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Raloxifene is a second generation
2021-03-27

Raloxifene is a second generation SERM that has tissue-specific effects that differ from those of tamoxifen. Raloxifene was marketed for prevention and treatment of osteoporosis in postmenopausal women in the US and Europe. In a phase II randomized double-blind study, tamoxifen and raloxifene were e
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In particular EphB has been one of the
2021-03-27

In particular, EphB4 has been one of the most studied receptor of the Eph family: inhibition of EphB4 expression using interfering-RNA or antisense oligonucleotides inhibited proliferation, survival and invasion of PC3 prostate cancer CBR-5884 in vitro and in vivo. Inhibition of EphB4 signalling usi
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One possible pitfall of using EPAC activators
2021-03-27

One possible pitfall of using EPAC2 activators in the treatment of T2DM is their potential to increase glucagon levels. As discussed previously, although the ability of EPAC2 to increase glucagon expression and production is controversial, several studies show that this protein increases Gcg mRNA le
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In the present study promoting
2021-03-27

In the present study, promoting bile BGB324 receptor synthesis by activating EP4 receptors was shown to exert protection against hepatic steatosis. This finding may be relevant for treatment of non-alcoholic fatty liver disease, a major cause of liver disease and prominent indication for liver tran
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Adding more pieces to the puzzle
2021-03-26

Adding more pieces to the puzzle, using a human-to-animal crossover study, blood taken from healthy volunteers that underwent exercise was used as a dialysate to perfuse a rabbit heart in a Langendorff model of MI [62]. Unprecedentedly, dialysate of plasma from exercised humans reduced infarct size
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Although DGK is a lipid modulating enzyme the
2021-03-26

Although DGKγ is a lipid-modulating enzyme, the role of DGKγ in integral cell metabolism has not been reported. We found that DGKγ made a difference on cell metabolism profile in HCC cells, which may be caused partially by the downregulation of GLUT1. Glucose is a major source of energy, and decreas
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br Materials and methods br Results br
2021-03-26

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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ISRIB Mechanistically GW treatment modulated cytokine expres
2021-03-26

Mechanistically, GW2580 treatment modulated cytokine expression within the kidney. We noted a decrease in the levels of TNF, MCP-1, IL-1β, IL-27, and GM-CSF in GW2580 treated mice. Decreased levels of these proinflammatory cytokines likely contributed to the attenuated proteinuria and improved renal
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Taken together our results demonstrate that
2021-03-26

Taken together, our results demonstrate that the changes of striatal dopamine release and locomotor activity observed following chronic nicotine treatment and consequent acute withdrawal are mediated by CRF1, but not CRF2. Previous studies have already indicated that blocking CRF1 would prevent some
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All of these experiments in GM matter
2021-03-26

All of these experiments in GM matter injury models have identified an array of signaling mechanisms that are potentially important. First, Kim et al. proposed that CK2 acts as a negative modulator of NADPH oxidase [55]. Then Blanquet et al. [50] found that increased CK2 correlated with inhibition o
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br Neurodegenerative diseases definition and categories Dise
2021-03-25

Neurodegenerative diseases: definition and categories Diseases that their progression is dependent on the formation of protein aggregates, are generally identified as protein aggregation diseases. Most common among them is neurodegenerative diseases, in which the protein abnormally Trigonelline a
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Caspase-3/7 Inhibitor Enzyme mimics belong to a
2021-03-25

Enzyme mimics belong to a type of rising catalysts which show the similar function with their corresponding natural enzymes [20], [21], [22], [23], [24], [25], [26], [27], although their structures are different from natural enzymes. In the area of prodrug activation, the widely-used enzyme mimics a
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Another enzyme class that has emerged as a potential
2021-03-25

Another enzyme class that has emerged as a potential alternative to P450s are the so-called ‘unspecific peroxygenases’ (UPOs). They also contain a heme but are extracellularly expressed fungal enzymes that are often more stable than P450 monooxygenases. Importantly, UPOs use H2O2 instead of O2 as th
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br Transparency document br Acknowledgments
2021-03-25

Transparency document Acknowledgments This study was funded by ICMR, Govt. of India. Alisha Dhiman acknowledges UGC-DSKPDF, India for post-doctoral fellowship and Monisha Gopalani acknowledges CSIR, India for Senior Research Fellowship. AIRF, JNU is acknowledged for TEM, confocal microscopy an
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Our study found a significant association between the degree
2021-03-25

Our study found a significant association between the degree of primary tumor lobulation and EGFR mutations status (P EGFR Triciribine status. However, only a small portion of these previous studies included the evaluation of lobulation, and almost all of them reported no association between EGFR m
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