Results 71 to 80 of about 6,410,919 (241)

Heteronemin, a Marine Sesterterpenoid-Type Metabolite, Induces Apoptosis in Prostate LNcap Cells via Oxidative and ER Stress Combined with the Inhibition of Topoisomerase II and Hsp90

Marine Drugs, 2018
Heteronemin, a marine sesterterpenoid-type natural product, possesses diverse bioactivities, especially antitumor effect. Accumulating evidence shows that heteronemin may act as a potent anticancer agent in clinical therapy.
Man-Gang Lee, Yi-Chang Liu, Yi-Lun Lee, Mohamed El-Shazly, Kuei-Hung Lai, Shou-Ping Shih, Seng-Chung Ke, Ming-Chang Hong, Ying-Chi Du, Juan-Cheng Yang, Ping-Jyun Sung, Zhi-Hong Wen, Mei-Chin Lu   +12 more
doaj   +1 more source

The Natural Product Corramycin Acts as a DNA Gyrase Poison and Overcomes Fluoroquinolone Resistance in Mycobacterium tuberculosis

Advanced Science, EarlyView.
Corramycin, a myxobacterial natural product antibiotic, exhibits potent bactericidal activity against multidrug‐resistant Mycobacterium tuberculosis. The compound hijacks bacterial transporters such as BacA and OppABCD to enter the cell and inhibits DNA synthesis through a previously unrecognized mode of DNA gyrase poisoning, locking the enzyme in an ...
Franziska Fries, Jennifer Herrmann, Michael Dal Molin, Yaëlle Wormser, Timo Risch, Yunsheng Gao, Gareth Prosser, Francesca Gubellini, Ariel Mechaly, Joshua B. Wallach, Anthony Castro, Arka Banerjee, Sari Rasheed, Alexander Horn, Mathias Müsken, Michael Kurz, Lindsay Sonnenkalb, Viola Dreyer, Stefan Niemann, Sönke Andres, Dirk Schnappinger, Uli Kazmaier, Norbert Reiling, Rolf Müller, Jan Rybniker, Stéphanie Petrella   +25 more
wiley   +1 more source

Unveiling the Taxonomic Diversity and Unprecedented Biosynthetic Treasure of the Phylum Myxococcota

Advanced Science, EarlyView.
Natural products remain vital sources of therapeutics, and the phylum Myxococcota constitutes an especially rich reservoir for them. Based on decades of microbiological efforts, we present 154 new Myxococcota genomes and revise taxonomy quadrupling the number of families and genera.
Amay Ajaykumar Agrawal, Ronald Garcia, Guangyi Chen, Chantal D. Bader, Peter Sullivan, Alexander Popoff, Daniel Krug, Maja Hunter, Sebastian Walesch, Emilia Oueis, Christine Frank, Haowen Zhao, Joachim J. Hug, Sebastian Keller, Pascal Hirsch, Azat Tagirdzhanov, Tatiana Malygina, Mary Victory E. Gutierrez, Alexey Gurevich, Judith Boldt, Boyke Bunk, Jörg Overmann, Ulrich Nübel, Andreas Keller, Olga V. Kalinina, Rolf Müller   +25 more
wiley   +1 more source

Discovery and Optimization of AMT‐676, a CDH17‐Targeting ADC for the Treatment of Advanced Gastrointestinal Cancers

Advanced Science, EarlyView.
AMT‐676 is a novel antibody‐drug conjugate targeting CDH17, an adhesion molecule uniquely exposed on gastrointestinal tumor surfaces. Engineered with an optimized exatecan payload, it demonstrates profound tumor regression and a robust bystander effect across diverse preclinical models.
Ying‐nan Wang, Dan‐yun Ruan, Jing Shi, Yue Huang, Hui Sheng, Ya‐ling Huang, Linjie Ma, Lijun Wang, Caiwei Chen, Yixuan Wang, Yue Zhang, Yi Shen, Qing Zhang, Jianjian Zhang, Yanfang Tang, Jin‐ling Zhang, Jia‐jia Hu, Chen‐yi Wu, Jia‐ying Chen, Xun Meng, Shu‐Hui Liu, Feng Wang   +21 more
wiley   +1 more source

Novel Molecular Mechanism of Allicin-Mediated Inhibition of Bacterial Topoisomerase IV: A Combined Computational and Experimental Analysis

Natural Product Communications
Background/Objectives Allicin, a bioactive compound from garlic, exhibits antibacterial activity by targeting bacterial proteins, including type II topoisomerases such as DNA gyrase and topoisomerase IV enzymes exclusive to prokaryotes.
Ammar Khazaal Kadhim Almansoori, Raoof J. A. Maaroof, Ghadah Ali Al-Oudah, Nada Khazal K. Hindi, Lo Hui Yu, Haider Mahmod Jasim, Mohd Adnan, Mutaman Hussein Abdullah   +7 more
doaj   +1 more source

Palindromic carbazole derivatives: unveiling their antiproliferative effect via topoisomerase II catalytic inhibition and apoptosis induction

Journal of Enzyme Inhibition and Medicinal Chemistry
Human DNA topoisomerases are essential for crucial cellular processes, including DNA replication, transcription, chromatin condensation, and maintenance of its structure.
Mateusz Olszewski, Natalia Maciejewska, Anoop Kallingal, Agnieszka Chylewska, Aleksandra M. Dąbrowska, Małgorzata Biedulska, Mariusz Makowski, José M. Padrón, Maciej Baginski   +8 more
doaj   +1 more source

High mobility group A2 is a target for miRNA-98 in head and neck squamous cell carcinoma

Molecular Cancer, 2007
Background HMGA2 expression has been shown to be associated with enhanced selective chemosensitivity towards the topoisomerase (topo) II inhibitor, doxorubicin, in cancer cells.
Nikitakis Nikolaos, Scheper Mark A, Norris Kathleen, Hebert Carla, Sauk John J   +4 more
doaj   +1 more source

Pyrroloquinolinone-based dual topoisomerase I/II inhibitor

, 2014
A new series of pyrroloquinolinones bearing different alkylamino side chains were synthesized and evaluated as cytotoxic compounds against three different human tumor cell lines (HeLa, HL-60 and A431).
Gia, O., Marzaro, G., FERRARESE, ALESSANDRO, Ferrarese, A., DALLA VIA, LISA, GIA, ORNELLA MARIA, Adriana Chilin, Dalla Via, L., Giovanni Marzaro, CHILIN, ADRIANA, MARZARO, GIOVANNI, Lisa Dalla Via, Alessandro Ferrarese, Ornella Gia, Chilin, A.   +14 more
core   +1 more source

Epigenetic Reactivation of TNFRSF19 Suppresses Mitophagy and Sensitizes Triple‐Negative Breast Cancer to Doxorubicin

Advanced Science, EarlyView.
TNFRSF19 is an epigenetically silenced regulator of mitophagy in triple‐negative breast cancer. TNFRSF19 deficiency activates the TGFBR1–SMAD3–PINK1 axis to promote mitophagy and confer doxorubicin resistance, whereas decitabine‐mediated restoration of TNFRSF19 suppresses mitophagy and enhances doxorubicin sensitivity, revealing a targetable epigenetic–
Shiyang Liu, Chenguang Liu, Weihong Zheng, Xiaofei Tong, Zhengwei Gui, Zonghong Lu, Sun Ieong, Lin Zhang   +7 more
wiley   +1 more source

Tackling the Cytotoxic Effect of a Marine Polycyclic Quinone-Type Metabolite: Halenaquinone Induces Molt 4 Cells Apoptosis via Oxidative Stress Combined with the Inhibition of HDAC and Topoisomerase Activities

Marine Drugs, 2015
A marine polycyclic quinone-type metabolite, halenaquinone (HQ), was found to inhibit the proliferation of Molt 4, K562, MDA-MB-231 and DLD-1 cancer cell lines, with IC50 of 0.48, 0.18, 8.0 and 6.76 μg/mL, respectively.
Shou-Ping Shih, Man-Gang Lee, Mohamed El-Shazly, Yung-Shun Juan, Zhi-Hong Wen, Ying-Chi Du, Jui-Hsin Su, Ping-Jyun Sung, Yu-Cheng Chen, Juan-Cheng Yang, Yang-Chang Wu, Mei-Chin Lu   +11 more
doaj   +1 more source