Publications by authors named "Emiko Sanada"
Article Synopsis
- β-TrCP is a specific protein involved in the ubiquitin-ligase complex that helps target proteins for degradation, which is important for regulating various cellular processes.
- Researchers developed a high-throughput screening system to find small molecules that can specifically inhibit β-TrCP, leading to the identification of several compounds that affect the ubiquitin-proteasome system.
- The hit compounds not only inhibited the degradation of specific proteins like IκBα but also revealed key molecular features like carboxyl and hydroxyl groups that interact with β-TrCP, contributing to potential therapeutic applications in regulating cellular signaling.
Article Synopsis
- * A screening of 5,600 microbial extracts led to the discovery of a broth from sp. RK19-A0402 that significantly inhibits c-Myc transcriptional activity and is structurally related to oligomycin A.
- * The identified compounds cause mitochondrial dysfunction, resulting in reactive oxygen species (ROS) production that activates GSK3α/β to phosphorylate c-Myc for degradation, suggesting a potential approach for developing anticancer agents.
Article Synopsis
- c-Myc is an important regulator of cell growth and its overexpression is linked to many cancers, making it a target for potential therapies.
- Researchers have faced challenges in developing specific inhibitors for c-Myc, so they instead focused on small molecules that affect its cofactors or repressors.
- A study identified antimycin A as a promising compound that enhances c-Myc degradation via ROS, linking its effectiveness to c-Myc levels in cancer cells and suggesting a new direction for cancer treatment.
Allantopyrone A is an α-pyrone metabolite that was originally isolated from the endophytic fungus Allantophomopsis lycopodina KS-97. We previously demonstrated that allantopyrone A exhibits anti-cancer, anti-inflammatory, and neuroprotective activities. In the present study, we showed that allantopyrone A up-regulated the protein expression of hypoxia-inducible factor (HIF)-1α in human fibrosarcoma HT-1080 cells.
View Article and Find Full Text PDFDiscovery of novel selenium derivatives as Pin1 inhibitors by high-throughput screening.
Biochem Biophys Res Commun
June 2016
Peptidyl prolyl cis/trans isomerization by Pin1 regulates various oncogenic signals during cancer progression, and its inhibition through multiple approaches has established Pin1 as a therapeutic target. However, lack of simplified screening systems has limited the discovery of potent Pin1 inhibitors. We utilized phosphorylation-dependent binding of Pin1 to its specific substrate to develop a screening system for Pin1 inhibitors.
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