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Signaling through Axl can lead
2023-02-25

Signaling through Axl can lead to activation of the PI3K/Akt and Ras/MAPK pathways which promote cellular phenotypes (e.g., transformation, migration) consistent with pro-survival and pro-metastatic effects., , Inhibition of Axl activity by a variety of approaches (including pharmacologic, dominant
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Altiratinib Lower LDL C mediated by variants in the
2023-02-25

Lower LDL-C mediated by variants in the ACL gene is causally associated with the risk of cardiovascular events. Because, genetic variants that mimic the effect of an ACL inhibitor have the same effect on the risk of cardiovascular events per unit change in LDL-C as variants that mimic the effect of
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Temsirolimus The amino hydroxy methyl isoxazolepropionic aci
2023-02-25

The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic Temsirolimus (AMPA) receptor is also enriched in postsynaptic striatal neurons (Bernard et al., 1997, Kondo et al., 2000, Reimers et al., 2011). Its activity is subjected to the regulation by a mechanism involving phosphorylation (Lu and Roche, 20
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FTI 277 HCl receptor To elucidate this relationship we devel
2023-02-21

To elucidate this relationship, we developed a spatial model of Ca-influx through N-methyl-D-aspartate receptor (NMDAR), CaMKII/PP1 activation, and AMPAR insertion in a realistic spine geometry. Using this model, we show that i) variables in membrane voltage mediated Ca-influx, particularly the numb
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Dose Response Studies Against Puromycin Sensitive Aminopepti
2023-02-21

Dose–Response Studies Against Puromycin–Sensitive Aminopeptidase (PSA). PSA is a ubiquitous metallopeptidase encoded by the NPEPPS gene with subcellular distribution in the cytosol and nucleus [49]. Comprising of a 919 amino Temsirolimus sequence, it has a broad substrate specificity, and is respon
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br There are three types
2023-02-20

There are three types of 5-HT2 receptors. 5-HT2A, 5-HT2B and 5-HT2C receptors Exhibit 46–50% overall sequence identity and couple preferentially to Gq/11 to increase inositol phosphates and cytosolic [Ca2+] and in agreement with their long known role in muscle contraction and stimulation in the br
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zilpaterol hydroxydopamine OHDA is a selective catecholamine
2023-02-20

6-hydroxydopamine (6-OHDA) is a selective catecholaminergic neurotoxin mainly used to generate lesions in the nigrostriatal pathway in rats (Ungerstedt, 1968). The most common use of 6-OHDA is via unilateral injection into the rat medial forebrain bundle (MFB). DA depletion, nigral DA cell loss, and
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Diabetes or inflammation is associated with up regulation
2023-02-20

Diabetes or inflammation is associated with up-regulation of A2AAR (Pang et al., 2010). High levels of A2AARs are found in macrophages and microglial cells that are poised, on activation, to abrogate the immune response (Trincavelli et al., 2008). In addition, hyperglycemia is associated with increa
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The first rationally designed dual mPGES LO inhibitor was
2023-02-20

The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic AZD2858 - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivatives have been synthesize
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In an AP scenario several inflammatory mediators
2023-02-20

In an AP scenario, several inflammatory mediators are produced locally to orchestrate an immune response. Eicosanoids are among those molecules and represent a class of lipid mediators synthesized from arachidonic AZD 0530 australia through the action of cyclooxygenases or lipoxygenases to generate
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NLX a k a F or befiradol exhibits
2023-02-20

NLX-112 (a.k.a. F13640 or befiradol), exhibits nanomolar affinity at 5-HT1A receptors, and, in Spermine NONOate to the 5-HT1A receptor agonists listed above, it presents exceptional selectivity and high efficacy at these receptors (Colpaert et al., 2002, Newman-Tancredi et al., 2017). Additionally,
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nkh In our previous report we synthesized derivatives with s
2023-02-20

In our previous report, we synthesized derivatives with some straight chain residues on the 2-position of the 3-cyanopyridine ring of compound 1. In this time we tried to introduce aromatic ring on the chain of the 2-position. Namely, we replaced the hydroxyl-alkylamino group in the position 2 of t
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br Introduction Lipoxygenases LOXs are
2023-02-20

Introduction Lipoxygenases (LOXs) are a heterogeneous family of enzymes that catalyze the peroxidation of polyunsaturated fatty acids (PUFAs). By oxidizing free PUFAs, they were shown to contribute to the generation of various bioactive lipid mediators. However, LOX-mediated oxidation of PUFAs es
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Tolcapone Receptor Subtypes and Their Function Critical Appr
2023-02-20

Receptor Subtypes and Their Function – Critical Appraisal Largely unselective ligands of the benzodiazepine binding site, such as diazepam, are known to elicit a wide range of in vivo effects including hypnosis, sedation, anxiolysis, and muscle relaxation. Genetically modified mice were introduced
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The MOB and AOB are important in ungulates Keller
2023-02-20

The MOB and AOB are important in ungulates (Keller and Levy, 2012, Sanchez-Andrade and Kendrick, 2009), which rely heavily on odorant information for social interactions (Baum and Cherry, 2015, Keller and Levy, 2012, Osada et al., 2014, Villagran and Ungerfeld, 2013). The release of GABA and glutama
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