Mechanisms regulating resistance to inhibitors of topoisomerase II

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Mechanisms regulating resistance to inhibitors of topoisomerase II

Inhibitors of topoisomerase II (topo II) are clinically effective in the management of hematological malignancies and solid tumors. The efficacy of anti-tumor drugs targeting topo II is often limited by resistance and studies with in vitro cell culture models have provided several insights on potential mechanisms. Multidrug transporters that are involved in the efflux and consequently reduced c...

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Topoisomerase Inhibitors and Types of Them

Objective: In this paper, we have introduced topoisomerase inhibitors, mechanism of action and types of them. DNA topoisomerases are ubiquitous enzymes that catalyze essential enzymes to solve the topological problems accompanying key nuclear processes such as DNA replication, transcription, repair and chromatin assembly by introducing temporary single or double strand breaks in the DNA. Result...

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Topoisomerase Inhibitors and Types of Them

Objective: In this paper, we have introduced topoisomerase inhibitors, mechanism of action and types of them. DNA topoisomerases are ubiquitous enzymes that catalyze essential enzymes to solve the topological problems accompanying key nuclear processes such as DNA replication, transcription, repair and chromatin assembly by introducing temporary single or double strand breaks in the DNA. Result...

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Altered DNA topoisomerase II activity in Chinese hamster cells resistant to topoisomerase II inhibitors.

Most DNA intercalators and epipodophyllotoxins inhibit mammalian topoisomerase II by trapping the enzyme within DNA cleavage complexes that can be detected in cells as protein-associated DNA strand breaks. We have characterized previously a line of Chinese hamster cells (DC3F/9-OHE cells) the resistance of which to the cytotoxic effect of intercalators and etoposide is associated with a reduced...

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ژورنال

عنوان ژورنال: Frontiers in Pharmacology

سال: 2013

ISSN: 1663-9812

DOI: 10.3389/fphar.2013.00089