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Mortality from breast cancer is
2021-09-22
Mortality from breast cancer is almost always attributed to metastatic spread of the disease to other organs, thus precluding resection as a treatment method. Unfortunately, conventional chemotherapy fails to eradicate most human cancers, including aggressive breast cancers. Studies over the past de
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We recently reported that the human derived PancCa cell line
2021-09-22
We recently reported that the human-derived PancCa cell line PANC-1 and the human-derived hepatocellular HepG2 cell line express GPR55 mRNA and protein [21]. In PANC-1 and HepG2 cells, knockdown of GPR55 with specific siRNAs abrogates cellular uptake of Tocrifluor 1117, a selective GPR55 ligand [21]
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br Conclusions br Acknowledgements The authors thank Matt JM
2021-09-22
Conclusions Acknowledgements The authors thank Matt JM Wood and colleagues (AstraZeneca, UK) for permission to use logD and protein binding data presented in Sup. Table S2. Introduction The number of people suffering from type 2 diabetes mellitus (T2DM) has escalated worldwide as a consequ
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Introduction Erythrocyte membrane proteins or their ortholog
2021-09-22
Introduction Erythrocyte membrane proteins or their orthologs are found in almost all PKC412 of the body [1,2]. Because of this compositional similarity and the erythrocyte membrane's accessibility, the red blood cell membrane (RBCM) has served as a crude model for mammalian plasma membranes for m
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Human Glucocorticoid Receptor hGR was first cloned in
2021-09-22
Human Glucocorticoid Receptor (hGR) was first cloned in 1985 (Hollenburg et al., 1985). It is a modular protein comprised of an N-terminal trans-activating domain (NTD), a C-terminal ligand-binding domain (LBD) and a central DNA- binding domain (DBD). The DBD is highly conserved and has two zinc fi
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br Experimental br Acknowledgments This
2021-09-22
Experimental Acknowledgments This project was generously supported by Grünenthal GmbH and IECB. We also thank the staff members of the technical platform of IECB and Grünenthal GmbH for their availability and their skills. Introduction Glucocorticoids (GCs) are essential steroid hormones t
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br Conclusion In conclusion we discovered
2021-09-22
Conclusion In conclusion, we discovered a pair of novel epimers CBC and CBD from plant C. bungei. These two natural compounds inhibit Hh pathway by blocking signaling at the level of Gli. They are effective in suppressing Hh pathway-dependent medulloblastoma growth in vitro and in vivo. Furthermo
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GLP is released in response to
2021-09-18
GLP-1 is released in response to ingestion of nutrients including carbohydrates, protein, and fat. Recent studies aimed at identifying the receptors involved in nutrient stimulated GLP-1 secretion have identified free fatty Temozolomide receptor 4 (FFA4/GPR120) as a potential 7TM receptor involved
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br PEPCK This enzyme decarboxylates and then phosphorylates
2021-09-18
PEPCK This enzyme decarboxylates and then phosphorylates oxaloacetate to form phosphoenolpyruvate (PEP) in the second step of gluconeogenesis after the carboxylation of pyruvate catalyzed by PC. PEPCK1 (PEPCK-C, encoded by the PCK1 gene) and PEPCK2 (PEPCK-M, encoded by the PCK2 gene) are two isof
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br Drug design Over the past decades the development of
2021-09-18
Drug design Over the past decades, the development of synthetic, direct fXa inhibitors has undergone four phase. Although these fXa inhibitors possess various scaffolds, most of them bind to the active site in a characteristic l-shaped conformation. In other word, they have a three-component syst
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Microglia after activation can show prominently
2021-09-18
Microglia after activation can show prominently pro-inflammatory but also anti-inflammatory characteristics [46]. Although the ageing process is not a pathological process, many of the age-associated changes resemble those observed under pathological conditions. An increase number of pro-inflammator
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CDX is also a tumor suppressor gene the ablation of
2021-09-18
CDX1 is also a tumor suppressor gene; the ablation of CDX1 and CDX2 results in a significant increase in tumor formation in the colon. CDX1 is regulated by epigenetic modification; the hypermethylation of the CpG island at the promoter is positively associated with severe clinical phenotypes. In add
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br Results and Discussion The Set sequence is homologous to
2021-09-18
Results and Discussion The Set7 sequence is homologous to the other identified histone methyltransferases in S. pombe (Figure S1) and also shares similarity with human HMTases, H3K9 GLP/Ga9, and H4K20 SUV420H1 (Figure S1). Set7 fused with the GFP (Set7-GFP) localized in the nucleus and cytoplasm
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The coenzyme S adenosylmethionine SAM binding pocket of Set
2021-09-18
The coenzyme S-adenosylmethionine (SAM)-binding pocket of Set7 is connected to the histone-tail binding groove by a conserved lysine-channel, similarly observed in vSET (Figures 2D and S3). The Set7 SAM-binding pocket is negatively charged as observed in other known HMTase structures. However, the b
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LUF6000 mg In order to establish proper
2021-09-18
In order to establish proper folding and enzymatic activity, G9a and GLP methyltransferases each contain four structural zinc ions. Both LUF6000 mg contain two distinguishable types of zinc fingers; three Zn(II) ions are chelated in a triangular cluster by 9 cysteines (b, top left), whereas one Zn(I
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