• Besides degrading cholesterol the cholesterol degradation pa

  2021-04-20

  

  Besides degrading cholesterol, the cholesterol degradation pathway also offers a route to obtain useful starting materials for the production of steroid drugs and hormones. Indeed, steroids are among the most marketed pharmaceuticals with about 300 approved steroid drugs [15] and a worldwide market

• Numerous small molecule CRF receptor antagonists have been r

  2021-04-19

  

  Numerous small molecule CRF receptor antagonists have been reported in the literature. Some representative examples are shown in . In preclinical studies (DMP696), , was found to be efficacious in preclinical behavioral models for anxiety and depression. In an open label clinical trial with (R121919

• chenodeoxycholic acid Three new trans P Hs AlP H

  2021-04-19

  

  Three new trans-P4Hs (AlP4H, MiP4H and ScP4H) discovered by a genome mining approach in this study were all located in branch A containing DaP4H sequence. Although another three candidates from Amycolatopsis mediterranei, Bradyrhizobium sp. ORS285 and O. indicum were successfully expressed as solubl

• This structure guided the variation of the compounds aiming

  2021-04-19

  

  This structure guided the variation of the compounds aiming either at enhanced interaction with CK1 or to exclude interaction with CK1 (R=Me, 15). We chose the 5-cloro substituted oxoindole as backbone as it is supposed to show enhanced metabolic stability, which is commonly used in medicinal chemis

• It is now well accepted that increased local

  2021-04-19

  

  It is now well accepted that increased local estrogen levels are associated with both the onset and growth of breast cancer. Tissue concentrations of estradiol (E2) in breast cancer are 10 times higher than that found in plasma [12]. Breast cancer tissues also contain increased activity and expressi

• To further define the importance of CYP

  2021-04-19

  

  To further define the importance of CYP3A for OSC metabolism in vivo, a strong CYP3A inhibitor ketoconazole was used to test whether CYP3A would affect its metabolism. As expected, the biotransformation of OSC to SC was significantly decreased by ketoconazole at all three substrate concentrations. H

• br Introduction Epidermal growth factor

  2021-04-19

  

  Introduction Epidermal growth factor receptor (EGFR)-activating-mutant non-small cell lung cancer (NSCLC) often initially responds well to EGFR tyrosine kinase inhibitors (TKIs) (Haber et al., 2011); however, the disease almost always recurs about 10–13 months of therapy. Analysis of clinical spe

• Palifosfamide OHC is a potent regulator of LXR

  2021-04-19

  

  25-OHC is a potent regulator of LXR-mediated pathways, that impact on Palifosfamide lipid homeostasis [8]. This oxysterol affects expression of the cholesterol efflux pumps ATP-binding cassette transporter (ABC)A1 [9] and ABCG1, and expression of apolipoprotein E [10], [11], [12]. 25-OHC is able to

• br EBV Infection Epstein Barr virus

  2021-04-19

  

  EBV Infection Epstein–Barr virus (EBV, human herpesvirus 4) was discovered 50 years ago, when Epstein, Achong, and Barr used electron microscopy to identify viral particles in Burkitt's lymphoma cells. It belongs to the lymphocryptovirus (LCV) genus of the gammaherpesvirus subfamily (Fig. 1A). Th

• In addition to glutamatergic inputs

  2021-04-19

  

  In addition to glutamatergic inputs, the RTn integrates cholinergic, serotonergic and noradrenergic synapses of fibers coming from nuclei located in the brainstem (Asanuma, 1992, Morrison and Foote, 1986, Pare et al., 1988) involved in the alternating firing mode and in the frequency changes of reti

• br Acknowledgments Studies in the Tomkinson laboratory on DN

  2021-04-19

  

  Acknowledgments Studies in the Tomkinson laboratory on DNA ligase III are supported by research grants from the National Institutes of Health (P01 CA92584 and ES12512 to AET), a grant from the V Foundation and the University of New Mexico Cancer Center. Introduction Ionizing radiation (IR) as

• An even more striking difference is observed when

  2021-04-19

  

  An even more striking difference is observed when comparing active site residues, which are evolutionarily very well conserved in other soluble PPases 18, 19. In 31 known PPase sequences, 13 functionally important active site residues are conserved in all sequences, but only two of them (D70 and D97

• Recently we have demonstrated that the synthesis of cysteiny

  2021-04-17

  

  Recently we have demonstrated that the synthesis of cysteinyl-LTs from LTA4 by human umbilical vein endothelial cells (HUVECs) is directly associated with the activation of the CysLT2 receptor (CysLT2R) in a typical autocrine fashion, and that solely the CysLT2R is responsible for the increase in in

• Berner et al used a

  2021-04-17

  

  Berner et al used a meta-analysis to show that sildenafil resulted in an effect of 9.65-point improvement. Tadalafil could be pooled into an effect of 8.52-point improvement, and vardenafil showed an effect of 7.50-point improvement. In our present studies, 200 mg udenafil resulted in an effect of 8

• In the present study we examined whether the gene for

  2021-04-17

  

  In the present study we examined whether the gene for estrogen receptor alpha, Esr1, plays a role in the expression of maternal memory in female rats. The approach utilized a newly developed rat Esr1 knockout (KO) rat model (Rumi et al., 2014) to evaluate whether deletion of the Esr1 k145 australia

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