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The structure of LO is divided
2024-03-12
The structure of 5-LO is divided in two domains, the catalytic C-terminal domain and the N-terminal regulatory C2-like domain (C2ld) [59,60]. The C2ld spans the Cy5.5 NHS ester 1-114 and is responsible for translocation and binding of calcium and membranes [61–63]. The catalytic domain is primarily
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Skeletal pain associated with bone fracture is another
2024-03-12
Skeletal pain associated with bone fracture is another area of critical need for a novel pain medication. NSAIDs and opiates are the two major therapies currently used to manage bone fracture pain. However, both of these therapies lead to significant unwanted side effects. Using the osteotomy model
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As with most G protein coupled receptors GPCRs sustained
2024-03-12
As with most G protein-coupled receptors (GPCRs), sustained activation of APJ can cause desensitization and this has been reported to occur for APJ-mediated effects on cytoplasmic Ca2+ concentration, as well as for effects on activity of adenylyl cyclase, ERK and Akt (Ishida et al., 2004, Masri et a
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Since artemisinin shows low solubility and poor
2024-03-12
Since artemisinin shows low solubility and poor oral bioavailability [8], [9], derivatizations of artemisinin were carried out and yielded different semisynthetic antimalarial drugs such as artemether and sodium artesunate. Artemether (decahydro-10-methoxy-3,6,9-trimethyl-3,12-epoxy-12H-pyrano [4.3-
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Various antiangiogenic drugs have been analyzed over the
2024-03-12
Various antiangiogenic drugs have been analyzed over the last few years; noteworthy, bevacizumab, a monoclonal antibody against VEGF-A, alone or in combination with cytotoxic agents showed interesting results in terms of radiographic response rates and progression-free survival in initial phase 2 st
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In our previous work diffuse deposition patterns of
2024-03-12
In our previous work, diffuse deposition patterns of neocortical Aβ and a hierarchical upward spreading pattern of tau were determined with in vivo 18F-florbetaben and 18F-flortaucipir positron emission tomography (PET) studies, based on the regional frequency of involvement by tau and Aβ (Cho et al
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Circular dichroism CD provides useful information about prot
2024-03-12
Circular dichroism (CD) provides useful information about protein structure, the extent and rate of structural changes and ligand binding. CD is a form of light TPCA-1 sale spectroscopy that measures differences in the absorbance of right- and left-circularly polarized light (rather than the commonl
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The RAS may have different
2024-03-12
The RAS may have different functions depending on whether we consider the circulatory component or the different local tissue systems (including brain) well described previously [29]. The cardiovascular control and hydroelectrolytic balance (among other functions), are largely the result of the infl
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Some of the earliest LOX inhibitors were redox inhibitors in
2024-03-12
Some of the earliest 12-LOX inhibitors were redox inhibitors, including nordihydroguaiaretic daunorubicin (NDGA), BW 755C, and baicalein 48, 49, 50. Redox inhibitors block the oxidation of the nonheme iron at the cataylytic site, preventing its conversion from the inactive (Fe2+) to the active (Fe3
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br Author contributions br Funding This work
2024-03-12
Author contributions Funding This work was supported by the Czech Science Foundation, project no. 14-16220S. Additional support was provided by NIH R01CA117907 grant awarded to J.M.E. Conflict of interest Introduction The dioxin-like family includes polyhalogenated aromatic hydrocarbons
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br Endocytosis of AdipoR Surface
2024-03-11
Endocytosis of AdipoR1 Surface receptor activity may be shut down by endocytic uptake and subsequent lysosomal degradation of the proteins [20]. Clathrin-dependent endocytosis (CDE) has been extensively studied and internalization from the plasma membrane is mediated through clathrin-coated pits
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br Experimental procedure br Introduction Migraine is
2024-03-11
Experimental procedure Introduction Migraine is a debilitating neurovascular disorder characterized by recurring unilateral pulsating headaches of moderate to severe intensity, associated with nausea, photophobia and/or phonophobia, lasting from 4 to 72 h (Headache Classification Committee of
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Adenosine is a ubiquitous homeostatic purine nucleoside that
2024-03-11
Adenosine is a ubiquitous homeostatic purine nucleoside that accumulates extracellularly in response to metabolic stresses such as hypoxia and inflammation. Activation of either G protein-coupled adenosine receptors (ARs; A1R, A2AR, A2BR, and A3R) by extracellular adenosine can modulate cell signali
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The role of DHT in early teleost
2024-03-11
The role of DHT in early teleost embryogenesis is not entirely clear or established, however additional studies that treat fish embryos to DHT or to specific srd5a inhibitors at critical stages of development (i.e. prior to sex differentiation) will shed light on the early functions of this androgen
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To identify the kinase s
2024-03-11
To identify the kinase(s) mediating H3.3S31 phosphorylation, we devised a 96-well-plate-compatible immunostaining assay, with Metformin specific for H3.3S31ph, and utilized it to screen both a Qiagen siRNA library covering 720 human kinases and a kinase inhibitor library (Selleck) containing 194 com
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