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NKY 80 Continuing studies of endocannabinoid ligands at GPR
2022-08-24
Continuing studies of endocannabinoid ligands at GPR55 reveal that virodhamine (O-arachidonylethanolamine) and AEA can act as a partial agonists at GPR55; at high micromolar concentrations can inhibit β-arrestin recruitment (Sharir et al., 2012). It is likely that there are allosteric as well as ort
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br Conflict of interest statement br Acknowledgments The aut
2022-08-24
Conflict of interest statement Acknowledgments The authors would like to thank Dr. Linda Console-Bram for her editing of this review, Valentina Lucchesi for help with the figures, and acknowledge funding from NIH/NIDA (DA023204). Introduction G protein-coupled receptor 55 (GPR55) has emerg
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Excessive adiposity is also a key
2022-08-24
Excessive adiposity is also a key pathogenic factor in the development of CVD. Through reductions in bodyweight, GPR120 agonism is therefore also implicated as a potential therapy for obesity and heart and vessel disease. In addition to weight loss, when compared with their wild-type littermates, GP
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br Evolution of multiple GnRH forms
2022-08-24
Evolution of multiple GnRH forms and GnRH receptors across vertebrates GnRH is an evolutionary ancient peptide that first appears prior to the protostome-deuterostome split, and is a member of the GnRH-adipokinetic hormone-corazonin superfamily of peptides (Roch et al., 2011, Roch et al., 2014).
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br Material and methods br Results br
2022-08-24
Material and methods Results Discussion Organisms have developed a variety of anti-glycation defense mechanisms. In I-BET 151 hydrochloride to the aldose-reductase-pathway or 2-oxoaldehyde dehydrogenase-pathway, the glyoxalase system is the only mechanism, which is not restricted to liver
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br Chronic obstructive pulmonary disease COPD is
2022-08-23
Chronic obstructive pulmonary disease (COPD) is characterized by progressive obstruction of airflow, not fully reversible, which is accompanied by a chronic inflammatory response, induced by deleterious particles or gases, in airways and lung parenchyma. The most important risk factor for COPD is
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The ability of GPX and other selenoproteins to
2022-08-23
The ability of GPX4 and other selenoproteins to be selectively induced by ferroptotic stimuli suggests that the stress-induced increase in the transcription of a number of putative, “antioxidant” selenoproteins is an adaptive homeostatic, but insufficient response to prevent cell death in the face o
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One of the main mechanisms enabling recycling of intracellul
2022-08-23
One of the main mechanisms enabling recycling of intracellular redox-active iron is lysosomal degradation of ferritin in the process of autophagy, often referred to as ‘ferritinophagy’ [128]. Autophagy was suggested to contribute to ferroptotic cell death by promoting the degradation of iron storage
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The release of FBPase and aldolase from subcellular
2022-08-23
The release of FBPase and aldolase from subcellular structures of muscle was dependent on the presence of the crowding agent imitating the physiological conditions – PEG 8000 (Table 1). The amount of both enzymes associated with structures of muscle CPI-455 was about 6–7 times higher in the presenc
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Through experimental models and clinical experiments those f
2022-08-23
Through experimental models and clinical experiments, those four drugs above can shown efficacy-enhancing and toxicity-reducing effects after compatibility. Our preclinical studies showed that XFC has a definite effect on relieving joint symptoms in RA patients. XFC can improve joint pain, swelling
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By measuring the accumulation of
2022-08-23
By measuring the accumulation of unprenylated Rap1a as a surrogate marker for the inhibition of FPPS [8], [9], [10], [11], we found that upregulation of FPPS expression in Hela cells reduced the accumulation of unprenylated Rap1a in response to 24h' treatment with 0–50μM ZOL. As expected, cells cult
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In general the FDP gene is
2022-08-23
In general the FDP gene is involved in isoprenoid biosynthesis for normal growth and development of plant species while it is specifically involved in rubber biosynthesis (cis-1,4-polyisoprene units) in Hevea plant. When the HbFDP gene was over-expressed under the control of constitutive promoter in
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MMV s distinct mode of inhibition addresses key impediments
2022-08-23
MMV019313's distinct mode of inhibition addresses key impediments in the development of PfFPPS/GGPPS inhibitors as antimalarial drugs. First, it is the first non-bisphosphonate inhibitor of Plasmodium FPPS/GGPPS with drug-like physicochemical properties satisfying the “Rule of 5” (Van Voorhis et al.
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Importantly both genetic deletion and
2022-08-23
Importantly, both genetic deletion and pharmacological inhibition of FAAH also reduced NTG-induced neuronal hyperactivity in the trigeminal nucleus, which receives sensory input from craniofacial deep tissues. NTG is known to evoke the robust neuronal activation, as evidenced by the induction of the
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The organ culture method has previously
2022-08-22
The organ culture method has previously shown to be a suitable model for investigations of receptor upregulation on vascular smooth muscle cells (Adner et al., 1996). In our study, the organ culture method was applied in order to examine whether LPS from P.g. was capable of altering the gene express
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