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brompheniramine maleate receptor Our co IP data show
2023-10-16

Our co-IP data show that 5HT1A or 5HT2A receptors do not heterodimerize with mGluR1α receptors. Given that both 5-HT and mGlu receptors are GPCRs and produce anxiolytic effects, a degree of cooperativity via a functional cross-talk may still exist between these receptors [11]. In addition to the fun
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Our previous studies found that some steroid
2023-10-16

Our previous studies found that some steroid mimetic structures such as stilbene, biphenyl, naphthalene and benzothiophene rings were suitable for lipophilic moieties of 17,20-lyase inhibitors, and several inhibitors obtained using a steroid A, C-ring mimetic approach have already been published. Du
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In this paper we describe the formation
2023-10-16

In this paper, we describe the formation of a structure-based pharmacophore which lead to the discovery of several hydrophobic, yet non-lipid inhibitors of ATX. These compounds docked within the same volume occupied by the initial non-lipid inhibitors of ATX used to build the pharmacophore. Violatio
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Physiological total plasma LPA levels are normally less than
2023-10-16

Physiological total plasma LPA levels are normally less than 1μM in healthy subjects. LPA levels have been reported to be increased in malignant effusions or plasma in cancer patients [20]. In addition, increasing ATX activity detected in healthy pregnant women in the third trimester of pregnancy ex
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Preliminary results of studies sponsored by
2023-10-16

Preliminary results of studies sponsored by the manufacturer of ETC-1002 have also shown positive results for monotherapy in statin-intolerant patients and for the combined use of the ACL inhibitor plus other cholesterol-reducing agents. In patients with a documented history of intolerance to statin
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br Experimental EPR spectra of probes a f
2023-10-13

Experimental EPR spectra of probes 1a–f were recorded on a Bruker EMX-1572 operating at X-band (9.0–9.9 GHz), at 21 ± 1 °C. The EPR parameters were the same in all experiments: microwave power, 1 mW; modulation amplitude, 5 G; time constant, 10.24 ms; and conversion time, 40.96 ms. Reduced gluta
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A has been reported to decrease insulin
2023-10-13

Aβ has been reported to decrease insulin receptors and impair insulin signaling in neurons, preventing phosphorylation of Akt and glycogen synthase kinase 3β (GSK-3β), downstream of insulin signaling, and to increase phosphorylation of tau protein causing neurofibrillary tangles (Tokutake et al., 20
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Hepatic inflammation and fibrosis are
2023-10-13

Hepatic Z-DEVD-FMK and fibrosis are hallmarks of the NASH phenotype and are thought to occur in a subset of patients with NAFLD. While it is hypothesized that therapeutic lowering of hepatic lipids will be sufficient to improve hepatic fibrosis and inflammation secondarily, this remains controversia
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Previous studies have demonstrated that synaptic AMPARs can
2023-10-13

Previous studies have demonstrated that synaptic AMPARs can differ greatly in their mobility; some rapidly and constitutively procollagen c proteinase in and out of the synaptic membrane, while others remain somewhat stable in the synaptic membrane (Luscher et al., 1999, Luthi et al., 1999). We fin
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In the present study AP B preferentially released hydrophobi
2023-10-13

In the present study, AP31-B preferentially released hydrophobic Cdk1/2 Inhibitor III such as leucine and alanine from N-terminal of peptide (Fig. 4). The debittering ability of AP31-B seemed to depend on such substrate specificity, but additional tests against other hydrophobic amino acids are need
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The functional significance of the cap
2023-10-13

The functional significance of the cap residues with regard to the established role of PfA-M1 in hemoglobin catabolism in the food vacuole is a key question that is difficult to address with in vitro studies. We note that three of the dipeptide substrates used in our study are found in the sequences
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What is the mechanism by
2023-10-13

What is the mechanism by which Wnt7a-Fz7 signaling enhances AMPAR localization and synaptic strength? Following induction of LTP, the number of AMPARs rapidly increases at extrasynaptic sites (Makino and Malinow, 2009, Yang et al., 2008a) through PKA-dependent phosphorylation of GluA1 at S845 (He et
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The metabolism of amino acids into volatile aldehydes involv
2023-10-13

The metabolism of amino acids into volatile aldehydes involves both decarboxylation and deamination steps. The order of these reactions and the enzymes performing the catalysis differ among plants [13]. In tomato fruit the conversion of L-Phe to 2-phenylethanal is catalyzed by two enzymatic steps, i
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Recently two distinct small molecule inhibitors of PHGDH
2023-10-13

Recently, two distinct small-molecule inhibitors of PHGDH were identified using high-throughput screens, both of which inhibit de novo serine biosynthesis and show selective toxicity to cancer 8711 with high SSP flux [50,51]. The inhibitor NCT-503, which has an IC50 of 2.5μM, reduces the growth and
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Adiponectin is an adipokine whose circulating level is deple
2023-10-13

Adiponectin is an adipokine whose circulating level is depleted in a number of metabolic diseases including insulin resistance, diabetes and cancer (Khan et al., 2015, Singh et al., 2014a, Singh et al., 2014b, Yamauchi et al., 2014). Despite its importance in health and pathophysiology, adiponectin
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