Results 71 to 80 of about 61,437 (248)

Peptomer Linkers Enable Kinetic Control over Co‐Delivery of Multiple Chemotherapeutics

Advanced Healthcare Materials, EarlyView.
A key challenge in combinatorial chemotherapeutic drug delivery is independent control over release kinetics, especially with drugs of similar size and structure. Here, peptoid substitutions to proteolytically degradable peptides enabled the design of fast and slow‐releasing drug linkers.
Carolyn M. Watkins, Samuel L. Hallam, Mariah J. Austin, Adrianne M. Rosales   +3 more
wiley   +1 more source

Phosphodiesterase Type 5 (PDE5) Inhibitors Sensitize Topoisomerase II Inhibitors in Killing Prostate Cancer Through PDE5-Independent Impairment of HR and NHEJ DNA Repair Systems

Frontiers in Oncology, 2019
Human castration-resistant prostate cancer (CRPC) is a significant target of clinical research. The use of DNA-damaging agents has a long history in cancer chemotherapy but is limited by their toxicities.
Jo-Fan Chang, Jui-Ling Hsu, Yi-Hua Sheng, Wohn-Jenn Leu, Chia-Chun Yu, She-Hung Chan, She-Hung Chan, Mei-Ling Chan, Lih-Ching Hsu, Shih-Ping Liu, Jih-Hwa Guh   +10 more
doaj   +1 more source

Hybrid Inhibitors of DNA Gyrase A and B: Design, Synthesis and Evaluation

Pharmaceutics, 2020
The discovery of multi-targeting ligands of bacterial enzymes is an important strategy to combat rapidly spreading antimicrobial resistance. Bacterial DNA gyrase and topoisomerase IV are validated targets for the development of antibiotics.
Martina Durcik, Žiga Skok, Janez Ilaš, Nace Zidar, Anamarija Zega, Petra Éva Szili, Gábor Draskovits, Tamás Révész, Danijel Kikelj, Akos Nyerges, Csaba Pál, Lucija Peterlin Mašič, Tihomir Tomašič   +12 more
doaj   +1 more source

Repurposing of the ALK Inhibitor Crizotinib for Acute Leukemia and Multiple Myeloma Cells

Pharmaceuticals, 2021
Crizotinib was a first generation of ALK tyrosine kinase inhibitor approved for the treatment of ALK-positive non-small-cell lung carcinoma (NSCLC) patients.
Joelle C. Boulos, Mohamed E. M. Saeed, Manik Chatterjee, Yagmur Bülbül, Francesco Crudo, Doris Marko, Markus Munder, Sabine M. Klauck, Thomas Efferth   +8 more
doaj   +1 more source

Distinct requirements for the Rad32(Mre¹¹) nuclease and Ctp1(CtIP) in the removal of covalently bound topoisomerase I and II from DNA [PDF]

, 2009
For a cancer cell to resist treatment with drugs that trap topoisomerases covalently on the DNA, the topoisomerase must be removed. In this study, we provide evidence that the Schizosaccharomyces pombe Rad32Mre11 nuclease activity is involved in the ...
Akamatsu, Antony M. Carr, Baldwin, Champoux, Connelly, Connelly, Edgar Hartsuiker, El-Khamisy, Farah, Gutz, Hartsuiker, Hopfner, Hopfner, Keeney, Keeney, Krogh, Krogh, Lengsfeld, Limbo, Liu, Malik, Matthew J. Neale, McKee, Miyoshi, Moreau, Neale, Nitiss, Osheroff, Porter, Pouliot, Prinz, Sartori, Shaw, Stracker, Subramanian, Takashima, Tomita, Utsugi, Young   +38 more
core   +2 more sources

Architecture of an All‐In‐One Microfluidic Platform for Accelerated Cancer Seeding, Enhanced Spheroid Formation, and Dynamic Drug Screening Trials

Advanced Materials Technologies, EarlyView.
An all‐in‐one microfluidic platform consists of two‐layered PDMS channels integrated with a hydrogel microwell array. This platform enables flow‐driven tumor cell capture, enhanced spheroid formation within the microwells, and advective drug testing. ABSTRACT Effective cancer drug screening requires platforms that replicate the physiological complexity
Omar M. Rahman, Shengxi Lan, Dae Kun Hwang   +2 more
wiley   +1 more source

Regulation of the Aurora-A gene following topoisomerase I inhibition: implication of the Myc transcription Factor

Molecular Cancer, 2010
During the G2 phase of the cell cycle, the Aurora-A kinase plays an important role in centrosome maturation and progression to mitosis. In this study, we show in colorectal cell lines that Aurora-A expression is downregulated in response to topoisomerase
Valo Isabelle, Giraud Sandrine, Troadec Marie-Bérangère, Vigneron Arnaud, Cherier Julia, Courapied Sandy, Prigent Claude, Gamelin Erick, Coqueret Olivier, Barré Benjamin   +9 more
doaj   +1 more source

RIG‐I Mediated Neuron‐Specific IFN Type 1 Signaling in FUS‐ALS Induces Neurodegeneration and Offers New Biomarker‐Driven Individualized Treatment Options for (FUS‐)ALS

Advanced Science, EarlyView.
Using iPSC‐derived motoneurons and postmortem tissue from FUS‐ALS patients, it is demonstrated that increased mitochondrial transcription leads to elevated cytosolic double‐stranded RNA (dsRNA) levels. This aberrant accumulation activates a RIG‐I–dependent innate immune response leading to neurodegeneration, which is amenable for FDA‐ and EMA‐approved ...
Marcel Naumann, Theresa M. Wierschin, Stefanie Kretschmer, Banaja P. Dash, Aaron Held, Andrea Salzinger, Kevin Peikert, Anže Karlek, Hannes Glaß, Dajana Großmann, René Günther, Susanne Petri, Annekathrin Rödiger, David Brenner, Francisco Pan‐Montojo, Eleonora Aronica, Markus Kipp, Vitaly Zimyanin, Jared Sterneckert, Torsten Grehl, Noah D. Seebacher, Tobias M. Böckers, Alberto Catanese, Brian J. Wainger, Patrick Oeckl, Min Ae Lee‐Kirsch, Andreas Hermann   +26 more
wiley   +1 more source

Interactions of Antibody Drug Conjugate Anti‐Tubulin and Topoisomerase I Inhibitor Payloads with Radiotherapy to Potentiate Immunotherapy

Advanced Science, EarlyView.
Antibody drug conjugates deliver their cytotoxic anti‐tubulin or topoisomerase I inhibitor payloads to tumors through cancer cell receptor targeting. The released drug payloads induce cellular changes that interact with radiotherapy resulting in radiosensitization that improves cancer cell kill and stimulates anti‐tumor immune responses.
Jacqueline Lesperance, Bryan S. Yung, Michael M. Allevato, Marcus M Cheng, Maria F. Camargo, Robert Saddawi‐Konefka, Kanika Dhawan, Ashwyn K. Sharma, Mahsa Mortaja, Sophie Bice, Daniel J. Scanderbeg, Diego Alvarado, Jyoti Mayadev, Ramez N. Eskander, Stephen R. Adams, Pippa F. Cosper, J. Silvio Gutkind, Sunil J. Advani   +17 more
wiley   +1 more source

Quantitative Structure Activity Relationship Studies of Topoisomerase I Inhibitors as Potent Antibreast Cancer Agents

Journal of Chemistry, 2013
Topoisomerase I (TOP I) is a valuable molecular target for the development of clinically used anticancer agents. Indenoisoquinolines have emerged as potent topoisomerase I inhibitors.
Supriya Singh, Sucheta Das, Anubhuti Pandey, Sarvesh Paliwal, Rajeev Singh   +4 more
doaj   +1 more source