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p is a tumor suppressor
2019-10-22
p16 is a tumor-suppressor gene that inhibits cyclin-dependent kinase 4 and 6 activities and arrests the Chymostatin receptor in the G1 phase. Aberrant methylation and mutation of p16/MTS1 in OSCC of patients was found in our previous study. Moreover, the frequency of hypermethylation of p16 from th
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A phenylacetic acid derivative discovered in
2019-10-22
A phenylacetic Cinobufagin sale 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 medi
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The synthesis of tricyclic analogs
2019-10-22
The synthesis of tricyclic analogs 28–33 is described in Scheme 3. Oxidative C–C bond cleavage of the terminal olefin of 39i afforded a tricyclic product 52 without isolation of an aldehyde expected as an intermediate. Aminolysis of the chloride 52 with optionally substituted anilines afforded 28–30
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br Methods br Discussion In a recent
2019-10-22
Methods Discussion In a recent survey among 2625 high risk patients on atorvastatin, 10.5% of patients achieved an LDL-target of thymidine phosphorylase level for improvement of acceptance and adherence to effective lipid lowering therapy are warranted to maximize the benefits of standard tre
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Nevertheless because of the preclinical work and
2019-10-22
Nevertheless, because of the preclinical work and the interference with EWS–FLI1 transcriptional activity, we believe that there may be a role for ET-743 in Ewing sarcoma. An analysis of the pharmacokinetic data published in the phase II clinical trial shows that at most the drug spent 5 to 6days ou
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ERK and p MAPK signaling
2019-10-22
ERK and p38 MAPK signaling pathways play critical role in genesis and metastasis of melanoma (Tang et al., 2018). >50% of melanoma protease inhibitors (Abildgaard and Guldberg, 2015) show abnormal activity of BRAF-RAS-RAF to activate MEK signal that drives the growth-promoting extracellular signal-
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br Methods br Results br
2019-10-22
Methods Results Discussion There are two particularly important facets of the present ERK findings relevant to drug conditioning. One is the strong ERK signal observed in the medial prefrontal cortex and the nucleus accumbens during the immediate post-trial interval following the final cond
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br Oxidoreductase like MEM for prodrug activation
2019-10-22
Oxidoreductase-like MEM for prodrug activation Future outlook Although MEM-mediated prodrug activation has been performed by different MEMs and prodrugs, and their effectiveness have been proved in vivo, only a few types of MEMs or prodrugs have been explored in prodrug activation until now [2
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CC-115 mg In conclusion we have found that
2019-10-22
In conclusion, we have found that Egr1 can play an inhibitory role on DBH promoter-driven transcription. This inhibition requires a newly identified Egr1 response CC-115 mg at the −227/−224 region of DBH promoter. This inhibition appears to result from Egr1 directly bound to the DBH promoter. We sp
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The vascular endothelium is a
2019-10-21
The vascular endothelium is a highly dynamic multifunctional organ that is critically involved in the regulation of vessel integrity, vascular growth and remodeling, tissue growth and metabolism, immune responses, cell adhesion, angiogenesis, hemostasis and vascular permeability [23]. Therefore, the
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br Disclosure statement br Acknowledgment This work was supp
2019-10-21
Disclosure statement Acknowledgment This work was supported by the National Natural Science Foundation of China (81270704, 81330018). Background Over-expression of cyclooxygenase-2 (COX-2) is common in many malignancies including non-small cell lung cancer (NSCLC) and is associated with po
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br Mechanisms of acquired resistance
2019-10-21
Mechanisms of acquired resistance to 1st and 2nd generation EGFR inhibitors After treatment with first or second generation EGFR TKIs, virtually all patients after approximately 12 months develop acquired resistance (AR). Different mechanisms of AR to EGFR TKIs have been reported to date and may
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Across the scaffold the platform anchors the
2019-10-21
Across the scaffold, the platform anchors the N terminus of the elongated cullin structure of APC2 [21]. This connects to the flexible cullin–RING catalytic core consisting of the C-terminal region of APC2 and the associated APC11 11, 12, 21. The flexibility and positions of the catalytic core are c
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br Experimental Procedures br Author Contributions M B
2019-10-21
Experimental Procedures Author Contributions M.B., with input and help from T.T.H., conceived the project, designed and performed the experiments, analyzed the data, and wrote the manuscript. B.B.B. and F.D.M. synthesized the wild-type and (nonhydrolyzable, NH) Ub tetramers and contributed Fig
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Our data also showed that D dopamine
2019-10-21
Our data also showed that D2 dopamine receptor was down-regulated in the hippocampus, NAc and striatum of F1-MEP animals, which was only significant in the hippocampus. Both agonists and antagonists of D2 dopamine receptor are able to decrease heroin self-administration (Hemby et al., 1996; Rowlett
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