• Since our new compound Fex could be a new

  2021-10-28

  

  Since our new compound Fex-3 could be a new FXR ligand, we try to demonstrate that Fex-3 was an intestinal-restricted FXR agonist which only activated FXR in the intestine not in the liver or other organs. Initially, we investigated this in Caco-2 pyruvate dehydrogenase kinase inhibitor with transw

• Pyr3 C prevents the glutamate and erastin

  2021-10-28

  

  C16 prevents the glutamate- and erastin-induced ROS accumulation but does not affect the decrease in GSH, indicating that prevention of ROS accumulation by C16 is not due to the restoration of GSH levels. Instead, C16 itself possessed superoxide anion scavenging activity in vitro at similar concentr

• Tubastatin A HCl Considering their good FAAH inhibitory acti

  2021-10-28

  

  Considering their good FAAH inhibitory activity, compounds and have been selected for an in vivo study in a DSS-induced colitis model. Specific Pathogen Free male 7weeks old C57/Bl6 mice received 2.5% DSS in drinking water during 8days. Concomitantly, they were administrated daily intraperitoneall

• br Discussion This study dedicated to histamine H and

  2021-10-28

  

  Discussion This study, dedicated to Pralatrexate H3 and H4 receptors, was carried out on superfused tissues preincubated with 3H-choline or 3H-noradrenaline; electrical stimulation was used to elicit quasi-physiological exocytotic release of the respective transmitter. Since inhibition of transm

• In mammalian cells Motins have

  2021-10-27

  

  In mammalian cells, Motins have been identified as a key link between F-actin and Hippo pathway regulation, as knockdown of all three Motins increased Yap activity even in the presence of cytoskeletal disruption [105]. Motins can physically associate with F-actin but this association is blocked by p

• Almost all of the series and compounds exhibited

  2021-10-27

  

  Almost all of the series and compounds exhibited higher activities compared with the compounds in the other series. In these series, the tetrazole group was directly linked to a nitrogen atom of the amide group at the C-28 position, and the C-3 hydroxy group was either unmodified, oxidized, esteri

• For further understanding of the interaction between these i

  2021-10-27

  

  For further understanding of the interaction between these inhibitors and proteins (BRafV600E and HDAC1) for guiding the SAR, compound 10e, the most potent compound of this series, was chosen as a representative for docking into the BRafV600E (PDB code: 1UWJ) and HDAC1 (PDB code: 1C3R), revealing ex

• In summary our findings support

  2021-10-27

  

  In summary, our findings support the hypothesis that activation of GPR55 protects against deficits in neurogenesis induced by inflammatory insult both in vitro and in vivo through direct targeting of NSCs. Better understanding of the mechanisms by which GPR55 provides neuroprotection is critically n

• In the present study recipient oestradiol serum levels on

  2021-10-27

  

  In the present study, recipient oestradiol serum levels on the day of donor oocyte retrieval or warming were found to be significantly higher in the antagonist group and higher than 100 pg/ml in all cases. Serum oestradiol level has been reported to have no effect on endometrial receptiveness in ooc

• Our initial lead optimization started with the modification

  2021-10-27

  

  Our initial lead optimization started with the modification of the indole head group as summarized in . Extensive exploration indicated that there was limited tolerance of structural change in this region of the molecule. All of the modifications to the indole moiety, including N-substitution (), li

• Using data from a large

  2021-10-27

  

  Using data from a large population-based cohort study in Finnish males and females, Suchankova et al. [97] looked at a subset of the aforementioned SNPs, namely one SNP on GHSR (rs2948694) and two SNPs on GHRL (rs4684677 and rs696217), in relation to alcohol use disorders identification test (AUDIT)

• G quadruplex structures can be resolved by helicases Consist

  2021-10-27

  

  G-quadruplex structures can be resolved by helicases. Consistently, many helicases are aberrantly expressed in cancer sigma receptor [47]. In this study, we correlated HOXC10 expression with that of all helicases using a microarray dataset derived from 759 breast cancer patients [36] and discovered

• In a follow up study the same

  2021-10-27

  

  In a follow up study, the same research group further characterized FFA4 involvement in DU145 and PC-3 cancer cell lines by demonstrating that the anti-proliferative and anti-migration activities of FFA4 require the presence of LPA1 receptor (LPA1R), suggesting a mechanism consistent with negative c

• We tested formyl MYVKWPWYVWL which we had

  2021-10-27

  

  We tested formyl-MYVKWPWYVWL, which we had previously shown to have essentially identical Kis for W190/N192, R190/K192 and R190/N190 [8] of 130 nM, for its ability to downregulate surface receptor (Fig. 5A). R190/K192 exhibited the lowest EC50 of 44±4 nM about 3 fold below the observed Ki and a maxi

• We have expanded these studies by doing EEG recording in

  2021-10-27

  

  We have expanded these studies by doing EEG recording in the ET-1 model. Using this technique, we demonstrated that activation of either the ETA CPI-455 or the ETB receptor induces electrical seizures. ET-1 induced electrical seizures occurred in the presence of either the ETA receptor antagonist or

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