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Differentiation to either Th or Th
2022-09-22
Differentiation to either Th1 or Th2 GSK2126458 receptor is significantly influenced by the relative expression of T-bet and GATA-3, respectively (Zhu et al., 2006, Jenner et al., 2009). T-bet acts as a key regulator of Th1 cell fate determination and directly activates IFN-γ and suppresses IL-4 (S
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br Introduction In the treatment of patients with AIDS
2022-09-22
Introduction In the treatment of patients with AIDS and human immunodeficiency virus type 1 (HIV-1), anti-retroviral therapy (ART), which uses anti-HIV drugs such as protease inhibitors, integrase inhibitors and reverse transferase inhibitors, has made a major contribution. There are still some s
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A major hurdle in purifying a
2022-09-21
A major hurdle in purifying a membrane protein is finding a detergent that can preserve the protein, after releasing it from a given membrane, in a stable and non-aggregated state during purification steps [18,50]. The ability of various detergents used to solubilize and purify membrane proteins has
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A number of models have been proposed in
2022-09-21
A number of models have been proposed in order to explain the mechanisms of protein transport through nuclear pore complexes. One theory is that the transport is mediated by specific peptide signals known as NLSs. The classical NLSs are short sequences containing a high proportion of the positively
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To synthesize the azaindole based compound
2022-09-21
To synthesize the 7-azaindole based compound , Suzuki coupling of 6-chloro-7-azaindole with 4-CFO-phenylboronic TAI-1 was carried out in the presence of Pd(dppf)Cl·CHCl to supply biaryl in quantitative yield (). Iodination at the C-3 position resulted 3-iodo-7-azaindazole . Alkylation of the -1 posi
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It was previously proposed that glucagon acts in the
2022-09-21
It was previously proposed that glucagon acts in the liver, in which a signal is produced and relayed to the CD 3254 via vagal nerves [8], [36], [37]. The concept that the liver is the primary target site was supported by the studies reporting that the glucagon receptor is localized in the liver but
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Primarily because secretase was a therapeutic
2022-09-21
Primarily because γ-secretase was a therapeutic target in AD, a plethora of γ-secretase inhibitors (GSIs) have been developed that effectively inhibit γ-secretase cleavage in humans [16]. Indeed, “druggability” of γ-secretase has not been an issue even when the identity of the target was unknown in
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br Materials Aspergillus oryzae GS
2022-09-21
Materials Aspergillus oryzae βGS (8.4 U mg−1 solid) was obtained from Sigma-Aldrich Chemicals Co. (USA). o-Nitrophenyl β-d-galactopyranoside (ONPG), sodium carbonate, zinc chloride, manganese chloride, calcium chloride and potassium chloride were procured from Sisco Research Laboratories (SRL), M
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Growing evidence supporting the anti inflammatory and tissue
2022-09-21
Growing evidence supporting the anti-inflammatory and tissue-protective effects of FPR antagonists led to the screening of commercial libraries for novel small-molecule FPR antagonists. As result of these screening efforts and/or structure–activity relationship (SAR)-directed design and synthesis, a
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Mammals and birds are sensitive either
2022-09-21
Mammals and birds are sensitive either to hypo or hyper glycemia. In contrary some frogs when freezing/thawing experience very high glycemia (Storey and Storey, 1986). Nevertheless when the effect of temperature on Fru-2,6P2 concentration was investigated, the constant glucose level in frogs kept at
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The exact mechanism by which N BPs inhibit
2022-09-21
The exact mechanism by which N-BPs inhibit FPPS remains unclear. Computer modeling [10] suggests that N-BPs mimic the structure of the enzyme’s natural isoprenoid pyrophosphate substrates, geranyl pyrophosphate (GPP)/dimethylallyl pyrophosphate (DMAPP) or act as carbocation transition state analogs
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In the Medicines for Malaria
2022-09-21
In 2011 the Medicines for Malaria Venture (MMV) distributed the Open-Access Malaria Box to accelerate antimalarial drug discovery (Spangenberg et al., 2013). The Malaria Box consists of 400 structurally diverse compounds, curated from >20,000 hits generated from large-scale screens, that inhibit the
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EZH mutations or amplifications have been found
2022-09-21
EZH2 mutations or amplifications have been found in a broad spectrum of human cancers including B cell lymphoma, ovarian cancer, breast cancer, melanoma, bladder cancer, gastric cancer, and other cancers (Kim and Roberts, 2016). Given the evidence of EZH2 as a cancer driver, numerous efforts have be
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The histamine H receptor H R
2022-09-20
The histamine H3 receptor (H3R; 326–445 amino-acids) is located on histaminergic neuron somata, dendrites and axon varicosities, as well as on the axon varicosities and somata of other neurons, providing negative feedback to inhibit histamine synthesis and the release of histamine or other transmitt
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Almost all of the series and
2022-09-20
Almost all of the series and compounds exhibited higher activities compared with the compounds in the other series. In these series, the tetrazole group was directly linked to a nitrogen atom of the amide group at the C-28 position, and the C-3 hydroxy group was either unmodified, oxidized, esteri
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