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Furthermore new strategies to achieve a total androgen depri
2024-12-12

Furthermore, new strategies to achieve a total androgen deprivation namely by blocking either androgen biosynthesis as well as AR are being considered and should be a relevant topic in the near future. A successful example of this approach is galeterone (159), which not only inhibits the CYP17 enzym
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Bioavailability has been defined as
2024-12-11

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
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Furthermore we also found that
2024-12-11

Furthermore, we also found that the basic level of ROS was markedly lower in mtDNA-reduced SW480 Adriamycin receptor than that in the parent cells. Endogenous ROS is most notably produced at the sites of complex I and complex III [5], it might be plausible that the decreased quantity of ROS observe
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It is now thought that tight binding of HMGB to
2024-12-11

It is now thought that tight binding of HMGB to condensed chromatin may not be restricted to apoptotic cells. That HMGB proteins might actually be involved in the organization and/or maintenance of heterochromatic regions is suggested by the results of experiments analyzing the stable binding of the
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br Mechanism of action In general the main
2024-12-11

Mechanism of action In general, the main targets for antifungal drug development are cell wall polymer (glucans, chitin, mannoproteins), cell membrane (especially ergosterol) biosynthesis, DNA and protein synthesis (topoisomerases, nucleases, elongation factors and myristoylation), and signal tra
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Introduction Plant pathogenic fungi are major pathogens
2024-12-11

Introduction Plant pathogenic fungi are major pathogens in agricultural diseases and the cause of large crop losses worldwide. There are many kinds of plant pathogenic fungi, with various modes of action. For example, Botrytis cinerea (B. cinerea) is the disease pathogen in the economically importa
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The sequential behavioral approach used in the
2024-12-11

The sequential behavioral approach used in the present study reinforced the involvement of the BDNF/TRKB system in the effect of losartan. In mice with dampened BDNF expression, losartan was no longer able to exert antidepressant-like effects. Similar to what was observed after losartan treatment, t
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br Material and methods br Results br
2024-12-11

Material and methods Results Discussion In order to find new and improved ways of treating type 2 diabetes (T2D) and other related conditions it is vital that investigators gain a more in-depth understanding of the effects that anti-diabetic treatments, such as TZDs, have on molecules impli
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It thus appeared reasonable that AR
2024-12-11

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]
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Spectroscopic techniques are powerful biophysical tools used
2024-12-11

Spectroscopic techniques are powerful biophysical tools used in the study of biomolecular structures, including those of proteins. UV–Vis conotoxin receptor spectroscopy makes use of absorption property of the protein peptide backbone at around 218 nm, and aromatic amino acid residues primarily at
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To validate the identified phosphorylation sites in the
2024-12-11

To validate the identified phosphorylation sites in the mouse heart, we analyzed HEK 293T mitomycin transfected with Adrb1 based on the hypothesis that protein residues phosphorylated both in vivo and in vitro are more likely to be physiologically relevant. All of the phosphorylation sites identifi
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Application of the broad acting HTR antagonist methiothepin
2024-12-11

Application of the broad-acting 5-HTR antagonist methiothepin (Bard et al., 1996, Hoyer et al., 1994, Peroutka, 1990) converted the TBS-induced response of both thalamocortical and intracortical A1 synapses from LTP to LTD, an effect that was mimicked by the selective 5-HT2R antagonist ketanserin (L
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A selected set of these
2024-12-10

A selected set of these new derivatives was then used for functional assays at the human A1AR showing, as expected, an antagonist profile with IC50 values at nanomolar level. The same molecules showed also to be efficacious as nanomolar antagonists in a functional assay aimed at analyzing their abil
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To better understand the pathophysiology of ASDs we would ne
2024-12-10

To better understand the pathophysiology of ASDs, we would need comprehensive information on a) the functions of ASD-associated proteins in the brain, b) how mutations affect the expression level and function of these proteins, c) how mutations affect their function in neurons, and d) how changed ne
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This raises an important question May the lack of
2024-12-10

This raises an important question: May the lack of ethnolinguistic theories and of explicit references to language be related to the lack of contact with other groups and their languages? For the past few centuries at least, the Aché seem to have been culturally and linguistically isolated (Hill and
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