• br Structures of human secretase Before the near atomic

  2021-12-29

  

  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 Deoxycorticosterone acetate receptor chamber in the transmembrane domain and two pores at the top and bottom of γ

• HCC metastasis is a multistep multifactorial process includi

  2021-12-29

  

  HCC metastasis is a multistep, multifactorial process, including adhesion of tumor Phenytoin sodium to the extracellular matrix (ECM), remodeling and degradation of ECM, invasion through local tissue, intravasation into blood or lymph vessels, and forming new tumors at distant sites [6,7]. Loss of

• br Drugs approved or in development To

  2021-12-29

  

  Drugs approved or in development To date, three drugs: RAL (MK-0518), EVG (GS-9137) and DTG (GSK1349572) [104], have been approved by the FDA. Their structures are shown in Fig. 5. DTG is under development by GlaxoSmithKline (GSK), and studies have shown DTG to be effective in patients with resis

• br Methods br Results br Discussion In the general

  2021-12-29

  

  Methods Results Discussion In the general population BNP has been established as a marker for potassium channel blockers failure diagnosis. Moreover, there is growing evidence that elevated levels of natriuretic-peptides may improve CV risk prediction in the general population above tradit

• Based on our results we

  2021-12-29

  

  Based on our results, we propose three possible mechanisms of HER2 loss after trastuzumab-based therapy (Fig. 3). The first possibility is a result of the differential effects of treatments on clonal subsets. In breast cancer, such selective pressure has been suggested to preferentially eradicate HE

• To date glycine receptors have been found in five

  2021-12-29

  

  To date, glycine receptors have been found in five distinct transmembrane protein subunits (one β subunit and four α subunit (α1–α4)), combining to form two different types of functional receptors [4], [14], either α homomeric, the immature extrasynaptic glycine receptor subtype, or αβ heteromeric,

• Recent studies revealed that synthetic oligomeric A

  2021-12-29

  

  Recent studies revealed that synthetic oligomeric Aβ1-42 decreased GLT-1 expression and promoted mislocalization of GLT-1 from the cell surface of primary astrocytes, leading to glutamate dyshomeostasis in synapses (Abdul et al., 2009, Scimemi et al., 2013). To address the cause for reduction of ast

• Some clinical reports have suggested that galanin has a role

  2021-12-28

  

  Some clinical reports have suggested that galanin has a role in the neurobiology of mood disorders [[6], [7], [8], [9], [10]]. In behavioral studies, contradictory results have been reported [11,12]. For example, systemic administration of non-selective galanin receptor agonists, such as galmic [13]

• Many natural flavonoids have been identified as

  2021-12-28

  

  Many natural flavonoids have been identified as influencing ionotropic GABA receptors through bioassay-guided fractionation of plant extracts (Fig. 4). HPLC-based activity profiling of extracts the traditional Chinese herbal drug Kushen (Sophora flavescens root) led to the identification of the 8-la

• To evaluate the role of increased FPPS expression

  2021-12-28

  

  To evaluate the role of increased FPPS expression in paclitaxel-treated cells, we investigated the effects of FPPS on Metronidazole synthesis progression. DNA content analysis showed that the number of cells accumulating in the G/M phase increased in a dose-dependent manner in paclitaxel-treated ce

• In studies described earlier IRL was administered intravenou

  2021-12-28

  

  In studies described earlier, IRL-1620 was administered intravenously; however, because of its short half-life (Rubin and Levin, 1994) (about 7–8min), the dosing had to be repeated three times. Also, a dose-dependent hypotension was observed with repeated doses of IRL-1620 in rats (Leonard and Gulat

• br ABT aR aR methyl hexahydropyrrolo b pyrrol yl

  2021-12-28

  

  ABT-288 (2-[4'-((3aR,6aR)-5-methyl-hexahydropyrrolo[3,4-b]pyrrol-1-yl)-biphenyl-4-yl]2H-pyridazine-3-one) is a selective H3R antagonist/inverse agonist developed by Abbott. Structurally, it is a compound with molecular weight (MW) 372.46 g/mol, three H-bond acceptors (HBA), and Moriguchi LogP (MLo

• Long non coding RNAs lncRNAs are

  2021-12-28

  

  Long non-coding RNAs (lncRNAs) are a class of RNA transcripts which are over 200 nucleotides in length and not translated into proteins (Ponting et al., 2009). Recent studies showed that lncRNAs have been identified as crucial regulators of gene expression, chromatin remodeling, and cell cycle (Wahl

• In an attempt to further optimize interactions

  2021-12-28

  

  In an attempt to further optimize interactions in the lipophilic P4 pocket, we next prepared compounds – () which possessed the preferred stereochemistry at P4, but with R-groups of varying size and shape. In addition to providing important structural information for maximizing potency, these compou

• In an attempt to further optimize interactions

  2021-12-28

  

  In an attempt to further optimize interactions in the lipophilic P4 pocket, we next prepared compounds – () which possessed the preferred stereochemistry at P4, but with R-groups of varying size and shape. In addition to providing important structural information for maximizing potency, these compou

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