• Later the same group designed and prepared several steroidal

  2024-03-20

  

  Later, the same group designed and prepared several Δ16-steroidal C17 benzoazoles and pyrazines and evaluated their CYP17 and 5α-reductase inhibitory activities, binding to and transactivation of the AR, as well as their antiproliferative effects against two human PC cell lines (LNCaP and LAPC4) [18

• In order to increase the oral

  2024-03-20

  

  In order to increase the oral bioavailability, abiraterone (157) is being used in the form of its 3β-acetoxy prodrug, abiraterone acetate (156). In spite of the fact that high-fat meals increase the oral Schizandrin A of abiraterone acetate (156), it is recommended that this drug should be taken on

• In the current study we provide evidence that enhanced ATX

  2024-03-20

  

  In the current study, we provide evidence that enhanced ATX activity correlates well with increased ATX protein concentration during cholestasis and pregnancy (Fig. 1). Hereby we have ruled out the possibility of ATX enzyme activation in these conditions, e.g. by circulating cholephiles. ATX clearan

• INCB024360 analogue br In vivo visualization of aromatase wi

  2024-03-19

  

  In vivo visualization of aromatase with positron emission tomography (PET) Positron emission tomography (PET) utilizes the high INCB024360 analogue photons formed during the annihilation of positrons to detect the changes in the amount and localization of injected radiopharmaceuticals in the liv

• br Materials and Methods br Results

  2024-03-19

  

  Materials and Methods Results Discussion XHP is a traditional Chinese anti-cancer medicine that is widely used for the treatment and adjuvant treatment of breast cancer. XHP has been shown to induce apoptosis in various breast cancer mct inhibitor in vitro, including Hs578T, MCF-7, and MDA

• Echinocandin resistance is systematically associated with

  2024-03-19

  

  Echinocandin resistance is systematically associated with point mutations in either FSK1 or FSK2 genes [7], [104]. These mutations are located in two different not spot regions of these genes named HS1 and HS2. Hot spot mutations have been reported in C. albicans, C. glabrata, C. tropicalis, C. krus

• br Acknowledgements br Introduction Microbial enzymes have g

  2024-03-19

  

  Acknowledgements Introduction Microbial enzymes have gained interest for their widespread uses in industries and medicine owing to their stability, catalytic activity, and ease of production and optimization than plant and animal enzymes (Singh et al., 2016). Microbial aminopeptidases (amino-a

• It thus appeared reasonable that AR needed to

  2024-03-19

  

  It thus appeared reasonable that AR needed to be inhibited and great experimental efforts began which are still on-going [6]. Indeed, hundreds of ARIs have been characterized but no significant drug development has followed. The case of Sorbinil, which did not pass clinical trials is emblematic [7]

• Differentiation of skeletal myoblasts is

  2024-03-19

  

  Differentiation of skeletal myoblasts is a tightly orchestrated process that involves myoblast proliferation, Proteinase K withdrawal, expression of muscle-specific genes, and fusion into multinucleated myofibers (Horsley and Pavlath, 2004; Krauss, 2010). The maintenance of muscle mass is important

• br Introduction Clinical manifestations of Alzheimer s disea

  2024-03-19

  

  Introduction Clinical manifestations of Alzheimer's disease (AD) are mainly characterized by progressive intellectual deterioration, memory impairment, cognitive impairment, and psychiatric symptoms. The pathogenesis of AD remains unclear, mainly containing genetic factors, neurotransmitter disor

• We observed PACAP immunoreactivity in the molecular layer of

  2024-03-19

  

  We observed PACAP2 immunoreactivity in the molecular layer of the cerebellar cortex in zebrafish. This result is consistent with the reporting of PACAP immunoreactivity in the soma and fibers of Purkinje cells and the presence of PACAP mRNA in the Purkinje-cell and granular-cell layers in rats [43].

• Because of its role in tumor growth proliferation and

  2024-03-18

  

  Because of its role in tumor growth, proliferation and metastasis, Axl is considered a therapeutic target. Several Axl inhibitors, including low-molecular-weight agents and antibodies, have been reported. Axl inhibition, using low-molecular-weight inhibitors or shRNA knockdown, resulted in reduced t

• In the last decade the zebrafish has emerged as a

  2024-03-18

  

  In the last decade, the zebrafish has emerged as a valuable vertebrate model to systematically dissect the genetic underpinnings of both vertebrate heart development and function [8,9], as well as distinct cardiac diseases such as congenital heart disease [10], cardiomyopathies [11,12] and cardiac a

• br Acknowledgements We would like to thank

  2024-03-18

  

  Acknowledgements We would like to thank Dr. Thomas Blanpied, Sai Sachin Divakaruni, Dr. Helmut Kessels, Feline Lindhout, Dieudonnée van de Willige, and all members of the MacGillavry lab for discussions and critical reading of the manuscript. This work was supported by NWO (ALW-VENI 863.13.020, A

• Therefore the rational design of target compounds is based

  2024-03-18

  

  Therefore, the rational design of target compounds is based on the hybrid of attractive phenotypic bis-indole (5, Fig. 1) and sulfonamide moieties, in which the indole core might anticipate in hydrophobic interaction, and the functionality of sulfonamide group may involve in H-bonding with the site

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