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Thus RhoA mediated inhibition of DGK is a well characterized
2021-08-13
Thus RhoA-mediated inhibition of DGKθ is a well-characterized pathway, conserved from C. elegans to mammalian tissues, which enables G-protein coupled receptors to regulate the extent and kinetics of DAG-mediated signaling by fine tuning DGK enzymatic activity. Acknowledgments Introduction Ce
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br Conclusion The present work describes the synthesis
2021-08-13
Conclusion The present work describes the synthesis of 18 naphthoquinonolyl-1,2,3-triazole compounds based on natural product modification with antiplasmodial activity. Lapachol derivatives disclosed higher activity than the natural product. Six of these final modified lapachol 1,2,3-triazole com
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br Conclusions This report describes
2021-08-13
Conclusions This report describes the discovery of a new class of host-directed antiviral agents characterized by a 1-aryl-4,6-diamino-1,2-dihydrotriazine scaffold, responsible for a host (human) DHFR inhibition mechanism. Host-targeting antivirals represent an alternative and emerging strategy t
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QSAR based on the D structures
2021-08-13
QSAR based on the 3D structures of ligands plays an important role in the ligand-based drug discovery and design [12]. Comparative molecular field analysis, CoMFA [11], and comparative molecular similarity index analysis, CoMSIA [12] are among the most popular QSAR models. They focus on changes in
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br DDR receptor and MMP expression Type II
2021-08-13
DDR2 receptor and MMP-13 expression Type II collagen protein in articular cartilage is highly stable structure as its half-life is 117 years [43]. The chondrocytes have limited ability to synthesis type II collagen protein in the matrix of mature articular cartilage once the collagen gets disrupt
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Some mechanistic experiments performed in the early s
2021-08-13
Some mechanistic experiments performed in the early 2000s by Ongusaha et al. [78], suggest that DDR1 induction protects Parathyroid Hormone (1-34), bovine mg from apoptosis in a p53-dependent manner, and that impairment of DDR1 expression or function leads to a pronounced increase of DNA damage-ind
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direct thrombin inhibitor br Contributors br Acknowledgement
2021-08-13
Contributors Acknowledgements Introduction Pemphigus disorders are characterized by autoantibodies binding to desmosomes between epidermal cells, resulting in the loss of cell to cell adhesion and blister formation. In pemphigus foliaceus, autoantibodies predominantly bind to desmoglein 1,
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As compared with the broad spectrum of chemicals
2021-08-13
As compared with the broad spectrum of chemicals known to serve as the ligands for PXR and CAR, the ligands of VDR are previously restricted to VD3 as well as its hydroxylated metabolites and the secondary bile LB Agar Miller LCA. Recently, the VDR-binding capacities of more compounds have been dis
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The structures of the set of pyrazoles of
2021-08-13
The structures of the set of pyrazoles of are contained in the supplied with this manuscript. Acknowledgments Prostaglandin D (PGD) is known to bind with high affinity to two G protein-coupled seven-transmembrane receptors DP1 and DP2. The latter receptor, also known as CRTH2 (chemoattractant re
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Sodium Aescinate The proliferation of CCA cell lines
2021-08-13
The proliferation of CCA cell lines can be stimulated by estrogen and other growth factors (Alvaro et al., 2006; DeMorrow, 2009; Mancino et al., 2009). It has also been reported that estrogen positively modulates cholangiocyte proliferation, which is associated with cholangiopathies found in humans
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br Acknowledgements The research leading to these results ha
2021-08-12
Acknowledgements The research leading to these results has received funding from the European Union Seventh Framework Programme (FP7-PEOPLE-2013-COFUND) under grant agreement no 609020 − Scientia Fellows (JB) and the Research Council of Norway (NFR-grant 221444) (JB, JPM, OB). Introduction Hu
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br Acknowledgements The study of RING
2021-08-12
Acknowledgements The study of RING-type E3s continues to grow extremely rapidly. We regret that it was possible to only cite a fraction of the outstanding primary publications in this field. This work was supported by the National Institute of General Medical Sciences grants R01 GM088055 and R01
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br Discussion Several DPP inhibitors are currently
2021-08-12
Discussion Several DPP-4 inhibitors are currently available for use in the treatment of type 2 diabetes mellitus. Due to the different chemical structures there are marked differences both in the binding kinetics on the target enzyme [10] and also different pathways of elimination [13] exist. In
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Herein the interactions of etamicastat nepicastat and zamica
2021-08-12
Herein, the interactions of etamicastat, nepicastat and zamicastat with P-gp and BCRP were evaluated. Although recent investigations have been performed to assess the involvement of P-gp in the Vinpocetine receptor exposure of nepicastat and etamicastat (Loureiro et al., 2015), the contribution of
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AMPHs facilitate dopamine release which further triggers dop
2021-08-12
AMPHs facilitate dopamine release, which further triggers dopamine depletion [72]. Indeed, we observed that repeated treatment of MPA significantly inhibited TH-, DAT-, and VMAT-2 levels. Since DAT and VMAT-2 are important for dopaminergic terminal markers [10], their decreases suggest that MPA-indu
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