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Most human diseases e g cancer diabetes and
2023-09-01
Most human diseases (e.g., cancer, diabetes, and neurodegenerative diseases) are complex and multifactorial. Several investigations in the literature focused on new multi-target drug development, which implies active pharmacophores incorporation in one scaffold (Meunier, 2008, Lazar et al., 2004, Te
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Introduction Heterotrimeric G proteins mediate signal transd
2023-09-01
Introduction Heterotrimeric Gαβγ proteins mediate signal transduction through seven-transmembrane domain receptors. In response to neurotransmitters or hormones, activated receptors bind GTP via the Gα subunit leading to the dissociation of Gα from the Gβγ dimer. G proteins regulate the levels of s
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To further clarify the vascular
2023-09-01
To further clarify the vascular cell types expressing AR subtypes, double immunofluorescence staining for ARs and vascular endothelial Puromycin or vascular smooth muscles was performed. As shown in Fig. 3, Fig. 4, overlay images show the expression of all ARs subtypes that we examined in vascular
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Furthermore new strategies to achieve a total androgen depri
2023-08-31
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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br Conclusion Growth survival and
2023-08-31
Conclusion Growth, survival, and invasion of most PCs have been shown to be androgen-dependent at the onset of castration therapy [31]. Thus, castration therapy has been central to systemic therapy and remains the standard approach to PC treatment. Even after progression to a castration-resistant
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MafB a member of the Maf
2023-08-31
MafB, a member of the Maf protein family, is essential for terminal differentiation of macrophages (Kelly et al., 2000). The phagocytic activity of polystyrene beads was found to be enhanced in U 73343 with exogenous expression of MafB (Tillmanns et al., 2007). However, in alveolar macrophages of do
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Having established the structural requirements for potency i
2023-08-31
Having established the structural requirements for potency in both the biochemical and biomarker (CRA) assays, we evaluated key compounds in the metabolic stability assay. Disappointingly, we found that all compounds had high intrinsic clearances in mouse microsomes. To ascertain whether the in vit
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Illustrated in is the protocol we
2023-08-31
Illustrated in is the protocol we applied for the screens of novel furoic acids as ACL inhibitors. We constructed our furan carboxylate library that contained 1446 2-furoic Parathyroid Hormone (1-34), bovine derivatives and 501 3-furoic acid derivatives by performing substructural searches of the
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The structural analysis of the ASK activation
2023-08-31
The structural analysis of the ASK1 activation segment, which was not phosphorylated in the crystal structure, showed interactions mimicking those found in activated kinases. In addition, the isolated unphosphorylated ASK1-CD is active and able to autophosphorylate itself at three sites, Thr813, Thr
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Songbirds are outstanding models in
2023-08-31
Songbirds are outstanding models in the study of vocal communication (Maney and Pinaud, 2011). Following the pioneering studies of William H. Thorpe and Peter Marler on the development of song in chaffinches (Fringilla coelebs) and white-crowned sparrows (Zonotrichia leucophrys) (Marler, 2004; Thorp
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There are in contrast many studies demonstrating that sex
2023-08-31
There are in contrast many studies demonstrating that sex steroids modulate ochratoxin a processing of stimuli related to reproduction and this correlates with the observation that steroid receptors and aromatase are expressed in many brain nuclei that are part of the olfactory, visual and auditory
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The R pycnus arginase was identical to the published
2023-08-31
The R. pycnus arginase was 65% identical to the published B. caldovelox arginase sequence (AAB06939). Furthermore, the R. pycnus arginase gene was 62%, 45%, 36% and 22% identical to the published arginase sequences from Bacillus thuringiensis (AJI37018), Thermus thermophiles (WP_038039155), Human ar
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Carbenicillin, Disodium Salt mg br Conclusions br Funding Th
2023-08-31
Conclusions Funding This work was supported by a Finnish government subsidy for health science research [grant numbers TYH2012141, TYH 2013218, and TYH 2014216]; the SSAC Foundation [grant numbers SLS-504141 and SLS-693781]; and the Paulo Foundation. The funding sources had no involvement in s
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br Materials and methods br Results
2023-08-31
Materials and methods Results Discussion Diabetic kidney disease (DKD) is the most common cause of end-stage renal disease [15], [16]. The pathogenesis of DKD is not fully understood, and there is no effective treatment. Although previous studies suggested that early lesions of DKD are foun
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br Obstructing SNARE zippering Sharma et
2023-08-31
Obstructing SNARE “zippering” Sharma et al. demonstrated for the first time that in the postmortem AD brains, the level of SNARE complex formation, which is necessary for driving synaptic vesicle fusion at the presynaptic active zone, is significantly reduced [123]. In the absence of changes in e
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