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br Structures of human secretase
2022-01-26
Structures of human γ-secretase Before the near-atomic resolution structures, the highest resolutions achieved for γ-secretase were 15 and 12Å [19, 21]. The 15-Å structure revealed a 87114 chamber in the transmembrane domain and two pores at the top and bottom of γ-secretase, which were speculat
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br Results br Discussion Immune
2022-01-26
Results Discussion Immune-mediated chronic inflammatory diseases (e.g. rheumatoid arthritis, psoriasis, multiple sclerosis, and inflammatory bowel disease) are characterized by a dysregulated migration of leukocytes from blood vessels into inflamed tissues. To date, several new targets and inh
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Over the last years the
2022-01-26
Over the last years, the signaling pathways initialized by fibroblast growth factors (FGFs) are found to be important for progression and development of several cancers11., 12., 13., 14.. To the best of our knowledge, currently 18 FGFs are identified in human genome, which regulated by four transmem
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Sensitivity to EphB TKI was
2022-01-26
Sensitivity to EphB3 TKI was also demonstrated in a colon cancer cell line, COLO 205, with high expression of EphB3. We found not only exogenous but also endogenous EphB3 protein was expressed in the COLO 205 salinomycin after transient transfection of pCMV6-AC-GFP/EphB3, and both were demonstrated
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Recently they reported an enyne chemotype agonist Fig
2022-01-26
Recently, they reported an enyne chemotype agonist (21, Fig. 13) with low lipophilicity, small polar surface area (PSA) and high potency (Clog P=3.8, tPSA=37 A2, EC50=20nM), further derived from TUG-424. The compound endowed fast oral atomoxetine hcl (tmax=15min) and a decent pharmacokinetic profil
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The current study aimed to understand the
2022-01-26
The current study aimed to understand the roles and the underlying mechanisms of XIST in LSCC, by focusing on the regulation by miR-124-3p, which was previously identified as a target of XIST [12]. We found that the XIST expression is positively correlated with the stages of LSCC in patients. Knockd
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Accumulating evidence suggests an important role for endothe
2022-01-26
Accumulating evidence suggests an important role for endothelin ETB receptors in renal homeostasis. ETB receptors promote vasodilation, natriuresis, and diuresis (Davenport and Maguire, 2011) and maintain renal perfusion via counterbalancing the effects of vasoconstrictors and regulation of water re
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Taking all these results into account we propose
2022-01-26
Taking all these results into account, we propose a model for the evolution of HIV DNA forms in blood during the natural history of HIV infection (Fig. 4a). During PHI, the labile linear and episomal HIV DNA forms are particularly abundant and mostly constitute evidence of active replication in rece
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br Tissue Specific Roles for HIF PHD Isoforms
2022-01-26
Tissue-Specific Roles for HIF/PHD Isoforms Hypoxia signaling pathways are active in almost all mammalian cells, including immune 520 3 and tissues such as the epithelium and endothelium. This is of crucial importance when considering the influence of environmental hypoxia in inflammatory conditi
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Aspartame l aspartyl l phenylalanine
2022-01-26
Aspartame (l-aspartyl l-phenylalanine methylester) is a dipeptide artificial sweetener that is widely used as a non-nutritive sweetener in various food products [1]. The increased market of dietary products and the development of new synthetic sweetening compounds have not been sufficiently explored
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Cy5 TSA In recent years several DPP IV inhibitors
2022-01-26
In recent years, several DPP-IV inhibitors have already been approved, such as sitagliptin, vildagliptin, saxagliptin, tenegliptin, alogliptin and linagliptin, etc. Among them, linagliptin (1, Fig. 1) is a non-peptide mimetic Cy5 TSA with a unique xanthine scaffold developed through high-throughput
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It is important to clarify whether the decrease in USV
2022-01-25
It is important to clarify whether the decrease in USV after administration was secondary to the central depressant actions of the test compounds. Several reports have addressed the possibility that central depressant actions such as motor incoordination or changes in body temperature might affect U
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The GlyR is pentameric with each subunit consisting of
2022-01-25
The GlyR is pentameric, with each subunit consisting of an extracellular ligand binding domain (LBD), four transmembrane (TM) segments, and a large intracellular loop between TM3 and TM4. Binding of neurotransmitter produces conformational changes that are rapidly transmitted to the membrane-spannin
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The existence of EAAT subtypes raises obvious questions as t
2022-01-25
The existence of 5 EAAT subtypes raises obvious questions as to the cellular and anatomical distribution of the various transporters (for review, see Gegelashvili & Schousboe, 1998, Danbolt, 2001). While difference in techniques (i.e., protein vs. mRNA), reagents, and preparations (i.e., in vivo vs.
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novobiocin Having shown that some of substitutions Cl CF at
2022-01-25
Having shown that some of substitutions (Cl, CF) at the 2-position of the thiophene improved rat microsomal stability, and polar groups at the 4-position of the aryl ring had a beneficial effect on stability in both human and rat microsomes, we combined these features in a new set of analogs. Methy
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