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br Conclusion br Acknowledgement This study was supported by
2024-01-15
Conclusion Acknowledgement This study was supported by NIH/NINDSR01 NS036812-16. Introduction Stroke is the leading cause of disability and the fifth leading cause of death in the United States (Writing Group et al., 2016). On average, every 4 min a human dies of stroke (Lackland et al., 2
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Aminoglutethimide first generation aromatase inhibitor
2024-01-15
Aminoglutethimide, first generation aromatase inhibitor, has been tried as an antiepileptic drug in combination with other standard drugs (Aguilar et al., 1961). Letrozole is a third generation reversible non-steroidal aromatase inhibitor, approved by US-FDA, for the treatment of postmenopausal wome
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There is little question that as we
2024-01-15
There is little question that as we become more proficient in the diagnosis of arginase 1 deficiency individuals with intermediary elevations in arginine on newborn screening and partial defects in enzymatic activity will be found. There are no reliable data to determine a safe level of arginine and
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Based on its kinetic parameters and quaternary
2024-01-15
Based on its kinetic parameters and quaternary structure, R. pycnus arginase is a typical ureotelic L-arginase [2]. The Km value of the enzyme was lower than other arginases from other organisms (Table 2), including S. cerevisiae (15.7mM), B. anthracis (10mM), B. caldovelox (3.4mM), human liver (2.3
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Dual acting RAAS blockade and neprilysin inhibition has
2024-01-15
Dual-acting RAAS blockade and neprilysin inhibition has been evaluated in several clinical HF trials. In PARADIGM-HF [6,7], LCZ696 was superior to enalapril in reducing mortality and HF hospitalizations in symptomatic patients with HF with reduced EF. Augmented benefits on maladaptive cardiac remode
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Based on structure activity relationship of several SARM tem
2024-01-15
Based on structure activity relationship of several SARM templates, Ligand Pharmaceuticals chose LGD2226 as their first clinical candidate (Miner et al., 2007). Although LGD2226 demonstrated myo- and osteo-anabolic activity and maintenance of sexual function in various preclinical models, the develo
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The AhR molecule is composed
2024-01-13
The AhR molecule is composed of multiple functional domains [38]. In the N-terminal end, the AhR contains bHLH domain which is involved in DNA binding, dimerization with ARNT and association with chaperone proteins. The PAS domain, which is situated next to the bHLH domain consists of two structural
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Since the cloning of ARs in the beginning of
2024-01-13
Since the cloning of ARs in the beginning of the 1990s, the efforts to characterize them have led to the accumulation of a substantial amount of experimental data. Decades of site-directed mutagenesis (SDM; Box 1) studies, in combination with pharmacological data and computational modeling, have pav
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br The role of AMPK beyond energy
2024-01-13
The role of AMPK beyond Iloperidone homeostasis: regulating metabolism AMPK plays a major role in glucose homeostasis by modulating glucose transport in peripheral tissues [20]. Skeletal muscle, one of the main peripheral tissues involved in glucose uptake and disposal, expresses glucose transpo
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Some alterations in the integrity of cell membranes caused b
2024-01-13
Some alterations in the integrity of cell membranes caused by toxic agents can be determined by measuring certain enzymes released by damaged cells [8]. The cholinesterases, for example, catalyze the hydrolysis of CFTRinh-172 synthesis (ACh) in choline and acetic acid. Theses enzymes are divided in
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br Funding br Introduction The interest in the effects of
2024-01-13
Funding Introduction The interest in the effects of endocrine disrupting chemicals (EDCs) in the aquatic environment continues to increase over the past decade, specifically those that act on steroidogenic pathways. EDCs that include synthetic androgenic and estrogenic compounds can severely a
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Acknowledgements The work was supported by
2024-01-13
Acknowledgements The work was supported by grants from Swedish Research Council (J.Z.H.) (A.R.M.). We thank Protein Science Facility (PSF), Department of Medical Biochemistry and Biophysics, Karolinska Institute, Stockholm, Sweden. We thank Prof. Ralf Morgenstern (Department for Environmental Medic
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2881 Regarding the HT B receptors they act as terminal recep
2024-01-13
Regarding the 5-HT1B receptors, they act as terminal receptors and are involved in the presynaptic regulation of the release of 5-HT. But at spinal level these receptors are principally situated post-synaptically (Sari, 2004). The ability of autoreceptors to regulate extracellular levels of 5-HT dur
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The extent to which GPCR oligomerization
2024-01-13
The extent to which GPCR oligomerization is a regulated process still remains unclear. Reported effects of ligands on both GPCR homo- and heteromers are highly variable and depend on GPCR subtypes and the specific ligand used. According to our data, chronic treatment of mice with both paroxetine or
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br Introduction Nausea and vomiting are among
2024-01-13
Introduction Nausea and vomiting are among the most distressing side effects associated with chemotherapy in cancer patients (Billio et al., 2010). Severe emesis can negatively affect a patient's nutritional state, ability to work and motivation, which can, in turn, interfere with the clinical co
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