• As part of our discovery efforts searching for

  2022-07-19

  

  As part of our discovery efforts searching for small molecule GPR119 agonists, we analyzed active pharmacophores of known agonists from the literature, and found that -methylsulfonylphenyl and substituted 4-hydroxyl piperidine are common fragments. In our initial efforts, we linked these two fragme

• Boc-D-FMK Several investigators including ourselves have

  2022-07-19

  

  Several investigators including ourselves have previously shown, that allogeneic HLA-DPB1 class II-alleles are powerful leukemia rejection Boc-D-FMK for CD4 T-cell therapy following allogeneic hematopoietic stem cell transplantation (Herr et al., 2017, Rutten et al., 2008, Stevanovic et al., 2012)

• In summary we have developed an efficient

  2022-07-19

  

  In summary, we have developed an efficient synthetic route to the required urea-isostere containing hydroxamic acid-based inhibitor . The target molecule, , was found to retain the inhibitory potency of the corresponding carbo-analog against glyoxalase-I while possessing resistance to cleavage by γ

• Petrat et al could show

  2022-07-19

  

  Petrat et al. could show, that even a low dosage of 10-mg/kg glycine (133 μmol/kg) has a beneficial effect on the small intestine after I/R. In regard to glycine, β-alanine has a clearly higher EC50 to the GlyR and activates the receptor with an efficiency of only 34.6%.16, 17 Therefore, it can be c

• br Transporter based brain targeting nano DDS Drug delivery

  2022-07-19

  

  Transporter-based brain-targeting nano-DDS Drug delivery to the central nervous system (CNS) is still challenging due to the bloodbrain barrier (BBB)53., 54.. The BBB is a natural defense barrier protecting the interleukin 1 receptor antagonist from harmful substances. Since only selected, neutr

• factor xa inhibitors Tetrazole is one of the most

  2022-07-19

  

  1-Tetrazole is one of the most commonly used bioisosteres for carboxylic acids arising from their similarity in pKa (ca. 4.5–4.9 vs 4.2–4.4, respectively)., Metabolically, tetrazoles may exhibit an advantage over carboxylic acids because they form -glucuronides which are not as chemically reactive

• Because of the relationship between carbohydrate consumption

  2022-07-19

  

  Because of the relationship between carbohydrate consumption and chronic diseases such as obesity and type II diabetes (Hu, van Dam, & Liu, 2001), there is mounting interest to evaluate the quality of alk pathway through analysis by glycemic index (GI) and Englyst assay, for example (Englyst, Kingm

• Ghrelin is a brain gut peptide

  2022-07-19

  

  Ghrelin is a brain-gut peptide hormone secreted from the stomach to stimulate food intake by acting on its receptor, growth hormone secretagogue receptor (GHSR). GHSR is expressed throughout the brain and in NPY/AgRP neurons in the ARC (Cowley et al., 2003, Willesen et al., 1999). Ghrelin-expressing

• br Structures of human secretase Before the near

  2022-07-19

  

  Structures of human γ-secretase Before the near-atomic resolution structures, the highest resolutions achieved for γ-secretase were 15 and 12Å [19, 21]. The 15-Å structure revealed a AT13148 chamber in the transmembrane domain and two pores at the top and bottom of γ-secretase, which were specula

• br Acute host defense Inflammation the

  2022-07-19

  

  Acute host defense Inflammation, the host response to infection and tissue injury, is crucial for survival and restoration of tissue structure and function. This acute response is mediated and governed by a variety of pro-inflammatory circuits to ensure recognition of invading pathogens, coordina

• The second patient had a

  2022-07-18

  

  The second patient had a homozygous substitution within exon 6 (c.538C>T). The parents were heterozygous and showed no clinical or immunological defect. The mutation has been predicted to alter a potential exonic splicing enhancer (ESE) site. Therefore, exon 6 skipping could be explained by the ESE-

• The exact mechanism by which N

  2022-07-18

  

  The exact mechanism by which N-BPs inhibit FPPS remains unclear. Computer modeling [10] suggests that N-BPs mimic the structure of the enzyme’s natural isoprenoid pyrophosphate substrates, geranyl pyrophosphate (GPP)/dimethylallyl pyrophosphate (DMAPP) or act as carbocation transition state analogs

• Previous evidence suggests that PRC is an important regulato

  2022-07-18

  

  Previous evidence suggests that PRC2 is an important regulator of chromatin looping interactions in embryonic stem irak inhibitor . The new study by Donaldson-Collier and colleagues provides the first evidence that similar processes may be at play in lymphoma. It is still largely unclear, however,

• br Role of catecholamines in HIV associated neuroinflammatio

  2022-07-18

  

  Role of catecholamines in HIV-associated neuroinflammation Concluding remarks However, more research is needed to determine the precise mechanisms responsible for the immunomodulatory effects of catecholamines, including the involvement of specific receptors and signaling pathways in immune ce

• br Acknowledgements This research was supported

  2022-07-18

  

  Acknowledgements This research was supported by the Natural Sciences and Engineering Council of Canada (NSERC) Discovery Grant awarded to RGM. LMW was supported in part by fellowships from the University of Regina and the Government of Saskatchewan Fish and Wildlife Development Fund (FWDF). We wo

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