• In conclusion we developed a new CysLT and CysLT

  2021-08-26

  

  In conclusion, we developed a new CysLT1 and CysLT2 receptors-mediated anaphylaxis guinea pig model that can be useful for screening both CysLT2 receptor and CysLT1/2 receptor antagonists. In addition, we have shown that the dual CysLT1/2 receptor antagonist ONO-6950 can exert protective effect agai

• CDK S phosphorylation status influences the differential cel

  2021-08-26

  

  CDK5-S47 phosphorylation status influences the differential cellular proliferation versus migration response: Previous work from our laboratory has shown CDK5 to be a critical determinant of the cellular proliferation-migration dichotomy whereby CDK5 activation downstream of stimulated epidermal gro

• Under optimized assay conditions very

  2021-08-26

  

  Under optimized assay conditions, very low concentrations (20pM) of [125I]YP20 bound to hCRF1-CHO 98 membranes with high specificity (>95% inhibited by 1μM astressin) and in a membrane protein-dependent manner. Specific binding was selective vs. the hCRF2α subtype because little specific binding wa

• Assessment of the activity of native and

  2021-08-26

  

  Assessment of the activity of native and denatured TAT-CPG2 after penetration suggests that TAT-CPG2 has been successfully delivered into the cells, and the transduced enzyme is functional inside the cells. The enzyme activity of both native and denatured TAT-fusion proteins in the cultured HepG2 no

• br Conclusions In the present study decreased AChE and incre

  2021-08-26

  

  Conclusions In the present study, decreased AChE and increased BuChE and BeChE activities were observed in greenhouse workers relative to control subjects; however, these changes cannot be related to OP exposure but likely to pesticide-induced oxidative stress or a mild inflammatory state. The in

• Ion Channel Compound Library synthesis Despite the sources o

  2021-08-26

  

  Despite the sources of error discussed above, several trends have emerged and much valuable data are available regarding binding affinities of progestogens for different steroid receptors. All the progestogens bind to the PR with a high affinity, typically in the nanomolar range. For example the syn

• The compounds listed in Table

  2021-08-26

  

  The compounds listed in Table 1, Table 2, Table 3, Table 4, Table 5 were biologically evaluated for their inhibition of the specific binding of a radiolabeled ligand [3H]PGE2 to membrane fractions prepared from cells stably expressing each mouse prostanoid receptor. The EP1 antagonist activity of th

• We should also note that although

  2021-08-25

  

  We should also note that, although AOAA is not a specific H2S inhibitor, its inhibitory effect on l-cysteine-induced relaxations are related to H2S since addition of AOAA to another H2S inhibitor PAG did not provide a further inhibition of these relaxations in penile tissue [37]. In our study, the c

• The imaging and biochemical data presented here demonstrated

  2021-08-25

  

  The imaging and biochemical data presented here demonstrated that in T cells, AEP played a specific function in cleaving Foxp3 but not Tbet. These results are in accordance with previous AEP studies where it has been shown that AEP substrates in part are not amenable to other protease activity. In a

• br Discussion The N terminal domain of DDRs has long

  2021-08-25

  

  Discussion The N-terminal domain of DDRs has long been recognized as a member of the DS superfamily (Johnson et al., 1993, Karn et al., 1993), and its role in collagen binding is understood in atomic detail (Carafoli et al., 2009, Ichikawa et al., 2007). Our crystal structure shows that the secon

• 5 aminosalicylic acid mg Historically covalent drugs have ha

  2021-08-25

  

  Historically, covalent drugs have had great success (e.g., aspirin and penicillin), and covalent drugs have become a focus in anticancer and antiviral drug discovery (Kalgutkar and Dalvie, 2012, Singh et al., 2011). These compounds contain low reactivity warheads that allow covalent adducts to form

• br GPCRs form heterotetramers In addition

  2021-08-25

  

  GPCRs form heterotetramers In addition to homodimers and heterodimers, for several family A receptor heteromers, experimental evidence supports the presence of higher order rearrangements as tetrameric structures, comprised of two different homodimers, each able to signal with its preferred G pro

• What does this mean for cancer

  2021-08-25

  

  What does this mean for cancer therapy? We found that components of the de novo pyrimidine synthesis pathway rarely mutate in cancer, clearly showing its importance. In our experimental models, the pathway, including DHODH itself, was primed to respond when the block in CoQ redox-cycling was removed

• br Fragment based drug discovery FBDD

  2021-08-25

  

  Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical PKI-402 space with libraries which are smaller in size, producing drug leads with high ligand-binding efficiency. It als

• Materials and methods Cell culture and receptor gene

  2021-08-25

  

  Materials and methods Cell culture and receptor gene transfection. PC12 Sodium Phenylbutyrate were purchased from the Institute of Cell Biology, Chinese Academy of Sciences, Shanghai, China. The cDNA for mouse CysLT1 or CysLT2 receptor (mCysLT1 and mCysLT2, subcloned into pcDNA3.0) was kindly gift

16499 records 620/1100 page Previous Next First page 上5页 616617618619620 下5页 Last page