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N-Glycoside of Indolo[2,3-]pyrrolo[3,4-]carbazole LCS1269 Exerts Anti-Glioblastoma Effects by G2 Cell Cycle Arrest and CDK1 Activity Modulation: Molecular Docking Studies, Biological Investigations, and ADMET Prediction.
Pharmaceuticals (Basel)
December 2024
Laboratory of Molecular and Cellular Neurogenetics, N.N. Burdenko National Medical Research Center of Neurosurgery, 125047 Moscow, Russia.
Indolo[2,3-]pyrrolo[3,4-]carbazole scaffold is successfully used as an efficient structural motif for the design and development of different antitumor agents. In this study, we investigated the anti-glioblastoma therapeutic potential of glycosylated indolocarbazole analog LCS1269 utilizing in vitro, in vivo, and in silico approaches. Cell viability was estimated by an MTT assay.
View Article and Find Full Text PDFSynergistic two-step inhibition approach using a combination of trametinib and onvansertib in KRAS and TP53-mutated colorectal adenocarcinoma.
Biomed Pharmacother
January 2025
Department of Pharmacy, College of Pharmacy, Institute of Pharmaceutical Science and Technology, Hanyang University, Ansan, Gyeonggi-do 15588, Republic of Korea. Electronic address:
Colorectal malignancies associated with KRAS and TP53 mutations led us to investigate the effects of combination therapy targeting KRAS, MEK1, or PLK1 in colorectal cancer. MEK1 is downstream of RAS in the MAPK pathway, whereas PLK1 is a mitotic kinase of the cell cycle activated by MAPK and regulated by p53. Bioinformatics analysis revealed that patients with colorectal cancer had a high expression of MAP2K1 and PLK1.
View Article and Find Full Text PDFThe histone H3.3 K27M mutation suppresses Ser31phosphorylation and mitotic fidelity, which can directly drive gliomagenesis.
Curr Biol
December 2024
The Hormel Institute, University of Minnesota, Austin, MN 55912, USA; Masonic Cancer Center, University of Minnesota, Minneapolis, MN 55455, USA. Electronic address:
Serine 31 is a phospho-site unique to the histone H3.3 variant; mitotic phospho-Ser31 is restricted to pericentromeric heterochromatin, and disruption of phospho-Ser31 results in chromosome segregation defects and loss of p53-dependant G cell-cycle arrest. Ser31 is proximal to the H3.
View Article and Find Full Text PDFUSP44 regulates HEXIM1 stability to inhibit tumorigenesis and metastasis of oral squamous cell carcinoma.
Biol Direct
December 2024
Clinical Systems Biology Laboratories, The First Affiliated Hospital of Zhengzhou University, 1 Longhu Zhonghuan Road, Jinshui District, Zhengzhou, Henan, 450001, China.
Oral squamous cell carcinoma (OSCC) is the most frequent type of oral malignancy with high metastasis and poor prognosis. The deubiquitinating enzyme Ubiquitin Specific Peptidase 44 (USP44) regulates the mitotic checkpoint, and its deficiency leads to aneuploidy and increases tumor incidence. However, the role of USP44 in OSCC is not well understood.
View Article and Find Full Text PDFbta-miR-484 Inhibits Bovine Intramuscular Adipogenesis by Regulating Mitotic Clonal Expansion via the MAP3K9/JNK/CCND1 Axis.
J Agric Food Chem
December 2024
College of Animal Science and Technology, Northwest A&F University, Yangling, Shaanxi 712100, PR China.
Intramuscular fat (IMF) content is a critical indicator of the beef nutritional value and flavor. In this study, we focused on bta-miR-484, a microRNA that is differentially expressed during the adipogenic differentiation of bovine intramuscular adipocytes and is negatively correlated with the IMF content across different cattle breeds. Our findings demonstrate that bta-miR-484 inhibits adipogenic differentiation without altering the fatty acid composition of bovine intramuscular adipocytes.
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