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Glutathione in reduced form GSH the tripeptide glutamyl
2022-05-25
Glutathione in reduced form (GSH, the tripeptide, γ-glutamyl cysteinyl glycine) is a non-enzymatic low-molecular-weight antioxidant necessary for the maintenance of a cellular redox state (Noctor et al., 2012). At the stage of the transition from germination to seedling growth the process of cell di
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The stress of accelerated lactate production in cancer cells
2022-05-25
The stress of accelerated lactate production in cancer Protease Inhibitor Cocktail (EDTA-Free, 200X in DMSO) is moderated by the overexpression of lactate transporters – symporters for lactate anions and protons called monocarboxylate transporters (MCTs) – that are capable of bidirectional transport
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Adenosine triphosphatase ATP is a signaling molecule
2022-05-25
Adenosine triphosphatase (ATP) is a signaling molecule in acute pain and chronic pain(Burnstock, 2009, Burnstock, 2013, Burnstock, 2014, Chizh and Illes, 2001). It is also known that presynaptic A1 receptors are involved in the inhibition of transmitter release (Vizi and Knoll, 1976). Extracellular
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br Regulation of Glu transporters The pivotal
2022-05-25
Regulation of Glu transporters The pivotal role of Glu transporters in the fine tuning and turnover of this excitatory amino kv1.3 inhibitor calls for a detailed characterization of its regulation. Several general mechanisms that modify Glu uptake activity have been described. These include trans
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fasudil Herein in consider of the high similarity between GR
2022-05-25
Herein, in consider of the high similarity between GR HBP site and AR HBP site, we applied rational drug design strategy to develop AR/GR antagonists based on the chemical structures of antiandrogens and crystal structure of GR. The following bioassay identified Z19 as a dual AR/GR antagonist. Z19 i
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During the course of the development of aminothiazole
2022-05-25
During the course of the development of aminothiazole-derived small molecule GSMs, SGSM-36 (Fig. 1A) was discovered and exhibited good activity for suppressing the production of Aβ42 (Aβ42 IC50=63nM) (Rynearson et al., 2016; Wagner et al., 2014). In addition, SGSM-36 exhibited improved physicochemic
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br Biologically active non peptide galanin receptor ligands
2022-05-25
Biologically active non-peptide galanin receptor ligands The first successful attempt in overcoming these weaknesses was undertaken by Saar et al. (2002). Screening of galanin sequence established that Trp-2, Asn-5, Tyr-9 were pharmacophores, responsible for biochemical action of the peptide. Bas
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Recently considerable effort has been invested in developing
2022-05-24
Recently, considerable effort has been invested in developing FDPS inhibitors based on alternative scaffolds (including nonbisphosphonates) that allow other tissue types and parasite-derived forms of FDPS , to be targeted. There are several limits in analyzing inhibitors of FDPS activity: the most w
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To date three other allosteric binding sites
2022-05-24
To date, three other allosteric binding sites of HIV-1 IN have also been reported. In the work of Wielens and co-workers [33], a pocket formed by the residues Tyr83, Trp108, Asn184, Ile200 and Val201 was found, which can be bound by small molecules. In the work by Rhodes et al. [34], a small-molecul
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Taking all these results into account
2022-05-24
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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In conclusions it is hypothesized that
2022-05-24
In conclusions, it is hypothesized that caffeine administration could lead to an increase in histamine neuronal activation or release of histamine [38] to induced locomotor stimulation via H1 receptor activation. In addition, the present study also propose that the spaced administration of caffeine
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br Trifluoromethylketones This group of
2022-05-24
Trifluoromethylketones This group of compounds was demonstrated to bind the zinc Fumagillin in the active site due to its easy hydration, forming the required chelating intermediate. Ontaria et al. [92] have proposed variations around the cap group of trifluoromethylthiophene as the core motif fo
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br Material and methods br Results br
2022-05-24
Material and methods Results Discussion In this paper, an HCV molecular epidemiological study was conducted in DU sentinel surveillance sites in 20 prefecture-level cities across Guangdong Province, and the different subtype distributions between IDU and NIDU were compared. Owing to the lac
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Compared with the tetrazole derivative the potency of analog
2022-05-24
Compared with the tetrazole derivative , the potency of analogs – was 3- to 17-fold improved. Of the range of heterocycles prepared, 1,2,4-thiadiazol-5(4)-one and 1,3,4-oxadiazol-2(3)-one showed the best potencies of 0.52μM and 0.61μM, respectively. Introduction of a second hydrogen bond donor, such
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INTRODUCTION Scar formation and tissue regeneration are oppo
2022-05-24
INTRODUCTION Scar formation and tissue regeneration are opposite results of the wound healing process. Although fibrosis is more common after skin injury, full skin regeneration results in complete replacement of adnexa and function. Examples of tissue regeneration in mammalian systems include annu
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