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Subsequently Palvimaki et al corroborated Ni and Miledi s
2025-01-26

Subsequently, Palvimaki et al. (1999) corroborated Ni and Miledi's study by demonstrating that treatment with fluoxetine leads to 43% occupancy of the 5-HT2C receptors. Moreover, the affinity of fluoxetine for 5HT2C receptors (Ki 65 nM) is close to its affinity for 5-HT transporters (Ki 33 nM) (Ni a
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Anti LT therapy by LO inhibition
2025-01-26

Anti-LT therapy by 5-LO inhibition has been hampered by occurring liver toxicities by Zileuton or the clinical phase II compound Atreleuton [36], [37] However both compounds possess a thiophene as well as an N-hydroxyurea moiety. These features could be linked with reactive thiophene intermediates
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ACET australia Having established the structural requirement
2025-01-26

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 vitr
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UNC 0631 br Materials and methods br Results
2025-01-26

Materials and methods Results Discussion Fluoride can readily penetrate cellular membranes and seriously damage the structure and physiological function of cells (Zhou et al., 2015). Several studies have shown that excessive fluoride can decrease the viability of cells and that the growth o
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Drug for Protein Degradation Finally intracrine androgen syn
2025-01-24

Finally, intracrine androgen synthesis/metabolism can be activated thus allowing Drug for Protein Degradation to bypass the low levels of androgens in the circulation by producing androgens themselves (Cai and Balk, 2011, Rahman et al., 2004). Moreover, changes in AR co-regulators like the overexpr
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This study demonstrates numerical alterations of
2025-01-24

This study demonstrates numerical alterations of creatinine levels potentially reflecting ongoing or even higher myocardial contraction of the LAA after successful LAAC. Creatinine is the direct breakdown product of creatine in muscle, the key metabolite for energy supply during muscular and myocard
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Overexpression of AR can lead to sorbitol accumulation leadi
2025-01-24

Overexpression of AR can lead to sorbitol accumulation, leading to diabetic complications (Ransohoff and Cardona, 2010). Therefore, AR is an important enzyme in the growth and development of organisms. With the aim of inhibiting the activity of AR in diabetic patients, screening for inhibitors and i
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br Acknowledgements Dr Paul J Gasser is supported by
2025-01-24

Acknowledgements Dr. Paul J. Gasser is supported by the National Institutes of Health (grant number R01DA032895), and the Charles E. Kubly Mental Health Research Center. Dr. Christopher A. Lowry is supported by the National Institutes of Health (grant number R21 MH116263), the Department of the N
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PTC209 HBr br Conclusion br Conflicts of interest br Introdu
2025-01-24

Conclusion Conflicts of interest Introduction Enzymes are widely applied as biocatalysts in fields such as synthetic chemistry [1], pharmaceuticals [2], environmental treatment [3], and food technology [4] because they can catalyze chemical transformations in a highly selective manner under
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br Introduction Myasthenia gravis MG is an
2025-01-24

Introduction Myasthenia gravis (MG) is an autoimmune disease in which antibodies against targets on the postsynaptic muscle membrane cause neuromuscular transmission failure. About 85% of patients with MG have autoantibodies against RS 127445 HCl receptor (AChR) [1]. In AChR negative MG patients
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Both subcutaneous s c and mucosal administration of
2025-01-24

Both subcutaneous (s.c.) and mucosal administration of short synthetic peptide derivatives of AChR prevent the onset of EAMG, but do not treat ongoing EAMG [80], [81], [82], [83], [84], [85]. The selection of peptides for treatment is mainly based on the identification of immunodominant T- and B-cel
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The first description of autophagy as a tumour
2025-01-23

The first description of autophagy as a tumour suppression process arises from the observation that the initial step regulatory gene, Atg6/BECN1, was monoallelically lost in 40% to 75% of human prostate, breast, and ovarian cancers [31]. However, while BECN1 heterozygous mutant mice develop, with lo
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In order to determine whether the faster Rh
2025-01-23

In order to determine whether the faster Rh2-induced apoptosis is specific of cholesterol depletion, we determined the cytotoxic effect of Rh2 in thiotepa sale depleted or not in sphingomyelin, another abundant plasma membrane lipid exhibiting enrichment in lipid rafts. We showed that, in contrast t
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br Conflict of interest br Acknowledgment The authors gratef
2025-01-23

Conflict of interest Acknowledgment The authors gratefully acknowledge the financial support from the National Natural Sciences Foundation of China (81070220 and 81170278), and the Aid Program for Science and Technology Innovative Research Team in Higher Educational Institutions of Human Provi
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The reduction of heterodimerization of KOR
2025-01-23

The reduction of heterodimerization of KOR and APJ by both doses of apelin found in the present study may result in inducing protective effects of apelin on the myocardium imposed to high pressure in renovascular hypertension conditions. The finding that apelin in both doses reduced heterodimerizati
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