Results 91 to 100 of about 4,050,496 (258)

Complete Pathway Refactoring and Combinatorial Biosynthesis of Anthracyclines for Modulation of Histone Eviction and DNA Damage Bioactivities

open access: yesAngewandte Chemie, EarlyView.
A synthetic biology platform was established for the complete refactoring of complex anthracycline biosynthetic pathways in Streptomyces coelicolor using standardized, chemically synthetic DNA parts. This modular construction enabled streamlined combinatorial biosynthesis, yielding novel analogs that decouple DNA damage from chromatin damage (histone ...
Rongbin Wang   +15 more
wiley   +2 more sources

Topoisomerase I poisons-induced autophagy: Cytoprotective, Cytotoxic or Non-protective

open access: yesAutophagy Reports, 2023
Topoisomerase I inhibitors represent a widely used class of antineoplastic agents that promote both single-stranded and double-stranded breaks in the DNA of tumor cells, leading to tumor cell death.
Ahmed M. Elshazly   +3 more
doaj   +1 more source

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

open access: yesAdvanced 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   +25 more
wiley   +1 more source

Tumor-targeted top1 inhibitor delivery with optimized parp inhibition in advanced solid tumors: a phase i trial of gapped scheduling

open access: yesNature Communications
Despite mechanistic rationale for combining PARP inhibitors with topoisomerase I inhibitors, clinical use has been hindered by dose-limiting toxicities.
Anish Thomas   +12 more
doaj   +1 more source

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

open access: yesAdvanced 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   +25 more
wiley   +1 more source

Structure Guided Design of Xanthomonas oryzae pv. oryzae Topoisomerase I Inhibitors

open access: yesProceedings, 2017
Topoisomerase inhibitors initiate the cell killing process by either stabilizing or increasing the amount of the covalent complex formed between the enzyme and cleaved DNA. [...]
Lakindu Samaranayake P. K.   +1 more
doaj   +1 more source

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

open access: yesAdvanced 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   +21 more
wiley   +1 more source

Anti-topoisomerase drugs as potent inducers of chromosomal aberrations

open access: yesGenetics and Molecular Biology, 2000
DNA topoisomerases catalyze topological changes in DNA that are essential for normal cell cycle progression and therefore they are a preferential target for the development of anticancer drugs.
Loredana Bassi, Fabrizio Palitti
doaj   +1 more source

DNA topoisomerases as molecular targets for anticancer drugs

open access: yesJournal of Enzyme Inhibition and Medicinal Chemistry, 2020
The significant role of topoisomerases in the control of DNA chain topology has been confirmed in numerous research conducted worldwide. The prevalence of these enzymes, as well as the key importance of topoisomerase in the proper functioning of cells ...
Kamila Buzun   +3 more
doaj   +1 more source

Long-lasting reduction in clonogenic potential of colorectal cancer cells by sequential treatments with 5-azanucleosides and topoisomerase inhibitors

open access: yesBMC Cancer, 2016
The currently approved therapies fail in a substantial number of colorectal cancer (CRC) patients due to the molecular heterogeneity of CRC, hence new efficient drug combinations are urgently needed.
A. Pawlak   +5 more
semanticscholar   +1 more source

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