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Perhexiline maleate In terms of the ring B C position while
2024-08-14

In terms of the ring B C5′ position, while C5′-F (compound ) was tolerated, C5′-Me (compound ) and C5′-Cl (compound ) substitutions resulted in a loss in potency. However, the C5′-OMe substitution (compound ) resulted in a ∼3-fold increase in potency compared to . Modeling suggested a pseudo hydroge
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Thus one possible target for CRPC treatment is the
2024-08-14

Thus one possible target for CRPC treatment is the enzyme 17,20-lyase, which plays a crucial role in androgen biosynthesis. This is because inhibition of 17,20-lyase would be expected to decrease serum androgen levels secreted not only by the testes but also by the adrenal glands.7, 8, 9 In recent
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br Results br Discussion Autophagy is considered as an
2024-08-14

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
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The co crystal structure of blebbistatin bound to myosin
2024-08-14

The co-crystal structure of ()-blebbistatin ()- bound to myosin II (PDB: ) was used to scout for possible favorable interactions with the residues lining the binding pocket. Looking at A, we hypothesized that -oriented hydrophilic moieties (e.g. hydroxymethyl) on C of the blebbistatin scaffold migh
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br Acknowledgments br Protein microarrays were developed to
2024-08-14

Acknowledgments Protein microarrays were developed to provide miniaturized high-throughput tools to study protein function, galactoside and post-translational modifications. Just a few years ago, the seminal work performed in Stuart Schreiber's laboratory at Harvard University () and at Michael
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Assessment of antibiotic appropriateness is receiving increa
2024-08-14

Assessment of antibiotic appropriateness is receiving increased attention in the face of growing concerns about the emergence of MDROs, as well as the rise in adverse outcomes associated with antibiotic use such as C. difficile infection. In this study, 15% of cultured Gram-negative organisms met th
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Histochemical analyses using antibody or cDNA
2024-08-13

Histochemical analyses using antibody or cDNA probes reveal the precise cellular location of the 12S-lipoxygenases in tissues of interest. An immunohistochemical study in various rat tissues showed specific expression of the leukocyte-type 12S-lipoxygenase in macrophages in lung and spleen [27]. In
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The first suggestions that the cleaved intracellular domain
2024-08-13

The first suggestions that the cleaved intracellular domain of APP, AICD, might transit to the nucleus and hence selectively regulate gene transcription arose from analogies with the Notch receptor signalling system where similar intra-membrane proteolysis occurs [84], [85] and it was later confirme
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The role of DHT in early
2024-08-13

The role of DHT in early teleost embryogenesis is not entirely clear or established, however additional studies that treat fish embryos to DHT or to specific srd5a inhibitors at critical stages of development (i.e. prior to sex differentiation) will shed light on the early functions of this androgen
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These results from the present study
2024-08-13

These results from the present study are summarized in Table 1. Eight drugs (doxorubicin, epirubicin, daunorubicin, idarubicin, irinotecan, imatinib, sunitinib and gefitinib) inhibited 5-HT-induced 5-HT3A and 5-HT3AB currents; three (irinotecan, topotecan and mitoxantrone) showed different responses
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In the nineties we knew that baclofen was
2024-08-13

In the nineties we knew that (-)baclofen was the stereo-selective ligand for the GABAB receptor which had been recognised by Norman Bowery as a receptor for GABA, which was different from the GABAA receptor (Hill and Bowery, 1981). GABAB receptor antagonists were also synthesised and made available
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The mitochondrial protein AIF was the first caspase independ
2024-08-12

The mitochondrial protein AIF was the first caspase-independent death effector. AIF can induce caspase-independent chromatin condensation and large-scale DNA fragmentation to approximately 50 KB. AIF that is released to cytoplasm can mediate apoptosis when special extracellular signals trigger the o
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br Application of bamboo in the food and
2024-08-12

Application of bamboo in the food and pharmaceutical industry For decades, the application of antioxidants in the food and pharmaceutical industry has been widespread. In the past, antioxidants were previously used to control oxidation and retard spoilage but today, many are used because of putat
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eif2a Previous studies demonstrate that chiral
2024-08-12

Previous studies demonstrate that chiral biointerface has great influence on cells adhesion and proteins adsorption [39], [40], [41], [42], [43], which inspired us to further develop antimicrobial materials or surfaces by taking advantage of the “chiral taste” of microbes. L-borneol is a hydrophobic
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br Concluding Remarks and Future Perspectives Fluorescent an
2024-08-12

Concluding Remarks and Future Perspectives Fluorescent Fusaric Acid have helped researchers to elucidate antibiotic MOA and off-target interactions, to screen for new antibiotics, to detect antibiotics in the environment, to track antibiotic uptake throughout cells and organisms, and to detect b
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