Pim-1 kinase is a cytoplasmic serine/threonine kinase that controls programmed cell death by phosphorylating substrates that regulate both apoptosis and cellular metabolism. A series of 2-styrylquinolines and quinoline-2-carboxamides has been identified as potent inhibitors of the Pim-1 kinase. The 8-hydroxy-quinoline 7-carboxylic acid moiety appeared to be a crucial pharmacophore for activity. Molecular modeling indicated that interaction of this scaffold with Asp186 and Lys67 residues within the ATP-binding pocket might be responsible for the kinase inhibitory potency.
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Constitutive surface expression of the thromboxane A2 receptor is Pim kinase-dependent.
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Department of Life Sciences, Faculty of Science and Engineering, Manchester Metropolitan University, Manchester, United Kingdom; Discovery and Translational Science Department, Leeds Institute of Cardiovascular and Metabolic Medicine, Faculty of Medicine and Health, University of Leeds, Leeds, United Kingdom. Electronic address:
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January 2025
Department of Neurosurgery, Qilu Hospital, Cheeloo College of Medicine and Institute of Brain and Brain-Inspired Science, Shandong University, Shandong, China.
Article Synopsis
- Endothelial-to-mesenchymal transition (EndMT) is a process where endothelial cells transform into a different cell type, contributing to the dysfunction that initiates atherosclerosis, but the exact triggers in atherosclerotic environments are not well understood.
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Department of Urology, Jinjiang Municipal Hospital, Luoshan Section, No. 16 Jinguang Road, Luoshan Street, Jinjiang City, Quanzhou, Fujian, China.
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View Article and Find Full Text PDFIntegration of bulk/scRNA-seq and multiple machine learning algorithms identifies PIM1 as a biomarker associated with cuproptosis and ferroptosis in abdominal aortic aneurysm.
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Department of Vascular Surgery, Shandong Provincial Hospital Affiliated to Shandong First Medical University, Jinan, Shandong, China.
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FDA-approved drugs as PIM-1 kinase inhibitors: A drug repurposed approach for cancer therapy.
Int J Biol Macromol
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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.
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