31. Quantitative insights on impurities in ice cores at the micro-scale from calibrated LA-ICP-MS imagingPascal Bohleber, Piers Larkman, Nicolas Stoll, David Clases, Raquel Gonzalez de Vega, Martin Šala, Marco Roman, Carlo Barbante, 2024, izvirni znanstveni članek Objavljeno v DiRROS: 10.06.2024; Ogledov: 256; Prenosov: 200
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32. Guanidine modification improves functions of natural RNA-targeting alkaloidsTamaki Endoh, Sagar Satpathi, Yutong Chen, Saki Matsumoto, Tatsuya Ohyama, Peter Podbevšek, Janez Plavec, Kazumitsu Onizuka, Fumi Nagatsugi, Naoki Sugimoto, 2024, izvirni znanstveni članek Objavljeno v DiRROS: 10.06.2024; Ogledov: 226; Prenosov: 173
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33. Exploring hybrid hard carbon/▫$Bi_2S_3$▫-based negative electrodes for Na-ion batteriesBlaž Tratnik, Sergio Aina, Elena Tchernychova, Matej Gabrijelčič, Gregor Mali, Maria Pilar Lobera, Maria Bernechea, Mathieu Morcrette, Alen Vižintin, Robert Dominko, 2024, izvirni znanstveni članek Objavljeno v DiRROS: 06.06.2024; Ogledov: 336; Prenosov: 249
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34. Protein G-quadruplex interactions and their effects on phase transitions and protein aggregationBikash Ranjan Sahoo, Vojč Kocman, Nathan Clark, Nikhil Myers, Xiexiong Deng, Ee L. Wong, Harry J. Yang, Anita Kotar, Bryan B. Guzman, Daniel Dominguez, Janez Plavec, James C. A. Bardwell, 2024, izvirni znanstveni članek Objavljeno v DiRROS: 03.06.2024; Ogledov: 304; Prenosov: 331
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36. Nature-inspired substituted 3-(imidazol-2-yl) morpholines targeting human topoisomerase IIα : dynophore-derived discoveryBarbara Herlah, Matej Janežič, Iza Ogris, Simona Golič Grdadolnik, Katja Kološa, Sonja Žabkar, Bojana Žegura, Andrej Perdih, 2024, izvirni znanstveni članek Povzetek: The molecular nanomachine, human DNA topoisomerase IIα, plays a crucial role in replication, transcription, and recombination by catalyzing topological changes in the DNA, rendering it an optimal target for cancer chemotherapy. Current clinical topoisomerase II poisons often cause secondary tumors as side effects due to the accumulation of double-strand breaks in the DNA, spurring the development of catalytic inhibitors. Here, we used a dynamic pharmacophore approach to develop catalytic inhibitors targeting the ATP binding site of human DNA topoisomerase IIα. Our screening of a library of nature-inspired compounds led to the discovery of a class of 3-(imidazol-2-yl) morpholines as potent catalytic inhibitors that bind to the ATPase domain. Further experimental and computational studies identified hit compound 17, which exhibited selectivity against the human DNA topoisomerase IIα versus human protein kinases, cytotoxicity against several human cancer cells, and did not induce DNA double-strand breaks, making it distinct from clinical topoisomerase II poisons. This study integrates an innovative natural product-inspired chemistry and successful implementation of a molecular design strategy that incorporates a dynamic component of ligand-target molecular recognition, with comprehensive experimental characterization leading to hit compounds with potential impact on the development of more efficient chemotherapies.
Ključne besede: topoisomerase II, catalytic inhibitors, chemotherapy, DNA damage, cancer
Objavljeno v DiRROS: 03.06.2024; Ogledov: 454; Prenosov: 284
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