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br Contributions br Acknowledgements This research was
2022-03-09
Contributions Acknowledgements This research was supported by Natural Sciences and Engineering Research Council (NSERC) Discovery grant No. 341538 and Ontario Graduate Scholarships to HM and VS. Introduction Sexual size dimorphism describes size difference between male and female individua
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Introduction Osteoarthritis OA is a prevalent disease charac
2022-03-09
Introduction Osteoarthritis (OA) is a prevalent disease characterized by chronic joint degeneration, including articular cartilage loss, synovitis and osteophyte formation [1], [2], [3], [4], [5]. The cause of OA is metabolic imbalance and mechanical stress, which is coupled with inflammation, lead
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Gap junction channels exhibit different types of gating prop
2022-03-09
Gap junction channels exhibit different types of gating properties. One alternative mechanism that should be mentioned is loop gating in which the extracellular loop of connexin assumes a configuration to form a narrow pathway for closure of unopposed hemichannels [53] and docked junction channels [
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SCPNs and CPNs exhibit similar strength of electrical coupli
2022-03-09
SCPNs and CPNs exhibit similar strength of electrical coupling (Maruoka et al., 2017) and had similar membrane properties (Experimental Procedures), and showed no significant difference in amplification and synchronization (Figs. 2E and 3C). However, a subset of CPNs exhibit very strong electrical c
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ganciclovir australia Iodination of commercially available w
2022-03-09
Iodination of commercially available with excess ICl in AcOH gave a quantitative yield of , which was cyclized with benzyl thioamides to give the 2-benzyl-9,10-dihydro-4-1-thia-3,4-diaza-benzo[]azulenes . Coupling of the iodides with heterocycles including imidazoles, triazoles, or zinc cyanide usin
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Growing evidence supporting the anti inflammatory and tissue
2022-03-09
Growing evidence supporting the anti-inflammatory and tissue-protective effects of FPR antagonists led to the screening of commercial libraries for novel small-molecule FPR antagonists. As result of these screening efforts and/or structure–activity relationship (SAR)-directed design and synthesis, a
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K-252c br Significance Metabolites present in the extracellu
2022-03-09
Significance Metabolites present in the extracellular environment can potently modulate cellular phenotypes and potentially serve as therapeutics for various diseases. Ferroptosis is a non-apoptotic cell death process characterized by the generation of toxic lipid reactive oxygen species (ROS). I
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MMV s distinct mode of inhibition addresses key impediments
2022-03-09
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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We have expanded these studies by doing EEG recording in
2022-03-09
We have expanded these studies by doing EEG recording in the ET-1 model. Using this technique, we demonstrated that activation of either the ETA PF-431396 or the ETB receptor induces electrical seizures. ET-1 induced electrical seizures occurred in the presence of either the ETA receptor antagonist
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br Introduction Ovarian cancer patients have the
2022-03-09
Introduction Ovarian cancer patients have the highest mortality rate amongst patients with gynecologic cancers. The 10-year survival rate of ovarian cancer patients is mimosine with BRCA1/2 mutation [2]. Several studies have indicated the role of dysregulation of histone methylation in carcinog
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ICLs represent of all generated DNA adducts for cisplatin
2022-03-08
ICLs represent ICL Inducers in Cancer Therapy Nitrogen mustards with aromatic substituents (chlorambucil, melphalan) or a bioactivatable phosphoramide group (cyclophosphamide) were one of the first identified DNA crosslinkers. These agents are still used in combined schemes for the therapy of chr
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br Conclusion and prospect Small GTPases are very important
2022-03-08
5. Conclusion and prospect Small GTPases are very important regulatory proteins of eukaryotes. They play crucial regulatory function in various movement processes of organism [75], [76], [77]. Different nanoparticles used to investigate the interaction with small GTPases inside Pimozide have bee
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The Bcl and Bcl xL genes contain the CRE
2022-03-08
The Bcl-2 and Bcl-xL genes contain the CRE binding site in their promoter regions for CREB and CBP to bind to, so CREB phosphorylation was shown to up-regulate these anti-apoptotic genes, Bcl-2 and Bcl-xL [[29], [30], [31]]. Bcl-2 and Bcl-xL prevent the activation of caspases and the release of mito
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In order to investigate whether this
2022-03-08
In order to investigate whether this off-target activity was related to a particular structural feature of this NG,NG-dimethyl-L-Arginine hydrochloride or was characteristic of the series, compounds , and were selected as being matched pairs with compound but with structural variation in terms o
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The two competitive bivalent GlxI inhibitors polyBHG nM
2022-03-08
The two competitive bivalent GlxI inhibitors polyBHG2-62 (=1nM) and polyBHG2-54 (=0.3nM) () were designed based on the transition-state analog -(-bromophenyl--hydroxycarbamoyl) glutathione (BHG) by an examination of the X-ray crystal structure of human GlxI in complex with one CHG at each active sit
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