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A great deal of research has focused on candidate
2019-11-19

A great deal of research has focused on candidate medications to modulate dopaminergic mechanisms through which psychomotor stimulants produce addictive effects, i.e., drugs that expressly target the DA transporter, D1-like receptor, or D2-like receptors., , However, effective dopaminergic-based pha
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br Significance Dysregulation of dopamine homeostasis contri
2019-11-19

Significance Dysregulation of dopamine homeostasis contributes to Parkinson\'s disease (PD). The nuclear receptor Nurr1 plays a central role in dopamine homeostasis, regulating the transcription of Sennoside A synthesis governing the synthesis, packaging, and reuptake of dopamine. Efforts to cap
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br Conclusion The role of DNA PK
2019-11-19

Conclusion The role of DNA-PK target in DNA DSB repair renders this caffeic acid mg kinase of great medicinal interest in cancer chemotherapy especially the cancer types of linked to DNA defects. Due to the absence of 3D DNA-PK target structure, different ligand-based methods were applied for de
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br Conclusion br Acknowledgement The project was supported
2019-11-18

Conclusion Acknowledgement The project was supported by National Natural Science Foundation of China, China (No. 31872535); Natural Science Foundation of Shandong Province, China (ZR2018MC027, ZR2016CQ29); and Funds of Shandong \"Double Tops\" Program, China. Introduction High-altitude hyp
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Hymenialdisine the most potent inhibitor of parasite TgCK en
2019-11-18

Hymenialdisine, the most potent inhibitor of parasite TgCK1 enzymes in vitro has no whole cell anti-parasitic activity (Table 2). Like purvalanol B however, this protease inhibitor also displays poor activity against target enzymes in cultured cells. For example, in vitro IC50 values for inhibition
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GSK 650394 Through an unknown mechanism RING Ubox type E dim
2019-11-18

Through an unknown mechanism, RING/Ubox-type E3 dimers and the N-terminal tail have been shown to function as a modulator of full E3 ubiquitin ligase activity [27]. LRSAM1 promotes a significant enhancement in the formation of the high-molecular-weight products or E3 activity when the RING domain is
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In Hevea brasiliensis both the
2019-11-18

In Hevea brasiliensis, both the soluble PPase and the membrane-bound V-PPase are present in the latex; the soluble PPase is in the C-serum (cytosol) of the latex [6] and the V-PPase is on the tonoplast of the lutoid, a special vacuole in the laticifers of rubber trees [7]. The V-PPase on the lutoid
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br CDK Inhibitors for the Treatment of inflammatory
2019-11-18

CDK Inhibitors for the Treatment of inflammatory Diseases Several CDKs have been implicated as regulators of inflammatory gene expression. It will thus be very important to determine the relative contributions of the various CDKs and their kinase function on a systematic basis. This work will be
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br Oxidoreductase like MEM for
2019-11-18

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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Despite the differences in the
2019-11-18

Despite the differences in the clustering abilities of DDR1b versus DDR2 upon ligand administration, we also noted striking similarities in the spatial distribution and phosphorylation of DDR1b-YFP and DDR2-GFP. We show for the first time that in MC3T3-E1 cells, after 4 h of collagen administration,
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The UPR is composed of three different pathways
2019-11-18

The UPR is composed of three different pathways that fall under the control of three respective ER transmembrane proteins: PERK, IRE1α (inositol-requiring enzyme 1α) and ATF6 (activating transcription factor 6). As a starting signal for the UPR, misfolded proteins induce the release of GRP78 from th
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Exemestane The use of SP in IPTp may not
2019-11-18

The use of SP in IPTp may not be the only driver of parasite polymorphisms in this population, because Senegal has used sulfadoxine and/or pyrimethamine in the national antimalarial treatment plan for many years, and furthermore these drugs are still being used in antibacterial combination therapy.
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The optimization of the lead
2019-11-18

The optimization of the lead compound () was initiated and the initial key SAR and the results of the structural modifications of lead compound are summarized in . Replacement of the carboxylic teniposide moiety with other functional groups led to loss of functional activity against EP4 receptor.
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Ample evidence has shown that ET
2019-11-18

Ample evidence has shown that ET-1 system plays a pivotal role in the development of cardiovascular anomalies and pharmacological inhibition of ETA prevents the development of cardiac hypertrophy [[37], [38], [39]]. Yanagisawa and coworkers, who first reported the cardiomyocyte-specific endothelin A
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Main Text Post translational modifications by ubiquitin Ub
2019-11-16

Main Text Post-translational modifications by ubiquitin (Ub) and ubiquitin-like proteins (Ubl) regulate a diverse array of cellular and physiological processes including protein degradation, localization, and activation. While ubiquitination has primary responsibility for targeting substrates for p
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