• Replacement of the saturated propoxy group

  2020-11-27

  

  Replacement of the saturated -propoxy group in compound with the unsaturated allyloxy group to obtain compound resulted in 10-fold decrease in ET receptor antagonism and more than 20-fold decrease in ET-selectivity. Analogous unsaturated allyloxy compound in the tetrazole series was found to have

• More importantly Santagata et al have

  2020-11-27

  

  More importantly, Santagata et al. have suggested a new breast cancer subtyping method according to ER, androgen receptor (AR), and VDR with a higher prognostic value than the ordinarily used method based on ER, progesterone receptor (PR) and Her2 (Santagata et al., 2014). This implies that such com

• For the current studies we used the

  2020-11-27

  

  For the current studies, we used the selective Epac agonist 8CPT-AM to directly activate the proteins. We chose this pharmacological approach since it allows a direct activation of Epacs rather than using receptor agonists such as PGE2 which could introduce confounding variables. One potential conce

• PRT062607 Hydrochloride Here two labs that helped characteri

  2020-11-27

  

  Here, two labs that helped characterize these two pathways have worked together to further test whether these apparently parallel pathways from β-AR to CaMKII-RyR might be related in series. Much of the work leading to the Epac pathway involved measurement of Ca sparks as an index of SR Ca leak, oft

• The ADME profile of AAT was very promising with high

  2020-11-27

  

  The ADME profile of AAT-008 () was very promising, with high stability in HLM. The pre-clinical pharmacokinetic properties of AAT-008 were also assessed in rats (Sprague-Dawley, male), dogs (beagle, male), and monkeys (cynomolgus, male). The experimentally determined parameters are summarized in . A

• The purpose of this study is to investigate

  2020-11-27

  

  The purpose of this study is to investigate KDM1B expression and its functional significance in PC. We used lentivirus-mediated shRNA to down-regulate KDM1B expression in PC cell lines in vitro and detected the changes of cell proliferation and apoptosis. These studies provided a novel insight into

• Among the Ub interactions observed in

  2020-11-27

  

  Among the ~Ub interactions observed in the HOIP structure is one that involves a RING2 domain (from the non-cognate HOIP) [47]. A similar binding interaction was defined between HHARI RING2 and the hydrophobic patch on Ub by NMR [54]. HHARI RING2 mutations that ablate the interaction inhibit formati

• Taken together these assays demonstrate that SUMOD

  2020-11-27

  

  Taken together, these assays demonstrate that SUMOD positioning is essential for all E3 ligases but dispensable for E2 and S*E2 sumoylation reactions. Thus, we propose SUMOD positioning as a key criterion to describe the enzymatic function of SUMO E3 ligases that distinguishes them from other enhanc

• Pol is responsible for the

  2020-11-27

  

  Pol ε is responsible for the bulk of leading-strand synthesis in vivo (Daigaku et al., 2015, Nick McElhinny et al., 2008, Pursell et al., 2007) and physically associates with CMG (Langston et al., 2014, Sengupta et al., 2013, Sun et al., 2015, Zhou et al., 2017). Furthermore, leading-strand synthesi

• In summary these results are consistent with

  2020-11-27

  

  In summary, these results are consistent with our hypothesis that chemical nitrosation of BMAA to N-BMAA results in the formation of an alkylating agent. Furthermore, we have shown that N-BMAA is more toxic than BMAA itself. Previously, methylazoxymethanol (MAM), which is also present in the cycad n

• ASC was reported as a potent antiviral and antifungal agent

  2020-11-27

  

  ASC was reported as a potent antiviral and antifungal agent, and its derivatives could modulate a variety of physiological activities, such as anti-tumor, anti-metastatic, and anti-diabetic activities in animals. Mie Tsuruga et al. found that 4-o-methylascochlorin had immunosuppressive activity, but

• A series of monocarboxylated chalcones e g compounds and

  2020-11-26

  

  A series of monocarboxylated chalcones (e.g. compounds 7 and 8, Fig. 2A) was previously identified as good CysLT1 antagonists [20], and none of them exhibited CysLT2 antagonistic activities (Supplementary Table S1). This study was consistent with reported result that CysLT2 PLX7904 was not sensitiv

• Preparation of the pyridyl ether analogs

  2020-11-26

  

  Preparation of the 2-pyridyl ether analogs (–) was accomplished by alkylation of alcohol with 2-bromopyridines in the presence of NaH to afford the desired pyridyl ether analogs in low to moderate yield. Preparation of the 3-pyridyl analog was carried out by conversion of alcohol to the tosylate, fo

• Following mutagenesis of the glucarpidase gene

  2020-11-26

  

  Following mutagenesis of the glucarpidase gene of Pseudomonas sp. strain RS-16 [30], approximately 73% of the clones retained enzyme activity, as indicated by the clear zones and yellow precipitate surrounding their colonies. However, there were very few that had ‘halos’ around colonies that were da

• br Overall system architecture In this section we provide

  2020-11-26

  

  Overall system architecture In this stat 3 inhibitor section we provide a description of the system under study, and its surrounding environment, on an “as is” basis. The architecture presented in the following is the one currently adopted on-field by ASTS (e.g., at Rome train station). The Tra

16370 records 794/1092 page Previous Next First page 上5页 791792793794795 下5页 Last page