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Clinical trials of all GSIs have ended
2022-03-09
Clinical trials of all GSIs have ended prematurely, raising the question on our understanding of their target, the γ-secretase/presenilin. Development of compounds to target γ-secretase and reduce Aβ production is complicated by the fact that γ-secretase/presenilin has critical biological function,
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br Results br Discussion In this study we investigated
2022-03-09
Results Discussion In this study, we investigated the role of galanin and GAL2 receptors on anxiety-like behaviours mediated by the dorsal hippocampus of rats. We showed that locally administered galanin (1 nmol) decreased exploration of the open arms in the EPM, suggesting an anxiogenic-like
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The importance of T currents in the control of
2022-03-09
The importance of T-currents in the control of thalamic GABA synaptic function is also demonstrated by the presence of T-channel-dependent long-term synaptic plasticity, either potentiation (LTP) or depression (LTD). Indeed, in the associative posterior thalamic medial nucleus, an LTP of the GABAerg
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No G C pattern managed to capture all GQ
2022-03-09
No G4C pattern managed to capture all GQ forming sequences of the reference dataset. The sequences that were missed by even the most flexible models were AGATGGAGTGGAGAGG, AGGAGATGCAGGAG, AGAGGGTAGATGG and TTTTTAAAAGAAGGGGAGGAATAGGGGATATGA. In fact, the former three are not expected to form any unim
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In the past two decades
2022-03-09
In the past two decades, studies of the non-B cell-derived Ig, including cancer cell-derived IgG, have been predominately facilitated by general anti-human Ig antibodies, which do not distinguish the non-B Ig from classical Ig derived from B cells. Due to this caveat, it remains obscure about whethe
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Dithiodipyridine also known as aldrithiol is a known
2022-03-09
2,2′-Dithiodipyridine , also known as aldrithiol, is a known zinc ejector, targeting for instance the zinc finger in nucleocapsid protein of human immunodeficiency SC75741 type 1. inhibited G9a activity with IC = 0.65 µM and GLP with IC = 2.6 µM. We also tested disulfide cysteamine dihydrochloride
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In our previous study we
2022-03-08
In our previous study, we designed and synthesized compounds of A series from the starting material 4-hydroxy-3-methoxycinnamic ARCA Cy3 EGFP (ferulic acid). These compounds with R group being amino acid residues, fatty acyl group and sulfuryl group showed moderate HDAC inhibition and in vitro anti
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Ras small GTPases are critical molecular switches
2022-03-08
Ras small GTPases are critical molecular switches that connect extracellular signals to intracellular signaling pathways initiated by membrane receptors, such as growth factor receptors and G protein-coupled receptors (Simanshu et al., 2017). When shifting between active GTP-bound and inactive GDP-b
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GPR GPR GPR GPR and GPR all
2022-03-08
GPR80, GPR81, GPR82, GPR93 and ψGPR79 all shared identities to P2Y GPCRs or P2Y-like oGPCRs. Previously, at least three different nucleotide receptor phenotypes have been observed in mammalian tissue, including GPCRs activated by glycerol phosphate sale nucleotides (e.g. P2Y1 and P2Y11), uridine nu
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Further our study provides the
2022-03-08
Further, our study provides the first evidence that zaprinast and kynurenic ML-098 receptor administration not only prevented the development of thermal and mechanical hypersensitivity but also enhanced morphine antinociceptive properties. Morphine is considered to be one of the most effective anal
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As part of their ongoing effort in the field
2022-03-08
As part of their ongoing effort in the field, Kalypsis recently disclosed that quinazolinones 5 [49], imidazo[1,2-a] [1,2]diazepin 6 [50] and quinolines 7 [51] all had activity as small molecule modulators of TGR5 (Figure 4). Intercept, however, disclosed different bile tgx australia derivatives as
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With an ever increasing incidence rate of type
2022-03-08
With an ever-increasing incidence rate of type 2 diabetes and obesity, it is imperative to develop new therapeutic regimes that may provide a benefit both in terms of efficacy and tolerability. The existing portfolio of drugs for the treatment of metabolic disorders, primarily type 2 diabetes and ob
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br Regulation of Glu transporters The
2022-03-08
Regulation of Glu transporters The pivotal role of Glu transporters in the fine tuning and turnover of this excitatory amino RG7227 australia calls for a detailed characterization of its regulation. Several general mechanisms that modify Glu uptake activity have been described. These include tran
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Studies of human and mouse GPR as
2022-03-08
Studies of human and mouse GPR84, as ascertained by mRNA levels in various tissues, have determined that GPR84 is highly expressed on bone marrow cells, splenic T and B cells, and circulating granulocytes/monocytes/macrophages. In the latter cells, mRNA expression of is up-regulated only under infl
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Prior to cellular uptake studies of compound
2022-03-08
Prior to cellular uptake studies of β-Sitosterol mg , docking simulation was performed (A). The result suggested this complex was capable of binding in the cavity of an outward open XylE. The orientation of the sugar moiety in the docked complex was similar to that of the glucose unit bound in the
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