• br Experimental br Results and discussions br

  2022-01-26

  

  Experimental Results and discussions Conclusions Declaration of interests Acknowledgements Financial support from the National Natural Science Foundation of China (21605089 and 81773483), the Ningbo Municipal Natural Science Foundation (2017A610228 and 2018A610217), the Open Subject o

• br Resistance to targeted therapy The

  2022-01-26

  

  Resistance to targeted therapy The idea of treating HER2 mutant tumors with specific therapies is relatively new and, as a consequence, little is known about the potential mechanisms of resistance to anti-HER2 agents in this setting. Primary resistance may be mediated by the presence of on-target

• br Materials and methods br Results br Discussion br Conclus

  2022-01-25

  

  Materials and methods Results Discussion Conclusion Pharmacophore modeling was applied to explore new probable Glo-I inhibitors. Ninety two pharmacophoric models were generated representing diverse types of interaction between co-crystallized ligands and corresponding binding site. The g

• To assess whether this coupling mechanisms might operate als

  2022-01-25

  

  To assess whether this coupling mechanisms might operate also in a native system of untransfected cells, we select a cell line SH-SY5Y neuroblastoma that is known to express both the dopamine transporter and the M-currents (Jiang et al., 2004; Wickenden et al., 2008). These experiments were performe

• FRAX486 MMV s distinct mode of inhibition addresses key impe

  2022-01-25

  

  MMV019313's distinct mode of inhibition addresses key impediments in the development of PfFPPS/GGPPS inhibitors as antimalarial drugs. First, it is the first non-bisphosphonate inhibitor of Plasmodium FPPS/GGPPS with drug-like physicochemical properties satisfying the “Rule of 5” (Van Voorhis et al.

• Earlier findings from different cancer entities such as chro

  2022-01-25

  

  Earlier findings from different cancer entities such as chronic myeloid leukemia (Yang et al., 2011), B cell chronic lymphocytic leukemia (Jantus Lewintre et al., 2009), prostate cancer (Zhu et al., 2009), epithelial ovarian cancer (Tokunaga et al., 2008), and colon cancer (Mazzoccoli et al., 2016,

• br Acknowledgments The work in

  2022-01-25

  

  Acknowledgments The work in the Vancurova lab is supported by St John’s University, and by NIHCA202775 grant. HDACs are Epigenetic Achilles’ Heels in Tumors with ICLs On the one hand, proficient and accurate DNA repair mechanisms ensure the genomic integrity of cells. On the other hand, the D

• A769662 receptor br Conclusion The addition of cellulose to

  2022-01-25

  

  Conclusion The addition of A769662 receptor to natural substrate increases the number of H-bonds which indicates an increase in the stability of the docking systems. The investigated compounds are more stable than natural substrate in docking systems, where the natural substrate has two H-bonds

• br Synthetic Antagonists for FFA

  2022-01-25

  

  Synthetic Antagonists for FFA4 To date, only compounds from a single chemical series have been reported as FFA4 ‘antagonists’ (Table 1). ‘Compound 39’ (4-methyl-N-9H-xanthen-9-yl-benzenesulfonamide), now available from commercial vendors as AH-7614, was initially reported as an antagonist at this

• br Introduction The glucagon receptor GCGR

  2022-01-24

  

  Introduction The glucagon receptor (GCGR) is a G-protein-coupled receptor expressed mainly in the liver and kidney. Upon glucagon binding, it activates the stimulatory G protein (Gs) and increases cAMP level, subsequently transducing glucagon signaling involved in glucose, amino acids and lipid m

• agomelatine receptor The widespread involvement of HH GLI

  2022-01-24

  

  The widespread involvement of HH/GLI in human malignancies has initiated a remarkable effort to identify selective HPIs. As shown in Table 2.1, most of these small molecule inhibitors target the essential effector protein SMO, which should lead to pathway abrogation by eventually decreasing the GLIA

• IWP-L6 Various strategies have been pursued

  2022-01-24

  

  Various strategies have been pursued in the search for GIPR antagonists. Antibodies raised against both GIP(1–42) [14], [15] or the GIPR [16], [17], a small molecule antagonist [18], amino IWP-L6 substitutions of GIP(1–42) [19], and various GIP(1–42) truncations and modifications such as e.g. Pro3(G

• br Site of expression FASTK is expressed in

  2022-01-24

  

  Site of expression FASTK is expressed in various parts of human body including heart, skeletal muscle, brain, placenta, lung, liver, kidney pancreas (Ota et al., 2004) and many other organs (Fig. 1). It has been reported that FASTK is highly expressed in pancreatic tumors, where it is involved in

• Data are expressed as means SE Statistical significance was

  2022-01-24

  

  Data are expressed as means±SE. Statistical significance was determined by the Student's -test or ANOVA with post hoc Bonferroni test. A value of U87MG Gemcitabine HCl expressing human FPPS. Western blot analysis showed a clear band, which indicated the overexpression of FPPS, in U87MG cells (A, in

• The present study also demonstrated

  2022-01-24

  

  The present study also demonstrated that edoxaban inhibited both free and clot-bound FXa activity. The IC50 values for free and clot-bound FXa in this study are well consistent with Ki values for free FXa and FXa incorporated in prothrombinase complex (0.561 and 2.98nM, respectively) in our previous

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