• br Rationale The present study was

  2022-08-03

  

  Rationale The present study was motivated to get further insight into the molecular recognition processes of 2-alkyl(amino)ethyl-1,1-bisphosphonates taking compounds 12–14 as reference structures. We have recently demonstrated that TcFPPS inhibitors 12 and 13 bind to the allylic site of the enzym

• To enhance the impact of GD

  2022-08-03

  

  To enhance the impact of GD2 as an immune target in this cancer, we investigated a novel strategy to upregulate expression on the cell surface of EwS cells by an epigenetic agent, based on the following rationale. Biosynthesis of GD2 and other gangliosides during organ development is driven by stage

• br Conclusions and perspectives br Acknowledgements This

  2022-08-03

  

  Conclusions and perspectives Acknowledgements This work was supported by the National Natural Science Foundation of China (Grant Nos. 21802173, 21405182 and 21773315), the Natural Science Foundation of Guangdong Province (Grant Nos. 2018A030310301, 201710010019 and 2014A030313232, 201804020025

• Several studies have found that GPR possesses a distinct

  2022-08-02

  

  Several studies have found that GPR55 possesses a distinct pharmacology from that of CB1 and CB2, and that only certain cannabinoids act at this receptor. In transfected Safingol expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, SR141716A (Rim

• diacerein GPR co localizes with ghrelin in the

  2022-08-02

  

  GPR120 co-localizes with ghrelin in the duodenum [17], α-gustducin in the small intestine and type II taste bud cells 18, 19, neuropeptide Y centrally in the arcuate nucleus [20] and glucagon-like peptide 1 (GLP-1) in the colon and circumvallate papillae taste bud cells 6, 21, 22. Interestingly GPR1

• In the present study both experimental and

  2022-08-02

  

  In the present study, both experimental and theoretical studies were performed to explore the inhibitory mechanisms of indomethacin and its analogues towards GLOI. A remarkable correlation (=0.974) was derived for the four structurally similar NSAIDs and two curcumins between the experimental bindin

• Through a large scale phylogenetic analysis of UDG

  2022-08-02

  

  Through a large-scale phylogenetic analysis of UDG superfamily in more than 1000 completely sequenced genomes, it is shown that family 3 Coenzyme Q10 can be separated into two clades with the traditional family 3 SMUG1 as one of them (Fig. 1) [31]. UDG enzymes in another clade are present in eubacte

• The effect of the selected compounds

  2022-08-02

  

  The effect of the selected compounds on NF-kB transrepression was assessed using the well-studied HeLa B2 cell line that expresses endogenous GR and NF-kB family members and responds properly to glucocorticoids and pro-inflammatory cytokines (such as TNF). Our data revealed that the two hit compound

• The elective controlled fasting study

  2022-08-02

  

  The elective controlled fasting study in our patient provides further metabolic profiling in patients with GCGR defect. Despite her lean body mass with low weight, at the age of 7 years old she demonstrated a good tolerance for fasting with hypoglycemia Bardoxolone methyl synthesis level, insulin,

• One effective approach to fine tuning the lipophilicity

  2022-08-02

  

  One effective approach to fine-tuning the lipophilicity profile of FFA1 agonists is to ‘decorate’ the 3-phenylpropahoic Oseltamivir acid scaffold with polar heterocyclic moieties. Alternatively, this scaffold could be replaced with heterocyclic isosteres (as in Takeda’s compounds 1,2 and 3 as well

• The knowledge that piroxicam competes with ligands that bind

  2022-08-02

  

  The knowledge that piroxicam competes with ligands that bind to FPR may be of importance for a deeper understanding of the anti-inflammatory effects possessed by this NSAIDs. It has recently been reported that not only phagocytes but also platelets express FPR on their cell surface and that these re

• Considering the conformational preferences of the SRSRY sequ

  2022-08-02

  

  Considering the conformational preferences of the SRSRY sequence in the x-ray structures of soluble uPAR (SuPAR) [18], [19], [20], [50], [51], it is included in a quite flexible linker delimited by Cys76 and Cys95 residues. The SRSRY sequence adopts either α-turned or β-extended conformation. In any

• Current studies have identified five orphan G protein couple

  2022-08-02

  

  Current studies have identified five orphan G protein-coupled receptors (GPCRs) that can be activated by free fatty acids (FFAs), GPR40, GPR41, GPR43, GPR84, and GPR120. Short-chain fatty acids (FAs) are specific agonists of GPR41 and GPR43 [21] and middle-chain FAs agonize GPR84 [22]. Long-chain FAs

• br Conflict of interest br Acknowledgments The research was

  2022-08-02

  

  Conflict of interest Acknowledgments The research was funded by the Major Programs of Pharmaceutical research project of Jiangsu Province (Q2018044). Introduction Lipids are important regulators of cell death. In mammalian cells, both apoptotic and non-apoptotic cell death pathways can be

• Autophagy plays a multifaceted role in regulating both the

  2022-08-02

  

  Autophagy plays a multifaceted role in regulating both the quality and quantity of protein (e.g., protein half-life and activity) and organelles (e.g., mitochondrial number and function), thus determining cell fate [15]. The induction of autophagy has been generally considered a programmed cell surv

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