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Antibiotic-derived approaches in cancer therapy: effectiveness of ikarugamycin in hexokinase-2 inhibition, tissue factor modulation, and metabolic regulation in breast cancer.
Anticancer Drugs
January 2025
Department of Biochemistry, Institute of Health Science.
We aimed to explore the role of ikarugamycin (IKA) in breast cancer, its connection with hexokinase-2 (HK-2) repression, and tissue factor (TF). This study sought to extend the role of HK-2 as a TF activator in a comprehensive analysis of these interactions from the enzyme, gene, and protein levels. The investigation was performed with MDA-MB-231 and MCF-7 breast cancer lines.
View Article and Find Full Text PDFPyrazinyl-Substituted Aminoazoles as Covalent Inhibitors of Thrombin: Synthesis, Structure, and Anticoagulant Properties.
ACS Pharmacol Transl Sci
January 2025
Institute of Pharmaceutical and Medicinal Chemistry, University of Münster, 48149 Münster, Germany.
This study presents a novel series of -acylated 1,2,4-triazol-5-amines and 1-pyrazol-5-amines, featuring a pyrazin-2-yl moiety, developed as covalent inhibitors of thrombin. These compounds demonstrated potent inhibitory activity, with derivatives and achieving IC values as low as 0.7 and 0.
View Article and Find Full Text PDFSibanin, a novel black fly-derived Kunitz protease inhibitor, prevents thrombus formation in mice by anticoagulation-antiplatelet duality.
Int J Biol Macromol
January 2025
School of Basic Medical Sciences, Kunming Medical University, Kunming 650500, Yunnan, China. Electronic address:
Most Kunitz inhibitors exhibit serine protease inhibitory activity, but limited information is available on the regulation of platelet function. Herein, we report the purification and characterization of a novel single Kunitz domain inhibitor (Sibanin) from the salivary glands of the black fly Simulium bannaense. Recombinant Sibanin prolonged activated partial thromboplastin time and prothrombin time, and exhibited high-affinity binding to FXa and elastase with a KD of 5.
View Article and Find Full Text PDFα-Synuclein Deletion Impairs Platelet Function: A Role for SNARE Complex Assembly.
Cells
December 2024
Biomedical Institute for Multimorbidity, Hull York Medical School, University of Hull, Hull HU6 7RX, UK.
Granule secretion is an essential platelet function that contributes not only to haemostasis but also to wound healing, inflammation, and atherosclerosis. Granule secretion from platelets is facilitated, at least in part, by Soluble N-ethylmaleimide-Sensitive Factor (NSF) Attachment Protein Receptor (SNARE) complex-mediated granule fusion. Although α-synuclein is a protein known to modulate the assembly of the SNARE complex in other cells, its role in platelet function remains poorly understood.
View Article and Find Full Text PDFAnticoagulant Activity of the Polysaccharide Fromgonad of Abalone Ino: The Role of Conjugate Protein.
Foods
December 2024
National Engineering Research Center of Seafood, School of Food Science and Technology, Dalian Polytechnic University, Dalian 116034, China.
Few studies are concerned with the effect of the conjugat protein on the bioactivities of the abalone gonad polysaccharide (AGP). In this study, a series of treatments, including raw material (female and male) defatting, extraction temperature (25-121 °C), proteolysis, ultrafiltration, and ethanol precipitation, was conducted to investigate the role of the conjugate protein on AGP anticoagulant activity. All AGP extracts significantly prolonged activated partial thromboplastin time (APTT) and thrombin time (TT).
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