3,266 results match your criteria: "Kyoto Pharmaceutical University.[Affiliation]"

Mucociliary clearance (MCC) is a host defense mechanism of the respiratory system. Beating cilia plays a crucial role in the MCC process and ciliary beat frequency (CBF) is activated by several factors including elevations of the intracellular cAMP concentration ([cAMP]), intracellular Ca concentration ([Ca]), and intracellular pH (pH). In this study, we investigated whether an artichoke-extracted component cynaropicrin could be a beneficial compound for improving MCC.

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SUMOylation, the modification of proteins with a small ubiquitin-like modifier (SUMO), is known to regulate various cellular events, including cell division. This process is dynamic, with its status depending on the balance between SUMOylation and deSUMOylation. While the regulation of cell division by sentrin-specific protease (SENP) family proteins through deSUMOylation has been investigated, the role of another deSUMOylase, deSUMOylating isopeptidase 1 (DESI1), remains unknown.

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Oxidation of thiol groups in membrane proteins inhibits the fertilization ability and motility of sperm by suppressing calcium influx.

Biol Reprod

December 2024

Division of Reproductive Engineering, Center for Animal Resources and Development (CARD), Institute of Resource Development and Analysis, Kumamoto University, 2-2-1 Honjo, Chuo-ku, Kumamoto 860-0811, Japan.

The redox state of thiol groups derived from cysteine residues in proteins regulates cellular functions. Changes in the redox state of thiol groups in the epididymis are involved in sperm maturation. Furthermore, the redox state of thiol groups in proteins changes during the process of sperm capacitation.

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Cutaneous colonization with Staphylococcus aureus (SA) is frequently observed in patients with atopic dermatitis. SA produces a wide variety of bacterial toxins, among which δ-toxin was found to induce degranulation of mast cells. Degranulation of mast cells could enhance bacterial clearance and protection from future SA infection but lead to exacerbation of atopic dermatitis.

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Ephexin proteins are guanine nucleotide exchange factors for the Rho GTPases. We reported that Ephexin4 regulates M-phase progression downstream of phosphorylated EphA2, a receptor-type tyrosine kinase, through RhoG activation; however, the regulation of Ephexin4 during M phase remains unknown. In this study, a novel Ephexin4 phosphorylation site was identified at Ser41, exclusively in M phase.

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TNK2 is a ubiquitously expressed nonreceptor-type tyrosine kinase. TNK2 participates in tumorigenesis, and TNK2 activation has been found in various cancers; therefore, TNK2 is a promising target for cancer chemotherapy. While the TNK2 inhibitor XMD16-5 is highly selective, it inhibits cytokinesis at higher concentrations by targeting Aurora B kinase, a key enzyme for cell division.

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Article Synopsis
  • * In Japan, there is a system for certifying pharmacists in palliative care, but research on the impact of their interventions is limited.
  • * A study found that interventions by certified pharmacists significantly reduced hospitalizations for pain management and extended both the timeline for hospitalizations after starting opioid treatment and the duration of outpatient visits, thus enhancing patient care.
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Background/aim: Aberrant activation of the Wnt/β-catenin signaling pathway contributes to the pathogenesis of acute myelogenous leukemia (AML). Thus, targeting this pathway offers a promising therapeutic strategy against AML. Here, we synthesized a novel dipeptide-type inhibitor of the Wnt/β-catenin signaling pathway, compound #41, and explored its anti-tumor effects on AML cells.

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Targeting Oxidative Phosphorylation with a Novel Thiophene Carboxamide Increases the Efficacy of Imatinib against Leukemic Stem Cells in Chronic Myeloid Leukemia.

Int J Mol Sci

October 2024

Division of Hematology, Respiratory Medicine and Oncology, Department of Internal Medicine, Faculty of Medicine, Saga University, Saga 849-8501, Japan.

Patients with chronic myeloid leukemia (CML) respond to tyrosine kinase inhibitors (TKIs); however, CML leukemic stem cells (LSCs) exhibit BCR::ABL kinase-independent growth and are insensitive to TKIs, leading to disease relapse. To prevent this, new therapies targeting CML-LSCs are needed. Rates of mitochondria-mediated oxidative phosphorylation (OXPHOS) in CD34CML cells within the primitive CML cell population are higher than those in normal undifferentiated hematopoietic cells; therefore, the inhibition of OXPHOS in CML-LSCs may be a potential cure for CML.

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Background: Boron neutron capture therapy (BNCT) is a next-generation radiotherapy, utilizing both an external neutron beam and a -containing pharmaceutical. A compact accelerator for a high intensity neutron source was installed to conduct BNCT in a hospital. The dose administered to a patient was evaluated by measuring the proton beam current.

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Seven new polyketides [moringols I-VII (1-7)], a new alkaloid [moringamine I (8)], and seven known compounds (9-15) were isolated from the fungus Curvularia moringae JKYM-KR4. The planar chemical structures and relative configurations of the new compounds were elucidated by high-resolution mass spectrometry, 1D and 2D NMR spectroscopy, and DP4+ analysis using the calculated C NMR chemical shifts. For moringols I and II (1 and 2), the planar chemical structures and relative configurations were confirmed using X-ray crystallography.

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Article Synopsis
  • Glioblastoma stem cells (GSCs) contribute to the aggressive nature of glioblastoma by making the tumor resistant to therapies, and high levels of γ-Glutamylcyclotransferase (GGCT) are linked to this resistance.
  • Inhibition of GGCT reduces GSC proliferation, and its expression is regulated by the protein c-Jun, which is influenced by the NRas protein.
  • GGCT knockdown not only hampers GSC growth but also disrupts the Delta-Notch signaling pathway by lowering Notch1 levels, suggesting GGCT is a promising target for new glioblastoma treatments.
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Elastin-like peptides (ELPs) exhibit lower critical solution temperature (LCST)-type behavior, being soluble at low temperatures and insoluble at high temperatures. While the properties of linear, long-chain ELPs are well-studied, short-chain ELPs, especially those with branched architectures, have been less explored. Herein, to obtain further insights into multimeric short ELPs, we investigated the temperature-responsive properties of branched molecules composed of a repeating pentapeptide unit of short ELPs, Phe-Pro-Gly-Val-Gly, as side components and oligo(Glu) as a backbone structure.

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Itch is a prominent symptom of atopic dermatitis (AD). However, the underlying mechanism remains complex and has not yet been fully elucidated. Mas-related G protein-coupled receptor A3 (MrgprA3) has emerged attention as a marker of primary sensory neurons that specifically transmit itch signals; however, its involvement in AD-related itch has not been extensively explored.

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Mechanistic Insights into the Effect of Sodium Iodide on Copper-Mediated Iododeboronation.

Chemistry

December 2024

Laboratory of Analytical and Bioinorganic Chemistry, Division of Analytical and Physical Sciences, Kyoto Pharmaceutical University, 5 Nakauchi-cho, Misasagi, Yamashina-ku, Kyoto, 607-8414, Japan.

The copper-catalyzed Chan-Evans-Lam (CEL) coupling reaction advances carbon-heteroatom cross-coupling and has facilitated the development of radiohalogenation methodologies in radiochemistry. This study investigated the mechanisms and side reactions of CEL iodination under conditions relevant to radiosynthesis and typical organic synthesis, focusing on the effects of sodium iodide. The concentrations of copper and iodide, as well as the copper-to-iodide ratio, were identified as significant factors for successful copper-mediated CEL iodination, influencing the reaction mechanisms and side reactions.

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Extracellular Vesicle Inhibitors Enhance Cholix-Induced Cell Death via Regulation of the JNK-Dependent Pathway.

Toxins (Basel)

August 2024

Laboratory of Microbiology and Infection Control, Division of Biological Sciences, Kyoto Pharmaceutical University, Kyoto 607-8414, Japan.

is an important foodborne pathogen. Cholix cytotoxin (Cholix), produced by , is a novel eukaryotic elongation factor 2 (eEF2) adenosine diphosphate ribosyltransferase that causes host cell death by inhibiting protein synthesis. However, the role of Cholix in the infectious diseases caused by remains unclear.

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Structure-activity relationships study of -ethylene glycol-comprising alkyl heterocyclic carboxamides against A549 lung cancer cells.

Future Med Chem

November 2024

Laboratory of Pharmaceutical Manufacturing Chemistry, Kyoto Pharmaceutical University, 1 Misasagi-Shichono-cho, Yamashina-ku, Kyoto, 607-8412, Japan.

Certain cancer cells depend on oxidative phosphorylation for survival; thus, inhibiting this process may be a promising treatment strategy. This study explored the structure-activity relationships of the mitochondrial inhibitor -ethylene glycol-comprising alkyl thiophene-3-carboxamide . We synthesized and evaluated 13 analogs (-) with different ethylene glycol units, heterocycles and connecting groups for their growth-inhibitory effects on A549 non-small cell lung cancer cells.

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Effectiveness of tramadol-including multimodal analgesia in spinal surgery: a single-center, retrospective cohort study.

J Pharm Health Care Sci

September 2024

Laboratory of Clinical Pharmacoepidemiology, Kyoto Pharmaceutical University, 5 Misasagi Nakauchi-Cho, Kyoto, Yamashina-Ku, Kyoto-Shi, 607-8414, Japan.

Background: Multimodal analgesia (MMA) is recommended for postoperative pain management; however, studies evaluating the effect of tramadol-including MMA on numerical rating scale (NRS)-based postoperative pain levels and the length of stay (LOS) in the hospital are limited. Therefore, this study aimed to compare the before and after effects of tramadol-including MMA application, and assess its effect on postoperative NRS scores and LOS.

Methods: Patients who underwent spinal surgery under general anesthesia at the Rakuwakai Marutamachi Hospital in fiscal years 2020 and 2022 were included in this study.

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Lipid-Mediated Mechanisms of Thermal Adaptation and Thermoregulatory Behavior in Animals.

Adv Exp Med Biol

September 2024

Department of Synthetic Chemistry and Biological Chemistry, Graduate School of Engineering, Kyoto University, Kyoto, Japan.

Temperature affects a variety of cellular processes because the molecular motion of cellular constituents and the rate of biochemical reactions are sensitive to temperature changes. Thus, the adaptation to temperature is necessary to maintain cellular functions during temperature fluctuation, particularly in poikilothermic organisms. For a wide range of organisms, cellular lipid molecules play a pivotal role during thermal adaptation.

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Radioimaging Foam Cells Infiltrating Atherosclerotic Plaques in Mice Using I-labeled oxLDL as a Radiotracer.

Mol Imaging Biol

December 2024

Joint Research Laboratory, Division of Integrated Pharmaceutical Sciences, Kyoto Pharmaceutical University, Misasagi, Yamashina-Ku, Kyoto, 607-8414, Japan.

Article Synopsis
  • Bioimaging techniques like magnetic resonance are currently used to track atherosclerotic plaques made up of foam cells formed from macrophages that ingest oxidized low-density lipoprotein (oxLDL), but these methods lack specificity and sensitivity.
  • This study tested iodine-125-labeled oxLDL (I-oxLDL) as a new radiotracer for better detection of foam cells in atherosclerotic plaques using various imaging techniques.
  • Results showed that macrophages effectively took up I-oxLDL, allowing a notable radioactive signal to be detected in atherosclerotic plaques, indicating I-oxLDL's potential to enhance bioimaging techniques in the future.
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Unlabelled: imaging of bacterial infection models enables noninvasive and temporal analysis of individuals, enhancing our understanding of infectious disease pathogenesis. Conventional imaging methods for bacterial infection models involve the insertion of the bacterial luciferase LuxCDABE into the bacterial genome, followed by imaging using an expensive ultrasensitive charge-coupled device (CCD) camera. However, issues such as limited light penetration into the body and lack of versatility have been encountered.

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Multiple site inflammation and acute kidney injury in crush syndrome.

Front Pharmacol

August 2024

Department of General Medicine Education, School of Medicine, Keio University, Tokyo, Japan.

Article Synopsis
  • - Crush syndrome is a common consequence of earthquakes that can lead to acute kidney injury caused by muscle breakdown (rhabdomyolysis) and is worsened by systemic inflammatory response syndrome (SIRS).
  • - A study using mice with rhabdomyolysis showed high levels of inflammatory markers in both serum and the peritoneal cavity, where inflammation was more pronounced in the peritoneum.
  • - Administering a novel peptide that inhibits inflammation in the intraperitoneal cavity helped reduce muscle damage and kidney injury, suggesting that targeting inflammation in multiple areas could be beneficial for treatment.
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Preparation and application of multiple particle binding-liposomes for electrochemiluminescent signal amplification in bioassays.

Anal Bioanal Chem

November 2024

Laboratory of Analytical Chemistry, Kyoto Pharmaceutical University, 5 Misasaginakauchi-cho, Yamashina-ku, Kyoto, 607-8414, Japan.

In this study, multiple particle binding-liposomes (MPB-Lips), encapsulating the luminophore tris(2',2-bipyridyl)ruthenium (II) complex ([Ru(bpy)]), were developed as an electrochemiluminescence (ECL) signal amplifier and were applied to detect the model analyte streptavidin (SA) using the indirect competitive ECL method. The MPB-Lips were prepared by mixing various ratios of two different liposomes-one containing a phospholipid with a primary amine group and a biotinyl group (BIO/NH-Lip) and one containing a phospholipid with an N-hydroxysuccinimide group (NHS-Lip) to allow binding between particles via amide bonds. Quartz crystal microbalance analysis using SA-modified gold-coated quartz crystals showed that the frequency shift values of MPB-Lips gradually decreased in the order BIO/NH-Lip:NHS-Lip = 1:0 < 1:1 < 1:3 < 1:5.

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Amino acid transporters play a vital role in cellular homeostasis by maintaining protein synthesis. L-type amino acid transporter 1 (LAT1/SLC7A5/CD98lc) is a major transporter of large neutral amino acids in cancer cells because of its predominant expression. Although amino acid restriction with various amino acid analog treatments is known to induce mitotic defects, the involvement of amino acid transporters in cell division remains unclear.

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