• Compared to methadone or morphine buprenorphine

  2022-06-16

  

  Compared to methadone or morphine, buprenorphine is a partial mu-opioid agonist, which shows high affinity for, and slow dissociation from, mu-opioid receptors. This maintenance of homeostasis may help to counter the development of an overt withdrawal syndrome, and may explain the lower risk of deve

• On the other hand it is quite possible that strychnine

  2022-06-16

  

  On the other hand, it is quite possible that strychnine-sensitive glycine sites are responsible for mediating the anticonvulsant effects of GlyT1 inhibitors. Strychnine, which acts as an antagonist at these sites, is a well-known as a convulsant drug, and elevation of endogenous glycine levels at th

• br Materials and methods br Results and discussion

  2022-06-16

  

  Materials and methods Results and discussion We recently found that the GlyT1 N-terminal and C-terminal sequences could be modified by phophorylation, or partially lost under pathological conditions by calcium-dependent proteolysis (Baliova and Jursky, 2005, Baliova and Jursky, 2010). While re

• br Materials and methods br

  2022-06-16

  

  Materials and methods Results Discussion All the UDG superfamily glycosylases examined here, UDG, SMUG1, TDGFL, and TDG82−308, are capable of completely converting U-containing duplex substrates to product, though at different rates. Under STO conditions, kobs reflects the slowest kinetic s

• Through the analysis of various synthetic GPR agonists as

  2022-06-16

  

  Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic Fmoc-Arg(Pbf)-OH receptor motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of

• Analgesic activity was evaluated by measuring tail flick lat

  2022-06-15

  

  Analgesic activity was evaluated by measuring tail flick latencies to the immersion of rat’s tail in water, maintained at ∼51°C [18] after recovery from anesthesia. Typically, rats were immobilized inside a restrainer, leaving only the tail exposed, which was then immersed into the hot water bath, a

• DNAzymes a series of nucleotide sequences with specific cata

  2022-06-15

  

  DNAzymes, a series of nucleotide sequences with specific catalytic activity, have been reported frequently applied in detection assays for such as ions and amino acids, due to the advantage in stability, high cost-effectiveness and modification convenience, by comparison with protein enzymes. The DN

• In summary the SAR of

  2022-06-15

  

  In summary, the SAR of a series of phenylpropanoic acid-free fatty sn38 australia receptor agonists is described which resulted in the identification of potent FFA4 agonists. The superior pharmacokinetic properties of compound led to its selection as an in vivo tool compound which afforded robust

• The first FPR ligand described is the fMLF peptide which

  2022-06-15

  

  The first FPR1 ligand described is the fMLF peptide, which binds with high affinity (in the nM range) to and activates FPR1. Formylated peptides derived from Listeria monocytogenes also selectively activate FPR1 [10] (Table 1). Formylation of peptides also occurs in mitochondria. Thus, the release o

• br Clinical development of FGFR inhibitors

  2022-06-15

  

  Clinical development of FGFR inhibitors in breast cancer The rationale to explore the role of FGFR inhibitors in patients with breast cancer comes from a variety of sources. These include genomic aberrations frequently identified in the FGF/FGFR pathway in breast cancer, the increased sensitivity

• Next we aimed to investigate

  2022-06-15

  

  Next, we aimed to investigate if the cardiac apoptosis induced by CO-HFD, LA, T1DM or hyperglycemia involves up-regulation and activation of Fas/FasL-mediated cell death and if such effects are mediated by ROS and/or Ca+2/calcineurin/NFAT signaling axis. Similar to previous reports, [8], [9], [10],

• Besides its carcinogenic role WTAP was also

  2022-06-15

  

  Besides its carcinogenic role, WTAP was also discovered to participate in several physical processes in normal cells. As previously reported, WTAP was involved in cell proliferation, survival, apoptosis [7,29,30], eye development [8] and embryonic development [7] owing to its complex function in tra

• EGTA Enhancer of zeste homolog EZH which

  2022-06-15

  

  Enhancer of zeste homolog 2 (EZH2), which functions as a methyltransferase, is a critical subunit of polycomb repressive complex 2 (PRC2), which has been demonstrated to be involved in the development of the EGTA [23]. Aberrant expression of EZH2 has been found to be associated with a variety of hum

• DZNep is a PRC inhibitor that inhibits

  2022-06-15

  

  DZNep is a PRC2 inhibitor that inhibits S-adenosylhomocysteine hydrolase, resulting in cellular accumulation of S-adenosylhomocysteine. S-adenosylhomocysteine is a competitive inhibitor of methyl donor for methyltransferases [38]. DZNep targets EZH2 by reduction in the level of the enzyme H3K27me3 a

• Not only has the cortical actin network

  2022-06-15

  

  Not only has the cortical e1 ubiquitin network been found to influence plasma membrane properties but also to interact with exo- and endocytic vesicles (Gormal et al., 2015, Tomatis et al., 2013). The interplay between actin and membranes is integrally regulated by the phosphoinositide composition

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