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br Materials and methods br Results and discussion
2020-12-21
Materials and methods Results and discussion In the present work, we have applied two methodologies, CoMFA and CoMSIA to build 3D-QSAR models. There is no crystal structure available; therefore, an indirect method i.e., a ligand-based approach is the method of choice. The highly active molecul
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1400W dihydrochloride Although PGD was initially considered
2020-12-21
Although PGD was initially considered to elicit its biological actions through a classical PGD receptor (DP1), later findings suggested that several PGD-mediated actions of eosinophils arise via DP2,, which is also known as CRTH2 (chemoattractant receptor-homologous molecule expressed on Th2 cells).
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Ranitidine Introduction Eicosanoid lipid prostaglandin D PGD
2020-12-21
Introduction Eicosanoid lipid prostaglandin D2 (PGD2) is the major prostaglandin produced by activated mast Ranitidine (Lewis and Austen, 1981). The physiological function of PGD2 is mainly mediated by two G protein-coupled receptors (GPCRs), PGD2 receptor 1 and 2 (DP1 and DP2), which share modest
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Crystal structures of various CRM complexes have
2020-12-21
Crystal structures of various CRM1 complexes have provided insight into molecular details of the interactions between CRM1 and its interaction partners during the transport cycle. CRM1 cooperatively binds RanGTP and cargo in the nucleus (Paraskeva et al., 1999). In this ternary complex, RanGTP is lo
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jsh Alternatively procedural factors may have contributed to
2020-12-21
Alternatively, procedural factors may have contributed to the conflicting results. For instance, in order to have a more circumscribed area of drug diffusion, a volume of 0.05μl was injected in experiment 1b, which is four times lower than the one used in the mentioned plus-maze investigation. Besid
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Under conditions of energy scarcity or nutritional
2020-12-21
Under conditions of energy scarcity or nutritional restriction, AMPK, a critical energy sensor, is activated in response to the increased ratio of AMP to ATP. Various kinases may phosphorylate AMPK, leading to its activation. For example, AMPK phosphorylation by liver kinase B 1 (LKB1) at Thr172 res
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Next to organophosphates carbamates and metals cholinesteras
2020-12-21
Next to organophosphates, carbamates and metals, cholinesterase activity can also be affected by other pesticides, such as newer generation neonicotinoid insecticides (NN). NNs do not inhibit AChE activity via the organophosphate-sensitive binding site of the enzyme, but rather, by acting as a struc
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Perturbations in cell cycle are
2020-12-21
Perturbations in AH 7614 are known to induce apoptosis. Our results show that a fraction of the DT40YB-1b+/− cells, in addition to becoming tetraploids, undergo apoptotic cell death. Similar observations linking polyploidy and apoptosis have been made in the past [23], [30], [31], [32], [33], [34].
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Introduction Angiotensin II Ang II and
2020-12-21
Introduction Angiotensin II (Ang II) and Endothelin 1 (ET-1) are potent vasoconstrictive peptides recognized as key players in many cardiovascular diseases [1]. Cardiac hypertrophy, ischemic arrhythmia, and stroke have been associated to an overstimulation of the angiotensin II type 1 (AT1) recepto
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Angiomatoid fibrous histiocytoma originally described as ang
2020-12-21
Angiomatoid fibrous histiocytoma (originally described as angiomatoid malignant fibrous histiocytoma) is a soft tissue tumor of intermediate biologic potential. AFH typically arises within extremity deep dermis and subcutis in children and young adults,157, 158, 159 but can arise in older adults and
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MoAbs targeting the tumourigenic pathways such as IGF R may
2020-12-21
MoAbs targeting the tumourigenic pathways, such as IGF-1R may theoretically have a dual working mechanism. On the one hand they block pathways having an anti-tumour working mechanism, and on the other hand they may also stimulate an immunological response inducing a reaction of the patients own immu
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In particular EphB has been one of the
2020-12-18
In particular, EphB4 has been one of the most studied receptor of the Eph family: inhibition of EphB4 expression using interfering-RNA or antisense oligonucleotides inhibited proliferation, survival and invasion of PC3 prostate cancer Lomerizine HCl in vitro and in vivo. Inhibition of EphB4 signalli
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Another milestone in the field is the de novo discovery
2020-12-18
Another milestone in the field is the de novo discovery of EPAC2 and EPAC1 specific inhibitors through fluorescence-based HTS assays. Due to the excellent EPAC/PKA selectivity of cytidine , it has been widely applied as a useful chemical probe to discriminate EPAC related signaling pathways and biol
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Although MMP might be a downstream
2020-12-18
Although MMP-9 might be a downstream target of Src kinase signaling (Liu and Sharp, 2011), a direct connection has not been established. We showed for the first time that, in the collagenase-induced ICH model, Src kinase signaling regulates MMP-9 activity and mediates EP1R toxicity. Consistent with
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Nitrid oxide NO and its potential endogenous production as a
2020-12-18
Nitrid oxide (NO) and its potential endogenous production as an endothelium-derived factor was the first gaseous molecule accepted to be a signaling mediator in the organism [4,5]. NO plays a key role in physiological regulation of the beta lapachone and exerts physiological functions in the nervou
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