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Introduction Lipoxygenases LOXs are key enzymes that
2024-09-24
Introduction Lipoxygenases (LOXs) are key enzymes that catalyze the polyunsaturated fatty acids (PUFAs) such as arachidic L-Carnitine inner salt sale (AA), linoleic acid (LA) and others unsaturated fatty acids (Brash, 1999). LOXs are expressed in immune, neural, epithelial, tumor cells and other c
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br Results br Discussion Tapinarof GSK is
2024-09-23
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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Our initial approach to identify hits was two
2024-09-23
Our initial approach to identify hits was two-pronged and included a high-throughput screening (HTS) campaign of the OSI MK2 inhibitor library as well as a virtual screening (VS) campaign, utilizing a publically available crystal structure of ACK1 (PDB code: ). A tolerance for protein flexibility wa
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We have expressed the ECDs
2024-09-23
We have expressed the ECDs of the human α1, β1, γ and ɛ AChR subunits in the past using the methylotropic yeast Pichia pastoris as soluble glycosylated proteins [15], [16]. Further work with the γ subunit ECD revealed a marked improvement of the solubility and yield following the mutation of hydroph
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Additionally regulation of GPCR heteromerization by specific
2024-09-23
Additionally, regulation of GPCR heteromerization by specific ligands may depend not only on the affinity of ligands for receptors, but also on presence of different interacting proteins co-localizing with the receptors in the specific cell, which may induce some conformational changes and contribu
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br Funding This work was supported
2024-09-23
Funding This work was supported by Arena Pharmaceuticals, Inc, San Diego, CA, USA. Introduction 5-hydroxytryptamine 1B (5-HT1B) receptors are widely distributed in the central nervous system (CNS); they have various modulatory functions in drug reinforcement, appetitive behaviors, stress, moo
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Illustrated in is the protocol we
2024-09-23
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 GW 6471 derivatives and 501 3-furoic acid derivatives by performing substructural searches of the ZINC database. We limited the
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3146 To circumvent these issues multiple approaches have bee
2024-09-23
To circumvent these issues, multiple approaches have been developed that target small fractions of the genome, thus reducing the sequencing burden (Dostie et al., 2006; Fullwood et al., 2009; Mumbach et al., 2016). Application of one such approach, chromosome conformation capture carbon copy (5C), w
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Additional support for a role of HMGN in
2024-09-23
Additional support for a role of HMGN1 in enhancing DNA repair comes from studies of transcription-coupled repair (TCR) in human cells. Lesions in the template strand of DNA induced by UV light stall the movement of RNA polymerase II (RNAPII) and interrupt transcription. Removal of these transcripti
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br Introduction Increased renin angiotensin system RAS activ
2024-09-21
Introduction Increased renin-angiotensin system (RAS) activity and inflammation in cardiovascular-related regions of the central nervous system contribute to the overactivity of neurohumoral systems that promote volume retention, cardiac remodeling and serious cardiac arrhythmias in systolic hear
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Under some pathological conditions AT R internalization is
2024-09-21
Under some pathological conditions, AT1R internalization is decreased when agonist exposure is prolonged. This weakens or removes the AT1R desensitization effect and leads to AT1R and downstream signal overactivation. AT1R overactivation can result in continued biological effects such as sustained
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br Conclusions br Declarations br Introduction The classical
2024-09-21
Conclusions Declarations Introduction The classical term of endocrine disruption includes any agent that interferes with the action of hormones within the human body; these agents are therefore named endocrine disruptors. Among these agents, that are mainly environmental chemicals (pollutan
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br Discussion In a series of
2024-09-21
Discussion In a series of linear mixed effects models of longitudinal neuroanatomical change, we have identified genetic risk variants associated with an increase in reductase enzyme shape asymmetry in AD. The closest genes associated with significant SNPs include BIN1 (rs6733839), CD2AP (rs10948
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br Materials and method br Result and discussion
2024-09-21
Materials and method Result and discussion Conclusion Acknowledgments This work is partly supported by the University Research Committee (URC) of the Senate of The Federal University of Technology, Akure. The authors thanked IFS for the funds (F/4449 1F and F/4449-2F) used to purchase th
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Ibandronate sodium In this study high concentrations mM of t
2024-09-21
In this study, high concentrations (0.5–4 mM) of thuringiensin were required to stimulate the basal adenylate cyclase activity Fig. 2, Fig. 3, Fig. 4, but low concentrations of thuringiensin (1–100 μM) were sufficient to inhibit the forskolin-stimulated adenylate cyclase activity in rat cerebral cor
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