• In order to improve the methodology

  2024-06-25

  

  In order to improve the methodology of the synthesis of steroidal derivatives, our goal was the investigation of aza-Michael addition of different N-nucleophiles to 16-dehydropregnenolone in the presence of [DBU][OAc] as catalyst and reaction medium. Michael addition of electron deficient steroidal

• Steroidal CYP inhibitors can further be

  2024-06-25

  

  Steroidal CYP17 inhibitors can further be classified based on their mode of action, namely as mechanism-based inhibitors and type I and type II competitive inhibitors [129]. Recent studies investigated other biological targets than CYP17, and some new compounds have shown interesting dual activity a

• br Patients and Methods br Results br Discussion

  2024-06-25

  

  Patients and Methods Results Discussion Gjerdrum et al showed that Axl 3965 is required to maintain the mesenchymal-like invasiveness of metastatic breast carcinoma cells, but Axl knockdown has no effect on the cell proliferation of MDA-MB-231 cells. Mackiewicz et al also showed that down-

• br Results br Discussion Autophagy is considered as

  2024-06-25

  

  Results Discussion Autophagy is considered as an important process in physiological and pathological ovarian function. It is related mainly to follicular atresia and CL regression (for review see [20]). However, an involvement in luteal cell survival is also proposed [21], [22]. The present st

• While the yeasts and see Glossary each contain

  2024-06-25

  

  While the yeasts and (see Glossary) each contain only one Aurora homolog, Ipl1p (increase in ploidy 1) and Ark1 (Aurora-related kinase 1), respectively 5, 6, , and Xenopus laevis contain two Aurora kinases: Aurora A and Aurora B [4]. Mammals have three Aurora kinases, A, B, and C (Figure 1). In an

• br Author contributions br Acknowledgments TJC KW

  2024-06-25

  

  Author contributions Acknowledgments TJC, KW, and VG are supported by awards made to MJN: a Consolidator Grant from the European Research Council under Grant no. 311336; a University Research Fellowship from the Royal Society, and a Career Development Award from the Human Frontiers Science Pro

• The class C receptors also share a

  2024-06-25

  

  The class C receptors also share a common agonist-binding mode. In all cases, an agonist induces VFT closure by forming intermolecular bonds with surface residues in both the LB1 and LB2 domains (Geng et al., 2013, Geng et al., 2016, Kunishima et al., 2000, Muto et al., 2007, Nuemket et al., 2017, T

• Several structural classes of ASK inhibitors mostly

  2024-06-25

  

  Several structural GSK2606414 of ASK1 inhibitors, mostly from industry but also from academia, have been identified over the last decade. In 2012, Terao et al. (Takeda) reported imidazo[1,2-α]pyridine () as a potent ASK1 inhibitor derived from structure-based drug design. GSK, Merck and Gilead rev

• Secondly leptin has been shown

  2024-06-25

  

  Secondly, leptin has been shown to enhance aromatase mRNA expression, aromatase content and its enzymatic activity in epithelial breast cancer Capecitabine receptor by inducing promoters II and I.3 via an enhanced binding of transcription activator protein 1 (AP-1) complex to specific DNA sites in

• Based on the results of studies

  2024-06-25

  

  Based on the results of studies done to-date, there are three characteristics that make a letrozole-based protocol attractive for use in cattle: 1) it is steroid-free, 2) it is cost-effective and requires a shorter time and fewer animal handlings than conventional methods (Table 1), and 3) it may ha

• Bioavailability has been defined as

  2024-06-25

  

  Bioavailability has been defined as the amount of a drug given by any route, other than intravenously, that reaches general circulation and is available at the site of action [86]. The low bioavailability observed with the initial intravaginal devices (16%) was attributed to the melting point of the

• In spite of this unexpectedly after three week

  2024-06-24

  

  In spite of this, unexpectedly, after three-week cherry puree consumption no AC increase was observed, irrespective of the method used (Table 2). A statistically significant decrease of AC was even measured by LOX-FL and ORAC methods (−3.5% and −9%, respectively). Nevertheless, a much more evident d

• Interestingly we found that co treatment with losartan preve

  2024-06-24

  

  Interestingly, we found that co-treatment with losartan prevented the increased participation of ROS from NADPH oxidase on the contractile response to Phe observed in Hg-treated rats. Moreover, losartan also prevented the reduction in the endothelial NO modulation of this response found in treated a

• FH1 Recent retrospective cohort studies have supported these

  2024-06-24

  

  Recent retrospective cohort studies have supported these preclinical findings in animals indicating the correlation of AR activation with the induction of FH1 carcinogenesis. First, men with prostate cancer who underwent androgen deprivation therapy were shown to have a significantly lower risk of s

• Thus far a tight coupling has

  2024-06-24

  

  Thus far, a tight coupling has been observed between mAbs that target aggregated Aβ and the occurrence of ARIA. If ARIA-E is caused by increased trafficking to and clearance of fibrillar Aβ from cerebral vessels (20), mAbs could be designed with conformationally specific epitopes selective for solu

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