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GABAB receptor is associated with brain and behavioral disea
2023-12-15
GABAB receptor is associated with NAD+ mg and behavioral diseases, including epilepsy, spasticity, anxiety and neuropathic pain (Bettler et al., 2004, Bowery et al., 2002, Froestl, 2010). Baclofen, a clinical drug and selective GABAB receptor agonist, is used to treat muscle spasticity in patients
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Chlorogenic acid an abundant polyphenol found in coffee and
2023-12-14
Chlorogenic rifadin (7), an abundant polyphenol found in coffee and the human diet, has various biological activities including antioxidant and anticancer effects [54]. Jiang et al. reported that compound 7 had a selective cytotoxic activity on human oral tumor cells (HSG, HSC-2) as compared with n
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br Materials and method br Results br Discussion Although se
2023-12-14
Materials and method Results Discussion Although several studies have showed the crude extracts of K. senegalensis possessed the anti-inflammatory and hypertensive activities (Olayinka et al., 1992). However, the anti-inflammatory effect and underlying molecular mechanisms of its bioactive
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HT modulates cortical and hippocampal pyramidal cell functio
2023-12-14
5-HT modulates cortical and hippocampal pyramidal cell function in a very complex manner, since most 5-HT receptor subtypes (excitatory as well as inhibitory) are expressed on pyramidal T-5224 as well as GABAergic interneurons that exert inhibitory control over pyramidal cells (Leiser et al., 2015,
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AdipoRon is an orally active synthetic small
2023-12-14
AdipoRon is an orally active, synthetic small molecule that activates adiponectin receptor (AdipoR). It mimics the antidiabetic effects of adiponectin, exhibiting its effect through the activation of AMPK and PPARα pathways via AdipoR1 and AdipoR2, respectively (Fig. 2) [62]. AdipoR activation has r
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The extent to which GPCR oligomerization
2023-12-14
The extent to which GPCR oligomerization is a regulated process still remains unclear. Reported effects of ligands on both GPCR homo- and heteromers are highly variable and depend on GPCR subtypes and the specific ligand used. According to our data, chronic treatment of mice with both paroxetine or
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Many metalloenzyme inhibitors consist of two chemical compon
2023-12-14
Many metalloenzyme inhibitors consist of two chemical components: the MBG, the portion of the inhibitor designed to bind to the metal, and the scaffold, the portion of the inhibitor recognized by the amino simvastin residues that form the substrate-binding site of the metalloenzyme. The MGB is often
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Aurora A the polar kinase is located at the centrosome
2023-12-13
Aurora A the ’polar kinase’ is located at the centrosome and is required for its maturation, division, for the mitotic spindle assembly and entry into mitosis., Mutation or transcriptional silencing of Aurora A impairs centrosome maturation and separation, leads to mono/multipolar spindles, to dela
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As shown in B the recombinant human LOX nM
2023-12-13
As shown in B, the recombinant human 15-LOX-1 (30nM) showed a time-dependent increase in fluorescent signal, and signal development was almost completed within 20min in the presence of 50μM arachidonic induced pluripotent stem cell and 5μM DHR. For both purified enzyme and cell lysates, the enzyme
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Previous studies have demonstrated ATR inhibition
2023-12-13
Previous studies have demonstrated ATR inhibition is effective for treating cancers combining with chemotherapies in lung adenocarcinoma, gastric cancer, HER2 positive breast cancer and chronic lymphocytic leukemia GANT61 to enhance chemotherapy sensitivity [[16], [17], [18],[20], [21], [22]]. VE-8
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Mitochondrial dysfunction resulting from mtDNA abnormalities
2023-12-13
Mitochondrial dysfunction resulting from mtDNA abnormalities may trigger retrograde signaling pathways from the mitochondrion to the nucleus, which regulate the expression of genes involved in diverse cellular processes, including metabolism, stress responses, tumor progression, nutrient sensing, li
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Thiol are reduced by two major
2023-12-13
Thiol are reduced by two major redox systems, glutathione/glutaredoxin (GRX) and thioredoxin (TRX), which have been extensively studied in plants [13], [14], [15]. Glutathione, a thiol-containing tripeptide, exists in a reduced (GSH) or an oxidized form (GSSG). It has a major role as a redox buffer.
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br HIF Signaling in AA Therapy Resistance An important resul
2023-12-13
HIF-α Signaling in AA Therapy Resistance An important result emerging from Phase 3 clinical trials testing AA therapies is improvement of progression-free survival (PFS) that is not accompanied by enhanced overall survival (OS) [26]. This dichotomy has been attributed to mechanisms of acquired re
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T-5224 The first identified auxiliary subunit stargazin
2023-12-13
The first identified auxiliary subunit, stargazin, is essential for AMPAR function in cerebellar granule neurons (Hashimoto et al., 1999). Subsequently, a family of six transmembrane AMPAR regulatory proteins (TARPs) were defined that modify channel trafficking, gating, and pharmacology (Kato and Br
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br Functional repercussions of each trimming pathway
2023-12-13
Functional repercussions of each trimming pathway A main difference between the two pathways presented in Fig. 1 lies in enzyme kinetics and selectivity. In pathway #1, the substrate for ERAP1 is free peptide, and so both kinetics and selectivity are determined by interactions between the peptide
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