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br Conflict of interest statement br Acknowledgement br Intr
2024-12-19
Conflict of interest statement Acknowledgement Introduction Lipoxygenases (LOs) are enzymes catalyzing the positional as well as stereo-specific introduction of molecular oxygen into 1,4-pentadiene structures found in unsaturated fatty acids such as arachidonic Telatinib or linoleic acid [
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br Experimental Procedures br Acknowledgments We
2024-12-18
Experimental Procedures Acknowledgments We thank the members of the Qing laboratory for helpful suggestions and Biotree Biotech Co., Ltd. (Shanghai, China) for metabolomics analysis and data interpretation. This study was supported by the National Key Research and Development Program of China
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br Results br Discussion Tapinarof GSK is a naturally
2024-12-18
Results Discussion Tapinarof (GSK2894512) is a naturally derived investigational topical medicine with demonstrated clinical efficacy for patients with AD and psoriasis (Bissonnette et al., 2010, Bissonnette et al., 2012a). The drug substance is a polyphenol produced by bacteria that is struct
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br Theoretical mechanism of ABCA activity in LE LY
2024-12-18
Theoretical mechanism of ABCA2 activity in LE/LY in modulation of cholesterol trafficking It is important to confirm that ABCA2 is a lipid transporter and identify the substrates that are mechanistic in its cholesterol sequestering activity. We hypothesize that ABCA2 modulates cholesterol sequest
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To further clarify the vascular
2024-12-18
To further clarify the vascular cell types expressing AR subtypes, double immunofluorescence staining for ARs and vascular endothelial LY500307 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 e
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br Transparency document br Introduction G protein coupled
2024-12-18
Transparency document Introduction G protein-coupled receptors (GPCRs) comprise a diverse family of seven transmembrane domain-containing receptors represented by over 800 genes in humans. GPCRs respond to a range of stimuli, including peptides, hormones, growth factors, lipids, odorants, and
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br Concluding remarks Following the disappointing outcomes o
2024-12-18
Concluding remarks Following the disappointing outcomes of Aβ immunotherapy trials for AD [62], the current prevailing concept is that disease-modifying therapy must be initiated from the presymptomatic stage of the disease because of the presumed incurability of chronic diseases once they become
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Phosphodiesterase inhibition increases the intracellular lev
2024-12-18
Phosphodiesterase inhibition increases the intracellular levels of cAMP to restore spontaneous contraction (Essayan, 2001, Qi and Kwan, 1996), acting downstream of adenylyl cyclase. Therefore, cardiac arrest induced by decreased intracellular cAMP levels could be reversed by phosphodiesterase inhibi
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br Experimental procedures Adk tg Adktm tg
2024-12-18
Experimental procedures Adk-tg (Adktm1−/−:tg(UbiAdk) mice were created by breeding a loxP-flanked Adk transgene under the control of a human ubiquitin promoter into ADK knockout mice (Fedele et al., 2005,). Fb-Adk-def (Adktm1−/−:tg(UbiAdk):Emx1-Cre-tg3) mice were generated by pairing Emx1-Cre-tg3
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The small fishers with little or no
2024-12-18
The small fishers with little or no quota who remained relied on quota leasing arrangements to continue their fishing operations. Such arrangements had relatively high transaction costs and by early 2000 it appeared that the demise of the small fisher was imminent [2]. The introduction in 2001 of t
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TMPyP4 tosylate ACE inhibition is often thought
2024-12-18
ACE inhibition is often thought to play a central role in the mechanisms of blood pressure reduction in vivo, and most ACE inhibitory (ACEi) peptides were characterized based on in vitro ACE inhibition. A relationship between in vitro ACE inhibition and antihypertensive activity, however, is not app
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The altered frequency of CD T cells in LO
2024-12-18
The altered frequency of CD4+ T cyclohexamide in 5-LO−/− mice led us to hypothesize that these leukocytes could be exerting a primary control of the inflammatory response. In fact, the lack of 5-LO resulted in the accumulation of CD4+CD25+ cells expressing Treg markers. It is plausible to speculate
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From our in vivo studies and previously reported findings we
2024-12-18
From our in vivo studies and previously reported findings [25], we have found that orteronel possesses excellent oral BA. Indeed, single oral dosing of orteronel at doses of 0.3–10.0mg/kg decreased serum DHEA levels in a dose-dependent manner. Of interest, DHEA levels did not return to levels compar
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Our previous studies found that some steroid mimetic structu
2024-12-18
Our previous studies found that some steroid mimetic structures such as stilbene, biphenyl, naphthalene and benzothiophene rings were suitable for lipophilic moieties of 17,20-lyase inhibitors, and several inhibitors obtained using a steroid A, C-ring mimetic approach have already been published. Du
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br Acknowledgements We would like to
2024-12-18
Acknowledgements We would like to thank Dr. Thomas Blanpied, Sai Sachin Divakaruni, Dr. Helmut Kessels, Feline Lindhout, Dieudonnée van de Willige, and all members of the MacGillavry lab for discussions and critical reading of the manuscript. This work was supported by NWO (ALW-VENI 863.13.020, A
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