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br GPR GPR has been described as a
2022-02-09

GPR55 GPR55 has been described as a type 3 cannabinoid receptor due to its ability to detect endocannabinoids and may play a role in the endocannabinoid lipid sensing system [28]. GPR55 is activated by both cannabinoid endogenous agoinsts (endocannabinoids) and non-cannabinoids fatty acids namely
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Typically upon chronic agonist exposure GPCRs
2022-02-09

Typically, upon chronic agonist exposure GPCRs undergo desensitization and internalization resulting in a loss of receptor responsiveness over time (Drake et al., 2006, Kelly et al., 2008). However, not all GPCR systems conform to this model of acute agonist-mediated regulation. Some receptors have
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FOLE was recently approved for use in
2022-02-09

FOLE was recently approved for use in PN-dependent patients in the United States. However, potential adverse effects of FOLE, including bleeding risk, and effects on the immune system [8], [39], render its use in certain patient populations controversial. Identification of key downstream modulators
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Autophagy as an important cellular process has
2022-02-09

Autophagy as an important cellular process has drawn attentions to its role in cardiovascular systems [16]. Autophagy is a self-digestion and degradation process that recycles the contents of the cytosol, including macromolecules and cellular organelles, resulting in self-repair and conservation for
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In addition this study also showed no obvious increase in
2022-02-08

In addition, this study also showed no obvious increase in apoptosis but obvious increase in necrosis after WZB117 treatment. The possible reason is that apoptosis is an ATP-utilizing process which is an active and programmed form of cell death. In contrast, necrosis is an uncontrolled or pathologic
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C steroids and their glycosylation
2022-02-08

C21 steroids and their glycosylation products distribute widely in Asclepiadaceae plants. Their anticancer activities have been shown in different human cell lines and in vivo animal experiments [[27], [28], [29], [30], [31], [32]]. However, the mechanisms of their anticancer activities are still un
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Rufinamide No specific inhibitor of KCC has progressed to
2022-02-08

No specific inhibitor of KCC has progressed to clinical trials, however, although compounds like H74 were shown to specifically target KCC over the related Na+-K+-2Cl− cotransporter (NKCC) (Ellory et al., 1990). This molecule, or its related analogues, represent compounds of promise. Simple Mg suppl
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Receptor interactions and binding mode of in hGPR
2022-02-08

Receptor interactions and binding mode of in hGPR40 were determined by docking studies. The compound was docked in the rebuilt co-crystal structure of hGPR40 (PDB ID: ) using MOE for loop modeling and energy minimization and Glide for molecular docking. The docking site used for the docking simulati
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We then explored the possible mechanisms by which integrin
2022-02-08

We then explored the possible mechanisms by which integrin α5β1 was involved in the PHEV proliferation process. Normally, the virus activates integrin and induces its downstream protein activation to promote its own invasion and proliferation. Human papillomavirus type 16 (HPV16) binds to heparan su
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Liposomes that are less than
2022-02-08

Liposomes that are less than 200nm in diameter are necessary to optimize uptake of liposomes by Brassinolide (Oesterling et al., 2014). The liposomes constructed in these experiments were found to be sufficiently small in diameter for use in in vivo and in vitro experiments. Even smaller diameters
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br Introduction Ovarian cancer patients have the highest mor
2022-02-08

Introduction Ovarian cancer patients have the highest mortality rate amongst patients with gynecologic cancers. The 10-year survival rate of ovarian cancer patients is cancer DY131 mg with BRCA1/2 mutation [2]. Several studies have indicated the role of dysregulation of histone methylation in c
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Further investigation of the effects of this inhibitor
2022-02-08

Further investigation of the effects of this inhibitor on histone acetylation revealed no HAT inhibitory effects at the level of global histone acetylation after 20h of incubation with C646. After 6h of incubation with C646, however, a slight increase in histone H3 acetylation was observed at lysine
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Apoptosis is one of critical toxic mechanisms of benzene
2022-02-08

Apoptosis is one of critical toxic mechanisms of benzene metabolites. In this work, overexpression of HIF-1a could significantly reduce the increase in cell apoptosis caused by 40 μM BQ. At the meanwhile, anti-apoptotic protein Bcl-2 level was significantly elevated in HIF-1a overexpression cells th
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However despite medicinal chemistry efforts lead to consider
2022-02-08

However, despite medicinal chemistry efforts lead to considerable improvement in potency and selectivity of new HO-1 inhibitors, still have not identified inhibitors in the low nanomolar range. Therefore, due to the possible in vivo non-specific effects at high dosage, novel strategies should be dev
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In conclusion while class I HDAC
2022-02-08

In conclusion, while class I HDAC inhibitors, isoform-specific HDAC3 and HDAC6 inhibitors may represent novel therapeutic targets for prevention of clinical AF onset and progression, the specific HDAC3 and HDAC6 inhibitors may be more appropriate because of their limited off-targets effects. Besides
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