Results 91 to 100 of about 61,437 (248)

Solvent dependency of the UV-Vis spectrum of indenoisoquinolines: role of keto-oxygens as polarity interaction probes. [PDF]

PLoS ONE, 2013
Indenoisoquinolines are the most promising non-campthotecins topoisomerase IB inhibitors. We present an integrated experimental/computational investigation of the UV-Vis spectra of the IQNs parental compound (NSC314622) and two of its derivatives ...
Andrea Coletta, Silvia Castelli, Giovanni Chillemi, Nico Sanna, Mark Cushman, Yves Pommier, Alessandro Desideri   +6 more
doaj   +1 more source

Ultrasound‐Boosted Liposomal Prodrug Overcomes Age‐Associated Biodistribution Disparity in Pediatric Solid Tumor Therapy

Advanced Science, EarlyView.
The age‐associated disparity of nanocarrier biodistribution limits the nanotherapeutics of childhood solid tumors. This study developed an ultrasound‐activated liposomal prodrug (CSCPTL) to overcome the age‐associated disparity of off‐target distribution.
Danfei Chen, Junjun Xu, Jian Chen, Jue Hu, Xiaobo Xuan, Haifang Cai, Mingdong Yang, Zhuxian Zhou, Guowei Wang   +8 more
wiley   +1 more source

Enhancing Antibacterial Efficacy: Combining Novel Bacterial Topoisomerase Inhibitors with Efflux Pump Inhibitors and Other Agents Against Gram-Negative Bacteria

Antibiotics
Background: The novel bacterial topoisomerase inhibitors (NBTIs) developed in our laboratory show potent on-target enzyme inhibition but suffer from low activity against Gram-negative bacteria.
Maša Zorman, Maja Kokot, Irena Zdovc, Lidija Senerovic, Mina Mandic, Nace Zidar, Andrej Emanuel Cotman, Martina Durcik, Lucija Peterlin Mašič, Nikola Minovski, Marko Anderluh, Martina Hrast Rambaher   +11 more
doaj   +1 more source

Mechanical Stimuli‐Induced Manipulation of Malignant Behavior in Bioprinted Cancer Microtissues via PI3K/NF‐κB Activation

Advanced Science, EarlyView.
A mechanically tunable ECM platform is created by integrating dECM–alginate matrices with in‐bath tumor printing. The mechanically tunable ECM environment drives tumors to acquire hypoxia, mechanotransduction signaling, metastatic traits, and drug‐resistant phenotypes that collectively promote malignant transformation.
Seok‐Hyeon Lee, Jeongho Lee, Min‐Seo Choi, Minjun Ahn, Sik Yoon, Dongjun Lee, Sae‐Ock Oh, Won‐Woo Cho, Byoung Soo Kim   +8 more
wiley   +1 more source

QSAR Modeling on Benzo[<em>c</em>]phenanthridine Analogues as Topoisomerase I Inhibitors and Anti-cancer Agents

Molecules, 2012
Benzo[<em>c</em>]phenanthridine (BCP) derivatives were identified as topoisomerase I (TOP-I) targeting agents with pronounced antitumor activity.
Thi-Ngoc-Phuong Huynh, Thanh-Dao Tran, Quang-Huynh Bui, Khac-Minh Thai   +3 more
doaj   +1 more source

Antibody‐Empowered Nanomedicine for Precise Biomedical Applications

Advanced Science, EarlyView.
This review explores strategies for functionalizing nanoparticles with antibodies to construct antibody‐empowered nanomedicine. It discusses the classification of these nanomedicines based on antibody structure, with a specific focus on their biomedical applications in diagnostics, bioimaging, and therapeutics for various diseases.
Chen Chen, Xinglin Chen, Zhenhao Gao, Meng Sun, Yaozong Yu, Fang Lv, Qiujun Wang, Jinfeng Zhang   +7 more
wiley   +1 more source

Artificial Intelligence for Bone: Theory, Methods, and Applications

Advanced Intelligent Discovery, EarlyView.
Advances in artificial intelligence (AI) offer the potential to improve bone research. The current review explores the contributions of AI to pathological study, biomarker discovery, drug design, and clinical diagnosis and prognosis of bone diseases. We envision that AI‐driven methodologies will enable identifying novel targets for drugs discovery. The
Dongfeng Yuan, Haicang Zhang, Liping Tong, Di Chen   +3 more
wiley   +1 more source

Topoisomerase II inhibitors induce DNA damage-dependent interferon responses circumventing Ebola virus immune evasion [PDF]

, 2017
Ebola virus (EBOV) protein VP35 inhibits production of interferon alpha/beta (IFN) by blocking RIG-I-like receptor signaling pathways, thereby promoting virus replication and pathogenesis.
Adolfo García-Sastre, Alexander Bukreyev, Ana Fernandez-Sesma, Benjamin C. Yen, Bersabeh Tigabu, Christopher F. Basler, Colette A. Pietzsch, Daisy W. Leung, Lorraine K. Morlock, Maria T. Sanchez-Aparicio, Noelle S. Williams, Priya Luthra, Sebastian Aguirre, Terence S. Dermody   +13 more
core   +3 more sources

Accelerating Primary Screening of USP8 Inhibitors from Drug Repurposing Databases with Tree‐Based Machine Learning

Advanced Intelligent Discovery, EarlyView.
This study introduces a tree‐based machine learning approach to accelerate USP8 inhibitor discovery. The best‐performing model identified 100 high‐confidence repurposable compounds, half already approved or in clinical trials, and uncovered novel scaffolds not previously studied. These findings offer a solid foundation for rapid experimental follow‐up,
Yik Kwong Ng, Sharon Ai Er Lam, Wei Chun Lim, Hannah Hui Min Toh, Shi Jun Ang   +4 more
wiley   +1 more source

Evodiamine Stabilizes Topoisomerase I-DNA Cleavable Complex to Inhibit Topoisomerase I Activity

Molecules, 2009
Evodiamine (EVO), an alkaloidal compound isolated from Evodia rutaecarpa (Juss.), has been reported to affect many physiological functions. Topoisomerase inhibitors have been developed in a variety of clinical applications.
Jau-Lang Hwang, Chiao-En Chen, Chun-Mao Lin, Chi-Ming Lee, Agnes L.-F. Chan, Wen-Shin Chang, Li-Min Chen   +6 more
doaj   +1 more source