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Despite the weak and transient
2021-02-20
Despite the weak and transient nature of E2–E3 interactions, this binding is required for the transfer of ubiquitin to the substrate. The low affinity characteristics of this interaction may be due to the fact that E2s use the same surface to interact with E1s and E3s, and hence while binding to an
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br DGKs bind and regulate other signalling proteins Based
2021-02-19
DGKs bind and regulate other signalling proteins Based on the evidence noted above, DGKs achieve specificity of function through a combination of post-translational modifications, the availability of cofactors, and through the availability and access to substrate DAG. DGKs appear to achieve an ad
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Cordycepin In this context we initiated a
2021-02-19
In this context, we initiated a program to develop new antiviral chemotypes towards a host factor implicated in Cordycepin replication: the host (human) dihydrofolate reductase (DHFR) [21]. We recently identified this enzyme as the molecular target of 1-aryl-4,6-diamino-1,2-dihydrotriazines, struct
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dmag These cytokines except for TGF can also
2021-02-19
These cytokines, except for TGF-β can also increase CysLT1R mRNA expression. We further demonstrated that TGF-β and IL-13 were able to increase the proliferation of human BSMC in response to LTD4. BSMC proliferation was CysLT1R-dependent, given that Montelukast ablated this effect. Taken together, o
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In cancer interactions between the transformed
2021-02-19
In cancer, interactions between the transformed cancer Etravirine and other cell types recruited to the tumor are important. Tumor associated macrophages provide cancer cells with a suitable low-grade inflammatory milieu including growth promoting factors. Our results suggest a novel pro-tumorigeni
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We next examined the effects of
2021-02-19
We next examined the effects of substituents around the carboxylic MDV 3100 moiety on CRTH2 binding (Table 4). The carboxylic acid moiety shared by the representative CRTH2 antagonists and is essential for the CRTH2 activity. Germinal dimethylation of the methylene moiety next to the carboxylic aci
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Stress is usually comprehended as an event affecting mainly
2021-02-19
Stress is usually comprehended as an event affecting mainly the HPA axis and initiating the alarm reaction represented by activation of the adrenal medulla. This means that the levels of related hormones and neurotransmitters are significantly elevated during and after the stress. CRF, following its
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Materials and methods br Results br Discussion Microbial
2021-02-19
Materials and methods Results Discussion Microbial production of trans-4Hyp, an added-value amino kinesin 5 for pharmaceuticals, offers significant advantages over conventional chemical extraction in economic and environmental aspects. However the low titer and productivity with the existing
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br Concluding remarks Some of the clinical trials
2021-02-19
Concluding remarks Some of the clinical trials of putative neutral competitive ERAs have been less successful than anticipated 6, 8, 11. This might be because of underestimation of the complexity of the molecular pharmacology of ETA. To resolve this, it will be necessary to define the signaling m
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Identification of the drug to be used as first step
2021-02-19
Identification of the drug to be used as first-step antihypertensive treatment has always been, and remains, a matter of debate. The decision wihich drug (or drug combination) to choose as first-line therapy depend on many variables such as coexisting metabolic disorders, obesity, presence of subcli
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Fusion genes are formed as
2021-02-19
Fusion genes are formed as the result of either structural chromosomal rearrangement including, primarily, translocation, inversion, amplification and deletion, or non-structural aberrations caused by cis- and trans-splicing or transcriptional read-through. Such events are known to play important ro
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GSK180 br STAR Methods br Acknowledgments We are grateful to
2021-02-19
STAR★Methods Acknowledgments We are grateful to Amaia Lujambio, James Fagin, and Ramon Parsons for providing cell lines and Evripidis Gavathiotis for critical reading of the manuscript. We would like to thank Saboor Hekmaty for providing expertise with RNA-seq analysis. P.I.P. would like to ac
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It is well known that acrolein a metabolite of cyclophospham
2021-02-19
It is well known that acrolein, a metabolite of cyclophosphamide, is responsible for the cyclophosphamide-induced cystitis, and that acrolein is capable of activating TRPA1 channels expressed in the capsaicin-sensitive primary afferents [2], [11]. In this context, it is likely that the early phase o
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In addition to providing substantial insight into substrate
2021-02-18
In addition to providing substantial insight into substrate recognition, structural studies have revealed important details about mechanisms of glycosylation and HCF-1 cleavage [28,30,33]. Activation of the nucleotide-sugar is accomplished through interactions of the β-phosphate with the N-terminus
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l6 mg br Results and discussion br Conclusion Based
2021-02-18
Results and discussion Conclusion Based on the structure of ThDP, in this study, a series of novel ThDP analogs 6a-6g and 8a-8g were designed by optimizing triazole-benzene linker and modifying the substituent group of triazole ring. Then they were synthesized as potential inhibitors of Cy-PDH
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