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Our own search towards aryl imidazole derived GSMs
2022-05-25

Our own search towards aryl-imidazole derived GSMs led to the discovery of the benzimidazole derivative (). It is one of the most potent GSMs to date, suffering however from sub-optimal drug-like properties. More recently, we have described the design and synthesis of bicyclic triazolo-derivatives,
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A common feature of ferroptosis is
2022-05-24

A common feature of ferroptosis is the iron-dependent accumulation of lipid-ROS and the subsequent depletion of polyunsaturated fatty apigenin phospholipids (PUFA-PLs) [118]. The PUFA chains of membrane lipids are more susceptible to both enzymatic and non-enzymatic oxidation, which results in PUFA
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Previously we have isolated liver FBPase from Pelophylax
2022-05-24

Previously we have isolated liver FBPase from Pelophylax esculentus (former Rana esculenta, Frost et al., 2006) and characterized its kinetic properties (Dziewulska-Szwajkowska and Dzugaj, 1999) on the contrary the muscle FBPase has never been fully characterized. The primary aim of the present pape
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br Introduction More than structurally different isoprenoids
2022-05-24

Introduction More than 30,000 structurally different isoprenoids, such as steroids, carotenoids, prenyl side-chain of quinones, prenyl proteins, and natural rubber, exist in nature. In a biosynthetic pathway, linear prenyl diphosphates are common structures as a precursor of isoprenoids, as shown
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Neither E nor Z FPP synthase catalyzed the reaction between
2022-05-24

Neither E- nor Z-FPP synthase catalyzed the reaction between 8-THPOGPP and IPP. However, a mutant E-FPP synthase (Y81S) produced 12-THPOFPP from the substrates 8-THPOGPP and IPP, and wild-type E-FPP synthase catalyzed the reaction betweeen 8-AcOGPP and IPP producing 12-AcOFPP. Mutant E-FPP synthase
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br Retrieval requires histamine H receptors in dorsal
2022-05-24

Retrieval requires histamine H1 receptors in dorsal hippocampus Retrieval is a dynamic process that requires neurotransmitter regulation (Barros et al., 2000, Barros et al., 2001). Recently, histamine, and histaminergic transmission has entered the list of putative neurotransmitter modulators of
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Classically HIF levels and consequently
2022-05-24

Classically HIF-α levels and consequently HIF transcriptional activity have been associated with hypoxic conditions. However, some years ago, regulation by hormones of HIF transcriptional activity under normoxic conditions was demonstrated. Different stimuli such as heregulin, IGF1 and insulin, amon
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In this precancerous condition though cancer develops from t
2022-05-24

In this precancerous condition, though cancer develops from the epithelium, the subepithelial connective tissue also play crucial biological role in pathogenesis and progression to malignancy. In this context it may be noted that some recent reports addressed the problem of the mechanical interactio
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Following our initial observation of an unexpected
2022-05-24

Following our initial observation of an unexpected increase in the maximal rates of cGMP formation by NO-stimulated sGC in the presence of cytosolic PCA preparations [15], we attempted to purify, identify and characterize the responsible protein(s). The purification protocol described in the present
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As more genes were identified to cause IRDs a
2022-05-24

As more genes were identified to cause IRDs, a relatively large proportion were found to either cause multiple phenotypes or multiple inheritance patterns. Out of the 112 autosomal genes that are listed in RETNET (as of July 22, 2016) that are known to cause non-syndromic IRDs (RP, LCA, and CRD), 16
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As comparators compounds and were made using the pyrazolopyr
2022-05-24

As comparators, compounds and were made using the pyrazolopyridine core with the CF triazole attached. The 2-fluorophenyl group was replaced with the methylpyrimidine in compound . The potency of these compounds were very good and compound looks attractive from a physicochemical perspective as it
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Ning et al showed that LPC appeared to increase insulin
2022-05-24

Ning et al. showed that LPC 18:1 appeared to increase insulin release through both GPR119-dependent and -independent mechanisms (Ning et al., 2008). In our study, we have shown that not only GPR119 but also GPR40 and GPR55 participate in LPC-stimulated insulin secretion (Fig. 4, Fig. 5) and target p
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Several studies have found that
2022-05-24

Several studies have found that GPR55 possesses a distinct pharmacology from that of CB1 and CB2, and that only certain cannabinoids act at this receptor. In transfected AP1903 expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, SR141716A (Rimon
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In conclusion the present study demonstrated
2022-05-24

In conclusion, the present study demonstrated that peripheral nerve exposure to HIV gp120 increased the expression levels of the P2Y12 receptor in DRG SGCs and enhanced mechanical and thermal hyperalgesia in rat models. Up-regulation of the P2Y12 receptor in DRG SGCs further promoted the release of
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Thermal analysis of the NQ peptide
2022-05-24

Thermal analysis of the NQ21 peptide was performed with the Solar CM2203 spectrofluorometer. We prepared three 1 μg/mL peptide solutions with different CBR-5884 levels (5.0, 7.4, 8.5) in 0.01 M phosphate buffers. Each solution was slowly heated up from 28 °C to 54 °C with a step of 1 °C. Spectra wer
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