• Recently unimolecular multi functional peptides that

  2022-05-09

  

  Recently, unimolecular, multi-functional peptides that combine GLP-1RA activity with orotic acid and/or GIP activity have been suggested as new therapeutic agents for glycaemic and weight control. In rodents, dual GIP and GLP-1 receptor agonists achieve significantly better glucose control and weigh

• Because of its role in the cleavage of A and

  2022-05-09

  

  Because of its role in the cleavage of Aβ and the fact that many genetic forms of AD are caused by mutations in the enzyme, GS has long been a target for drug development, though previous clinical trials of Semagacestat, a GS inhibitor, have failed due to an increase in skin cancer, and a decrease i

• The sexual dimorphism in dlGALR a and

  2022-05-09

  

  The sexual dimorphism in dlGALR1a and dlGALR1b receptors found in the gonads of adult fish led us to hypothesize that the gene expression difference between female and males might be attributed to the differences in steroid production between female and male gonads. Interestingly we have found that

• We have previously designed an azobenzene based

  2022-05-09

  

  We have previously designed an azobenzene-based molecule, Razo, which could switch the conformations of G-quadruplex structures by photoregulation. 12, 13, 14, 15 However, it lacks selectivity to different G-quadruplexes. Therefore, we want to find a way to modify this molecule so that it could be u

• uPAR promotes cell associated proteolysis by binding to uPA

  2022-05-09

  

  uPAR promotes cell-associated proteolysis by binding to uPA which locally converts plasminogen into active plasmin [10]. Ligand-engaged uPAR also acts as a potent regulator of cell migration and matrix attachment. Being a membrane receptor, uPAR needs to interact with extracellular matrix (ECM) prot

• Of the cases identified herein three known and novel FGFR

  2022-05-09

  

  Of the 52 cases identified herein, three known and 11 novel FGFR fusion partners were identified. Notably, an oligomerization domain, including coiled-coil dimerization domains similar to that seen in echinoderm microtubule associated protein like 4 gene (EML4), which is the most common ALK partner

• In the previous paper we described the design

  2022-05-09

  

  In the previous paper, we described the design and synthesis of tricyclic thiazoles as FBPase inhibitors, and a series of SAR studies led to the identification of phosphate 3 and difluoromethylenephosphonate 4 exhibiting potent FBPase inhibitory activities (IC50=13, 47nM, respectively) (Fig. 2). In

• br Memories can last a lifetime

  2022-05-09

  

  Memories can last a lifetime, long after the transient events have passed. The fact that information stored in the Bay 11-7085 synthesis can outlast the environmental trigger implies that enduring cellular changes in the central nervous system underlie memory. Epigenetic modifications of DNA and

• Alogliptin receptor Most studies of HIF have

  2022-05-09

  

  Most studies of HIF-1α have focused on its transcriptional activity-dependent functions. However, our results indicate that the oxidative stress-related effects of mtHIF-1α occur independently of its translocation to the nucleus and do not require its transcriptional activity. In fact, several studi

• br Conclusion br Conflict of interest br Introduction The

  2022-05-09

  

  Conclusion Conflict of interest Introduction The human epithelial receptor 2 (HER2 or erbb2) is a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases that act through the EGF signaling cascade [1,2]. Approximately 20% of breast cancers overexpress HER2

• To date several studies have suggested that serum HER could

  2022-05-09

  

  To date, several studies have suggested that serum HER2 could be used as a biomarker for monitoring the disease course and the patient's response to therapy [110], [111]. However, the clinical usefulness of serum HER2 has not been fully validated because of conflicting data [31]. The enzyme-linked i

• An isoflavone type secondary metabolite Glabrescione B

  2022-05-09

  

  An isoflavone type secondary metabolite, Glabrescione B (GlaB), from Derris glabrescens (Benth.) J.F. Macbr. from the family Fabaceae, was found to possess the capacity to bind the Gli1 zinc finger domain and to further block DNA binding capacity [118]. Pyrvinium, an anthelmintic drug approved by th

• In summary we have designed and explored

  2022-05-09

  

  In summary, we have designed and explored synthetic routes towards novel acylsulfamoyl benzoxaborole-based HCV NS3 protease inhibitors. Interestingly, the resulting, unoptimized P1–P3 and P2–P4 macrocyclic inhibitors were equipotent in an enzyme assay and somewhat less potent in replicon assays, com

• Overall more males were HCV

  2022-05-09

  

  Overall, more males were HCV mono- and co-infected, though there was no significant age difference among groups and between men and women (all p>0.05). Almost all patients included in this study were over 40 years, in line with the period in which no HCV screening was performed in Brazilian blood b

• Cinobufagin The occurrence of naturally HCV NS resistance as

  2022-05-09

  

  The occurrence of naturally HCV NS3 resistance-associated substitutions (RAS) affects virological outcome of DAA-based combination therapies [14], [15], [16], [17], [18], [19]. For the majority of NS3 protease inhibitors the frequency of natural occurrence of single RASs in HCV genotype 1-infected p

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