• 3-isomangostin br Concluding Remarks Synthetic cytokine biol

  2021-05-06

  

  Concluding Remarks Synthetic cytokine biology has become an important research area with novel solutions and ideas for therapeutic approaches, for example, synthekines, fusokines, immunocytokines, neoleukins, MESA receptors, or synthetic Notch or cytokine receptors. In addition to their huge impa

• br Materials and methods br Results br Discussion Neointimal

  2021-05-06

  

  Materials and methods Results Discussion Neointimal VSMC accumulation contributes considerably to vessel occlusion observed in both autologous vein graft degeneration [1], [2] and in-stent restenosis [26], [27]. In this study, the potential for retarding VSMC proliferation and hence amelior

• E-64-d br Results Table shows demographics and clinical feat

  2021-05-06

  

  Results Table 1 shows demographics and clinical features of subjects with obesity and controls. Before surgery five obese were diabetic, only one on glucose-lowering therapy; three obese were dyslipidemic and assumed lipid lowering medications. Lathosterol levels were significantly higher in pati

• A number of chemical strategies have been developed

  2021-05-06

  

  A number of chemical strategies have been developed to design activatable optical imaging probes and have been summarized in several excellent reviews 11., 12., 13., 14., 15.. Fluorogenic enzyme substrates are one of the most explored activatable probe types for enzyme detection. These probes contai

• Based on the SUMO SIM interaction involved in SUMOD

  2021-05-06

  

  Based on the SUMO–SIM interaction involved in SUMOD positioning, a SUMO2ΔSBD (SIM-binding domain; Q30A, F31A, I33A) mutant can be investigated that disrupts this important binding interface (Eisenhardt et al., 2015; Meulmeester, Kunze, Hsiao, Urlaub, & Melchior, 2008). In Fig. 4A, multiturnover assa

• br Conclusion br Competing interests br Authors contribution

  2021-05-06

  

  Conclusion Competing interests Authors' contributions Acknowledgements The work was supported by Aurigene Discovery Technologies (M) Sdn. Bhd., Industrial Doctoral Program sponsorship by Ministry of Higher Education, Malaysia and research grants by the University of Malaya, grant number

• The in vivo IC M in the adipose

  2021-05-06

  

  The in vivo IC (0.0003μM) in the adipose tissue assay is in very good agreement with the in vitro IC (0.0005μM), and it is larger than the one measured in the OLTT assay (0.00005μM) for this compound. These differences in in vivo IC between OLTT and TAG synthesis are expected as we used free NU 7441

• NMR was employed for the determination of un

  2021-05-06

  

  NMR was employed for the determination of un-ligated domain 1 structure of DDR2 receptor. The collagen-binding site on the same was identified by cross saturation experiment and mutagenesis [40]. Birgit leitinger identified the binding site of collagen with DDR2 receptor, which was three spatially a

• orbifloxacin mg br Fragment based drug discovery FBDD is a p

  2021-05-05

  

  Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical orbifloxacin mg space with libraries which are smaller in size, producing drug leads with high ligand-binding efficiency.

• Confidence with which data of animal safety

  2021-05-05

  

  Confidence with which data of animal safety/toxicity studies can be translated to human depends upon the knowledge that whether humans would be exposed to similar chemical entities (parent and its metabolites) as the animals exposed during toxicity studies. In this regard, in vitro qualitative evalu

• A phenylacetic acid derivative discovered in a

  2021-05-05

  

  A phenylacetic ZLN005 sale derivative (), discovered in a high throughput screen for CRTH2, inhibited the binding of H-PGD to CRTH2 receptors on 293 cells with an IC of 0.010μM, and inhibited the binding of H-PGD to DP receptors with an IC of only 8.3μM (). Compound also inhibited CRTH2 mediated

• Several highly selective COX inhibitors coxibs

  2021-05-05

  

  Several highly selective COX-2 inhibitors (coxibs) have been reported and marketed [6], including celecoxib [7] and etoricoxib [8] (Fig. 1). Even though these drugs produce less ulceration than conventional NSAIDs, coxibs still produce significant gastric and cardiovascular side effects due to the d

• The small intestine in addition to its

  2021-05-05

  

  The small intestine, in addition to its primary role of absorption, has the ability to metabolize drugs and other xenobiotics through phase 1 and phase 11 metabolisms [25] since almost all the cytochrome P450 RO5185426 present in the liver are also present in the small intestine although, in lower c

• At the therapeutic level the logical approach to

  2021-05-05

  

  At the therapeutic level, the logical approach to address the cooperation between FGFR4 and EGFR was the combined inhibition of both receptors. To explore the potential efficacy and specificity of this approach, we tested the effect of FGFR and EGFR inhibitors in monotherapy or in combination in syn

• br Inhibiting APC C during Interphase and prior to

  2021-05-05

  

  Inhibiting APC/C during Interphase and prior to Anaphase Because ubiquitylation by APC/C triggers cell division, it is essential that APC/C is restrained until cells are prepared for its substrates to be degraded. In addition to regulation by phosphorylation, an additional layer of control comes

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