• A selected set of these new derivatives was then used

  2024-08-14

  

  A selected set of these new derivatives was then used for functional assays at the human A1AR showing, as expected, an antagonist profile with IC50 values at nanomolar level. The same molecules showed also to be efficacious as nanomolar antagonists in a functional assay aimed at analyzing their abil

• br ACK signaling partners ACK interacts with

  2024-08-14

  

  ACK1 signaling partners ACK1 interacts with and tyrosine phosphorylates many cellular proteins regulating critical cellular processes [11]. While ACK1 shares common intracellular effectors such as AKT with other signaling pathways, it imparts specificity to signaling by phosphorylating effectors

• The biological characteristics of cancer invasion

  2024-08-14

  

  The biological characteristics of cancer invasion and metastasis are mainly attributed to the poor prognosis in cancer. It has been reported that overexpression of Ack1 promoted the migratory and invasive properties of breast cancer glutamate transporter by sustaining expression of epidermal growth

• The fact that the BPloopAsn

  2024-08-14

  

  The fact that the α1-BPloopAsn141 regains its α-Btx binding with a Kd similar to that of the wild type α1 ECD [18], suggests that the AChBP Cys-loop does not interfere with the correct conformation of the mutant ECD. Data from analogous mutants of the human neuronal α7 subunit ECD showed improved li

• Phos-tag Biotin BTL-105 synthesis The overall adjustment the

  2024-08-14

  

  The overall adjustment, the non-toxicity and the addiction-free treatment methods are the advantages of EA. EA treatment for depression has achieved great clinical effect in recent years (Dong et al., 2017). The clinical practice guideline of the American college of physicians (ACP) have pointed out

• br The Molecular Machinery of Autophagy and Regulation by Sp

  2024-08-14

  

  The Molecular Machinery of Autophagy and Regulation by Sphingolipids Sphingolipid-Mediated Autophagy in Cancer: Dr. Jekyll and Mr. Hyde Autophagy is an evolutionarily conserved stress response that typically promotes survival and antagonizes apoptosis. However, excessive autophagy was found to

• br Results and discussion br Conclusion

  2024-08-14

  

  Results and discussion Conclusion In summary, a series of indazole-based derivatives were synthesized and SAR studies conducted, with view to the development of a novel Aurora kinases inhibitor. The carboxylic amine-reactive biotinylation reagent group extending from the C-3 position of the a

• A unique finding in this study is that LO influences

  2024-08-14

  

  A unique finding in this study is that 12/15-LO influences CREB phosphorylation in the murine brain. While previous reports have found that knockout of 5-lipoxygenase, a related enzyme that also uses arachidonic live dead stain for substrate, can regulate CREB phosphoryation in the context of Alzhe

• Significant reductions in GYN cancer patient mortality and

  2024-08-14

  

  Significant reductions in GYN cancer patient mortality and morbidity rates require treatments that proactively prevent and reverse resistance to chemotherapy and radiation. Combining chemotherapy and radiation with inhibitors of key DDR proteins targets is likely to enhance the ability of genotoxic

• Crystal structures were obtained of

  2024-08-14

  

  Crystal structures were obtained of sulfonamide 18 and amide 19 as a derivative of amide 36 (Fig. 7A and B). The precise rotameric orientation of amide 36 was of significant interest to understand the compound's interaction with the protein. As it would be difficult to assign the rotomer of 36, the

• Coincident with APJ receptor several cell types

  2024-08-14

  

  Coincident with APJ receptor, several cell types in the body can synthesize apelin protein. For example, the highest apelin concentrations in the body have been found in the rat central nervous system, pituitary gland, lungs, cardiac muscle, gastrointestinal tract and mammary glands, with lower valu

• Although the gene that encodes DHFR

  2024-08-14

  

  Although the gene that encodes DHFR has been strongly conserved during evolution, subtle differences in the active sites of bacterial, human and parasite 2'-O-Methyl-ATP receptor have been exploited to develop DHFR inhibitors specific to particular pathogens 1, 3. For example, pyrimethamine and cyc

• Introduction Diabetic nephropathy is a rapidly growing cause

  2024-08-13

  

  Introduction Diabetic nephropathy is a rapidly growing cause of end-stage renal disease [1]. Glomerular, tubular and vascular toxicity resulting from hyperglycemia (glucotoxicity) have been evaluated extensively at the molecular level as contributing factors for diabetic nephropathy [[1], [2], [3]]

• Several dehidropregnenolone derivatives functionalized at C

  2024-08-13

  

  Several 16-dehidropregnenolone derivatives functionalized at C3, C4, C5 and C6 (Fig. 7) were prepared and evaluated as 5α-reductase inhibitors bearing in mind that after the formation of an enzyme-steroid complex a nucleophilic portion of the enzyme attacks the double bond of the steroid through Mic

• br Introduction Stroke is a devastating

  2024-08-13

  

  Introduction Stroke is a devastating condition that causes cognitive and motor dysfunction, neurodegenerative diseases and even acute death, and is a leading cause of mortality and morbidity worldwide (Chen et al., 2014a, Wang et al., 2016). Thus, exploration or identification of novel therapeuti

15871 records 100/1059 page Previous Next First page 上5页 96979899100 下5页 Last page