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br Conclusion There have been multiple clinical trials
2023-09-22
Conclusion There have been multiple clinical trials and pre-clinical studies that have tested the utility of 5ARIs in treating prostate disease, as summarized in Fig. 1. Inhibiting androgen action through the use of finasteride and dutasteride has been established as a valuable resource for physi
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To test the compounds metabolic stability we measured
2023-09-22
To test the compounds metabolic stability, we measured the half-life of compounds and in mouse hepatic microsomes (1mg/mL) and found them to have modest stability, with half-lives of 7.5 and 2.9min respectively, indicating these compounds may be unsuitable for studies. In order to gain structural i
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An alternative more rarely used electron
2023-09-22
An alternative, more rarely used, electron microscopy-based approach exploits labeling of phagosomes with DAMP (3-(2,4-dinitroanilino)-30-amino-N-methyldipropylamine). DAMP is a weakly basic compound which is membrane-impermeable once it has been protonated. This way, DAMPH+ accumulates in acidic in
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The Type A series contains
2023-09-22
The Type-A series contains 6 of the 11 confirmed hits, making it a highly attractive lead template. Seven (7) out of 8 Type-A series of 3-substituted-2-furoic acids are highly active (84–100% inhibition) at the high concentration of 100μM. We could deduce some interesting, albeit preliminary structu
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CORT induced hippocampal damage has been implicated in depre
2023-09-22
CORT-induced hippocampal damage has been implicated in depression, aging and long-term glucocorticoid therapy. Therefore, finding a drug that can protect hippocampal neurons from the adverse effects of CORT could have significant clinical benefits. In this regard, we tested the potential protective
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Gene regulation of MMPs is influenced by the transcription f
2023-09-22
Gene regulation of MMPs is influenced by the transcription factor activating factor-1 (AP-1). AP-1 complexes are heterodimers of proteins of the two proto-oncogene families (jun and fos) and have cholecystokinin receptor in the promoter region of MMPs, as well as in genes mediating inflammatory res
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The AT hook motif is
2023-09-22
The AT-hook motif is highly conserved in evolution from bacteria to humans and is found in one or more copies in a large number of other, non-HMGA, proteins, many of which are transcription factors or are involved in chromatin remodeling [8]. For example, AT-hook peptide motifs are essential compone
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br Conflict of interest br
2023-09-22
Conflict of interest Acknowledgement We wish to thank the Program of National Key R&D Program of China (2017YFD0200500) and the Fundamental Research Funds for the Central Universities (KYTZ201604) for partially funding this work. Introduction Chitosan ((1→4)-2-amino-2-deoxy-β-d-glucose) is
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br Materials and methods br Results and discussion br Conclu
2023-09-22
Materials and methods Results and discussion Conclusions Acknowledgements Introduction Infections in children aged 0–21 years who reside in long-term care (LTC) facilities are common due to underlying complex medical conditions, use of invasive devices such as urinary catheters and ve
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Perforation of the surface membrane however is not the
2023-09-22
Perforation of the surface membrane, however, is not the only mechanism of calcium dysregulation by Aβ at the presynaptic terminals. When in excess, both monomers and oligomers modulate biophysical properties of voltage-activated calcium CCG 203971 synthesis as well as calcium release from the endo
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br Conclusion br Acknowledgement This work
2023-09-21
Conclusion Acknowledgement This work was supported by JSPS KAKENHI (Grant Number 15K18770). Introduction Neural crest HBX 41108 are multipotent progenitors in the vertebrate embryo that give rise to a vast array of different cell types including pigment cells, craniofacial skeleton and me
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br Materials and methods br Results br Discussion br
2023-09-21
Materials and methods Results Discussion Conclusions These studies provide important mechanistic insights to explain the long-established physiological observation that obese adipose tissue has higher rates of basal lipolysis. Increased lipolysis contributes to increased hepatic TOK-001
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br Acknowledgements MC and PD were funded by the Michael
2023-09-21
Acknowledgements MC and PD were funded by the Michael J Fox Foundation (Grant ID 9969). We would like to thank Pierluigi Saba, Francesco Traccis and Barbara Tuveri for their technical assistance. Introduction In the prostate, androgens play a crucial role in normal, BPH and cancerous growth b
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For the NSCLC patients with EGFR activating mutations EGFR
2023-09-21
For the NSCLC patients with EGFR-activating mutations, EGFR-TKIs (gefitinib and erlotinib) are effective clinical therapies [21], [22]. However, approximately 10% of patients harboring EGFR-sensitizing mutations exhibit intrinsic resistance, and up to 40% do not attain a major response to treatment
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Jesus et al discovered a new series of
2023-09-21
Jesus et al. discovered a new series of azaindole as Aurora inhibitors through various modification of GSK1070916 (47). They synthesized series from modification of the GSK1070916 and evaluated for in-vitro Aurora-B/INCENP and Aurora-A/TPX2 inhibition assays. Modified ionophores 48 and 49 showed IC
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