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The most significant source of DAG
2020-04-28
The most significant source of DAG originates from the PLC family of enzymes, which produces DAG in an agonist-regulated reaction. PLCs constitute a wide family of enzymes acting on both phosphatidilinositols (PI) and phosphatidilcoline (PC) (Li et al., 2010) in the plasma membrane and other intrace
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kd025 LTD and LTC cause contraction
2020-04-28
LTD4 and LTC4 cause contraction in the rat stomach and these contractions are sensitive to CysLT1 receptor antagonists (Goldenberg and Subers, 1983, Miura et al., 1992, Miyata et al., 1995). However, effects of other leukotrienes in the gastric contraction and inhibitory effects of potent, selectiv
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neuron specific enolase Flexible alignment of isopropylpheny
2020-04-28
Flexible alignment of 7-isopropylphenylaminobenzimidazole 16 with the lead neuron specific enolase 1 was performed using MOE. It was found that the aryl group of compound 16, exemplified as a yellow circle in Figure 2, overlapped well with the corresponding alkyl chain of compound 1 as well as the o
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MAPK Inhibitor Library Introduction The term myeloproliferat
2020-04-27
Introduction The term “myeloproliferative disorders” was first proposed by William Dameshek in 1951. With the discovery of the Philadelphia chromosome, myeloproliferative disorders were classified into two groups: BCR-ABL positive chronic myeloid leukemia (CML) and BCR-ABL negative chronic myelopr
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AZD6738 br Conclusion br Conflict of interest br
2020-04-27
Conclusion Conflict of interest Acknowledgment The authors acknowledge the grant support of the Tehran University of Medical Sciences (94-02-49-29647). Introduction Earlier in vitro observations have also established that the human 5-HT2A, while very similar to the rat isoform, exhibits
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Compound was advanced to a chronic efficacy study
2020-04-27
Compound 52 was advanced to a chronic efficacy study in db/db mice maintained on a high fat diet. Animals were dosed with 0.5% methylcellulose vehicle, Tioconazole australia 52 (1, 3 or 15mg/kg, po, Q.D.) or 1 (0.3mg/kg) for 14days. Over the course of the study body weight and food intake were measu
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Arsenic is an endocrine disruptor
2020-04-27
Arsenic is an endocrine disruptor with estrogenic activity. Further study has shown that arsenic exposure can significantly increase the expression of estrogen receptor-related genes, steroid metabolism-related enzymes and lung cancer-related genes in the lung tissues of female mice on the occurrenc
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In order to evaluate the in
2020-04-27
In order to evaluate the in vivo pharmacology associated with EP receptor antagonism, we wished to discover antagonists presenting a higher degree of selectivity over the other prostanoid receptors. We also wanted to increase the brain–blood ratio since it is probable that centrally mediated EP agon
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Geneticin We also discovered important clues
2020-04-27
We also discovered important clues to domain Geneticin of DGKs and how to exploit these regions for development of DGKα-selective inhibitors. The identification of a probe-modified site at the C1 domain provided the first evidence of a ligand binding site remote from the ATP binding region of DGKs.
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With the recent expanse of technology to evaluate
2020-04-27
With the recent expanse of technology to evaluate synthetic lethality, new combinations with DHODH inhibitors may be uncovered (O\'Neil, Bailey, & Hieter, 2017). Many oncogenic backgrounds share synthetic lethality with DHODH. Cells with mutant PTEN have increased glutamine metabolism and are sensit
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Almost all previously published haplotype association studie
2020-04-27
Almost all previously published haplotype association studies have demonstrated the importance of haplotype reconstruction because the combinations of SNPs exert synergistic effects on protein function. Even synonymous polymorphisms within haplotypes can have functional consequences that are drastic
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br Materials and methods br Results and
2020-04-27
Materials and methods Results and discussion Conclusions In this study, we have investigated the possibility that hierarchical phosphorylation by CK2 may play a role in cellular signal transduction. Hierarchical phosphorylation by CK2 requires multiple consensus determinants with specific s
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The third challenge is to understand the mechanisms of
2020-04-27
The third challenge is to understand the mechanisms of drug resistance. There are several different mechanisms of ES tumor to develop drug resistance. First, cancer stem cells are capable of proliferate and generate tumor cells with new sets of mutations which may harbor different protein targets [1
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br E E backside interaction The E possesses an important
2020-04-26
E3–E2 backside interaction The E2 possesses an important regulatory interface which is termed its backside as it is opposite to the catalytic cleft that bears the active-site cysteine forming the thioester with SUMOD. This backside site interacts noncovalently with a scaffold SUMOB and was origin
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Nicotinic Acid br Material and methods br Results br Discuss
2020-04-26
Material and methods Results Discussion Cysticerci located in host tissues are exposed to several effector mechanisms of the immune system (Flisser et al., 1986; Sciutto et al., 2000; Amit et al., 2011; Singh et al., 2013). In addition, the extensive uptake of host proteins by cysticerci ha
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