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SND1-SMARCA5 interaction strengthened by PIM promotes the proliferation, metastasis, and chemoresistance of esophageal squamous cell carcinoma.
Int J Biol Macromol
December 2024
Department of Thoracic Surgery, Affiliated Hospital of Southwest Medical University, Luzhou 646000, China. Electronic address:
Chromatin remodeling plays a pivotal role in the progression of esophageal squamous cell carcinoma (ESCC), but the precise mechanisms remain poorly understood. Here, we elucidated the critical function of staphylococcal nuclease and tudor domain-containing 1 (SND1) in modulating chromatin dynamics, thereby driving ESCC progression in both in vitro and in vivo models. Our data revealed that SND1 was markedly overexpressed in ESCC cell lines.
View Article and Find Full Text PDFFDA-approved drugs as PIM-1 kinase inhibitors: A drug repurposed approach for cancer therapy.
Int J Biol Macromol
December 2024
Department of Biotechnology, Faculty of Life Sciences, Jamia Millia Islamia, New Delhi 110025, India. Electronic address:
PIM-1 kinase, a member of the Serine/Threonine kinase family, has emerged as a promising therapeutic target in various cancers due to its role in promoting tumor growth and resistance to conventional therapies. In this study, we employed a structure-based approach to screen 3800 FDA-approved drugs to discover potential inhibitors of PIM-1 after an initial selection of 50 candidates based on high docking scores. Four drugs, stanozolol, alfaxalone, rifaximin, and telmisartan, were identified as strong PIM-1 binders, interacting with key residues in the ATP-binding pocket of the kinase.
View Article and Find Full Text PDFHarnessing natural compounds for PIM-1 kinase inhibition: A synergistic approach using virtual screening, molecular dynamics simulations, and free energy calculations.
Cell Mol Biol (Noisy-le-grand)
November 2024
Department of Health Informatics, College of Applied Medical Sciences, Qassim University, Buraydah 51452, Saudi Arabia .
Cancer has substantial economic ramifications for healthcare systems. PIM kinases, specifically PIM-1, are commonly upregulated in different types of cancers, thereby promoting cancer development. PIM-1 inhibitors have garnered interest for their potential efficacy in cancer therapy.
View Article and Find Full Text PDFPro-viral Insertion site for the Moloney Murine Leukemia virus 1 (PIM-1) is widely involved in various biological processes and diseases, which is based on its structure and functional sites. However, the relationship between active sites and function of PIM-1 kinase remains unclear due to the lack of effective study approaches in live cells. Herein, to visualize the effect of different active sites in PIM-1 protein on its function activity and relation with PI3K/Akt/mTOR pathway, three mutant probes of EPHY which was developed previously based on fluorescence resonance energy transfer (FRET) technology to detect PIM-1 kinase activity in living cells were further constructed and transfected into cells followed by treating with PIM-1 inhibitors, ATP and PI3K inhibitor, respectively.
View Article and Find Full Text PDFSynthesis of novel pyridine and pyrazolyl pyridine conjugates with potent cytotoxicity against HepG2 cancer cells as PIM-1 kinase inhibitors and caspase activators.
RSC Adv
December 2024
Department of Chemistry, Faculty of Science, Suez Canal University Ismailia 41522 Egypt
A novel series of nicotinonitrile and pyrazolyl nicotinonitrile were synthesized, and their PIM-1 kinase inhibitors and caspase activators were investigated. New Manich bases 6-8 were synthesized reaction of pyridine 4 with piperidine, dimethyl amine, and morpholine in the presence of formalin. On the other hand, the pyrazolyl analogues 10-12 were synthesized heterocyclization of acetohydrazide derivative 9 with acetylacetone, malononitrile, and ethyl cyanoacetate, respectively, in ethanol.
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