
2020-06-28
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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In some cases more than
2020-06-28
In some cases, more than one CYP450 enzyme may be involved in the metabolism of a drug, and an Eadie–Hofstee plot is usually more reliable for assessing the involvement of multiple Thiola receptor (Bu, 2006). Therefore, we first plotted the Eadie–Hofstee curves and observed their shape to determine
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HS-173 The loss of secondary mutation T M mutation after AR
2020-06-28
The loss of secondary mutation T790M mutation after AR and SCLC transformation was also reported for Rociletinib. Piotrowska et al. using the MGH NGS platform recently reported in 13 biopsies among 12 EGFR T790M+ patients progressing after treatment with Rociletinib the loss of EGFR T790M mutation i
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EPAC induces SOCS gene expression in VECs resulting in
2020-06-24
EPAC1 induces SOCS3 gene expression in VECs, resulting in suppression of the JAK–STAT activation initiated by the sIL-6Rα/IL-6 trans-signalling complex [67]. EPAC1 regulates SOCS3 gene induction through the activation of C/EBP and c-Jun transcription factors, which interact directly with the SOCS3 p
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Neonatal hydronephrosis induced by TCDD exposure via
2020-06-24
Neonatal hydronephrosis induced by TCDD exposure via lactation has a critical window for onset: the incidence of this disease peaks around PNDs 1–4, followed by a rapid decrease to a substantially null level in adulthood (Couture-Haws et al., 1991; Yoshioka et al., 2016). The EP1 protein was localiz
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br Conformational Activation of APC
2020-06-24
Conformational Activation of APC/C Enables Binding to the Coactivator CDC20 APC/C comes to life by binding a coactivator. This is controlled in part by phosphorylation and APC/C conformational changes that expose the PKI-587 for the C box and IR tail of the coactivator. In interphase when mitoti
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The lungs dissected from week mice
2020-06-24
The lungs dissected from 4–5-week mice were cut into small pieces and then immersed in Dulbecco\'s modified Eagle\'s medium (Invitrogen, Carlsbad, CA) containing collagenase II (2 mg/ml), trypsin (2.5 mg/ml), Dnase I (2 mg/ml), penicillin (100 U/ml), and streptomycin (100 μg/ml) for 12 hours at 37 °
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br Funding This work was supported by a research
2020-06-24
Funding This work was supported by a research grant of the Deutsche Forschungsgemeinschaft (SCHN477-9-2 to R.S.S), the Manfred-Stolte-Stiftung (to R.S.S.) and by a research grant from the German Cancer Aid (Deutsche Krebshilfe, No. 106696/TP 5 to T.F.). Introduction Death-associated protein k
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br Conclusions Taken together the roles of CDK and
2020-06-24
Conclusions Taken together, the roles of CDK8 and miR-152-3p in the process of HCC likely performed opposite effect completely. Both CDK8 and miR-152-3p could serve as the independent prognostic factors for predicting the OS and DFS in HCC patients. We identified that miR-152-3p as a post-transcr
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A phenylacetic acid derivative discovered in
2020-06-24
A phenylacetic am580 australia derivative (), discovered in a high throughput screen for CRTH2, inhibited the binding of H-PGD to CRTH2 receptors on 293 cells with an IC of 0.010μM, and inhibited the binding of H-PGD to DP receptors with an IC of only 8.3μM (). Compound also inhibited CRTH2 media
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It is well known that corticotropin
2020-06-24
It is well-known that corticotropin-releasing factor (CRF) exerts its biological functions through binding to type-1 (CRF1) and/or type-2 (CRF2) receptors. Several clinical evidences suggest the association of a high level of CRF and the onset of anxiety and depressive disorders.2, 3, 4, 5, 6, 7 Si
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