• Several dehidropregnenolone derivatives functionalized at C

  2024-04-19

  

  Several 16-dehidropregnenolone derivatives functionalized at C3, C4, C5 and C6 (Fig. 7) were prepared and evaluated as 5α-reductase inhibitors bearing in mind that after the formation of an enzyme-steroid complex a nucleophilic portion of the enzyme attacks the double bond of the steroid through Mic

• br Materials and methods br Results br Discussion Many studi

  2024-04-19

  

  Materials and methods Results Discussion Many studies investigate the role of 12/15-LOX in cancer cell,23, 24, 25 however we here first found that host 12/15-LOX also plays an important role in metastasis progression. We have demonstrated that 12(S)-HETE increased melanoma cell adhesion to

• exemplifies three of the compounds investigated in

  2024-04-19

  

  exemplifies three of the compounds investigated in the selection for a candidate drug (CD). Our first criteria was an IC The ap-1 as such did not show any genotoxicity in the SOS/umu assay, but this does not say anything about any possible genotoxicity of its metabolites or degradation products. A

• citco Another factor that is involved in the severity of EAE

  2024-04-19

  

  Another factor that is involved in the severity of EAE is apoptosis signal-regulating kinase 1 (ASK1), which is one of a growing number of mitogen-activated protein kinase (MAPK) kinase kinases identified in the upstream of the c-Jun N-terminal kinase and p38 MAPK pathways [12]. We previously report

• br Current limitations and future directions There are sever

  2024-04-19

  

  Current limitations and future directions There are several limitations associated with PET imaging of aromatase using carbon-11 labeled aromatase inhibitors. Due to the very short half-life of carbon 11 (20min), PET studies with currently available, validated tracers can only be performed in med

• Introduction Cytochrome P CYP aromatase catalyzes the conver

  2024-04-19

  

  Introduction Cytochrome P450 19 (CYP19; aromatase) catalyzes the conversion of androgens to estrogens in a three-reaction sequence, where each step depends on NADPH and O2 [[1], [2], [3]]. The first two steps are accepted to be hydroxylations of the steroid C19 methyl group, whereas the final step

• Once apoptosis has been initiated the

  2024-04-19

  

  Once apoptosis has been initiated the HMGA proteins themselves undergo marked changes in both the types and extent of their post-translational modifications (PTMs; review in [149,175]), some of which are likely correlated with alterations in chromatin structure. For example, the early stages of apop

• There are increasing repeated reports

  2024-04-19

  

  There are increasing repeated reports of amphotericin B-resistance in pathogenic fungi including Candida spp. [35], [36]. Nolte et al. characterized some fluconazole and amphotericin B-resistant Candida albicans isolates from leukemia patients [37]. Fan-Havard et al. (1991) have shown multi-antifun

• Tetracyclines constitute one of the

  2024-04-19

  

  Tetracyclines constitute one of the most important antibiotic groups used as veterinary and human medicine and as feed additives in the agricultural sector (Li et al., 2011a, Simon, 2005). Annual worldwide production of tetracyclines is estimated to be in the thousands of tons (Michalova et al., 200

• br Selective Androgen Receptor Modulators SARMs The AR and

  2024-04-18

  

  Selective Androgen Receptor Modulators (SARMs) The AR and its endogenous ligands, androgens, are important for development and maintenance of muscle and bone, secondary sexual organs, and development of other tissues (Mooradian et al., 1987). Although androgens are important for normal developmen

• ac 723 receptor br Conclusion We have identified three non c

  2024-04-18

  

  Conclusion We have identified three non-competitive inhibitors of the human and porcine APN with Ki values in the μM range, by combining virtual screening and kinetic assays. Molecular docking simulations suggest these novel inhibitors block APN activity by an alternative mechanism to Zn coordina

• br Materials and methods br Results

  2024-04-18

  

  Materials and methods Results Discussion The novel and central finding of the current study is that endothelial 12/15-LO rather than the monocytic/macrophagic 12/15-LO has a critical role in hyperglycemia-induced leukocyte adhesion and retinal endothelial barrier dysfunction. The following

• In previous research we determined that blocking

  2024-04-18

  

  In previous research, we determined that blocking mAC during heparin-induced capacitation result in sperm having a lesser oxygen consumption, suggesting that cAMP produced by this enzyme would be linked to mitochondrial activity and, therefore, with the regulation of sperm metabolism (Fernández and

• We have previously shown that the human gonadotropins

  2024-04-18

  

  We have previously shown that the human gonadotropins hLH and hCG trigger a partly irreversible stimulation of intracellular cyclic AMP accumulation in mouse Leydig Tumor Tryptone (MLTC) in contrast to all other tested mammalian LHs and CG (Klett et al., 2016). In order to get a better insight in th

• The UV vis and fluorescence spectra have been

  2024-04-18

  

  The UV–vis and fluorescence spectra have been used to study the interaction between small chemical molecules and biomolecules (Punith and Seetharamappa, 2012). The UV Phosphate Colorimetric Assay Kit peak of the protein changes with the microenvironment of the chromophore. That is, the peaks may sh

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