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Recently considerable effort has been invested
2022-06-09
Recently, considerable effort has been invested in developing FDPS inhibitors based on alternative scaffolds (including nonbisphosphonates) that allow other tissue types and parasite-derived forms of FDPS , to be targeted. There are several limits in analyzing inhibitors of FDPS activity: the most
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Next we were interested in replacing the
2022-06-09
Next, we were interested in replacing the ketobenzimidazole fragment of our inhibitors with a noncarbonyl bearing heterocycle. We reasoned that if we could replace the carbonyl while maintaining comparable FAAH inhibition, it would provide evidence for a noncovalent mechanism of action. Thus, we eva
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Mitochondrial binding by HK prevents mortality by inhibiting
2022-06-08
Mitochondrial binding by HK prevents mortality by inhibiting pro-apoptotic factor (Bcl-2 family)-mediated opening of the mitochondrial permeability transition pore (mPTP) (Arora and Pedersen, 1988, Calmettes et al., 2016, Kodde et al., 2007, Pedersen et al., 2002, Rosano, 2011, Schindler and Foley,
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As indicated by the wide variety of
2022-06-08
As indicated by the wide variety of pharmaceuticals for IOP management (Table 1), each case of glaucoma is unique and requires a unique treatment regimen to effectively lower IOP. This often results in patients utilizing several medications at once and/or combining medications with surgical interven
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GR activity prevents GSSG overaccumulation by reducing this
2022-06-08
GR activity prevents GSSG overaccumulation by reducing this molecule to GSH (Kranner et al., 2006). High GR activity seems to be essential for undisturbed seed germination as GR and other enzymatic antioxidants maintain sunflower (Helianthus annuus L.) seeds vigour (Bailly et al., 2002). Germinatio
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br FXR Agonists Azepinol b
2022-06-08
FXR Agonists Azepinol[4,5-b]indole 1 (hEC50=600nM, efficacy (eff)=100%) was identified as a FXR agonist lead from a high-throughput screening effort. Structure–activity relationship (SAR) studies around the azepine ring demonstrated that dialkyl substitution at C-1 led to a 30-fold improvement in
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Naringin has been shown to have significant anti inflammatio
2022-06-08
Naringin has been shown to have significant anti-inflammation, anti-oxidative stress, glucolipid metabolic regulation, and myocardial protection effects (Gopinath et al., 2011, Gopinath and Sudhandiran, 2012), suggesting that it may mitigate ADC by inhibiting P2X7 receptors. In the present study, na
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Dendritic damage and loss of synaptic connections correlate
2022-06-08
Dendritic damage and loss of synaptic connections correlate with cognitive decline in HAND patients. Synapse loss induced by HIV proteins occurs early and via a different signaling pathway from that leading to neuronal death (Kim et al., 2008), suggesting that synapse loss might be a mechanism to re
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Hepcidin expression was not affected
2022-06-08
Hepcidin expression was not affected under GlyT1 inhibition. Hepcidin downregulation is well documented in conditions of ineffective erythropoiesis and dyserythropoietic anemias, including sideroblastic anemia 33, 34. Systemic iron acquisition under these types of anemia is obviously independent fro
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The amyloid precursor protein APP is a membrane
2022-06-08
The amyloid precursor protein (APP) is a membrane protein thought to be involved in plasticity, synapse formation and repair, and export of metal ions [68]. The APP present in the brain can be cleaved by three different secretases [73], [74]. Cleavage of APP first by alpha secretase and then gamma-s
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br Introduction Herpes viruses are members of Herpesviridae
2022-06-08
Introduction Herpes viruses are members of Herpesviridae family. This family consists of DNA viruses and it is a very large family. The viruses related to this family cause many diseases in animals and humans [1]. Herpes simplex viruses cause mucocutaneous lesions in the affected humans. These l
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The current study also inferred that MT content in
2022-06-08
The current study also inferred that MT content in Crassostrea gigas might be associated with the Cd level, and can be affected by MT turnover. The Nicotinamide of MT in cytosol is beneficial for aquatic organisms to adapt the seawater contaminated by heavy metals, and MT is a biomarker for marine
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Compared to previously reported atypical N glycosites
2022-06-08
Compared to previously reported atypical N-glycosites that were identified based on the deamidation of asparagine residues after PNGase F treatment [106], [107], these two studies further validated the identified atypical motif glycosites by directly identifying their intact glycopeptides. Since the
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This resembles a vicious cycle since
2022-06-08
This resembles a vicious cycle since BBB disruption and inflammation are thought to be caused by epilepsy, but other contributing factors are also known to be their cause, such as peripheral infection, autoimmunity, AR-42 inhibitor synthesis trauma and stroke that also underlie epilepsy [18]. Addit
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AG-014699 Because sleep and metabolism are intimately linked
2022-06-08
Because sleep and metabolism are intimately linked, the authors next move to study whether Eaat2 also controls metabolic rate. First, we must ask how sleep and metabolism are connected at a functional level. The AG-014699 allocation hypothesis of sleep posits that organisms temporally partition spe
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