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Cited by 949

The DOI matches its Crossref record; 3 of the 3 references it cites were found in a registry or an index.

Modes of action of the DNA methyltransferase inhibitors azacytidine and decitabine

Stresemann, Carlo, Lyko, Frank·2008·International Journal of Cancer

Abstract

The cytosine analogues 5‐azacytosine (azacytidine) and 2′‐deoxy‐5‐azacytidine (decitabine) are the currently most advanced drugs for epigenetic cancer therapies. These compounds function as DNA methyltransferase inhibitors and have shown substantial potency in reactivating epigenetically silenced tumor suppressor genes in vitro. However, it has been difficult to define the mode of action of these drugs in patients and it appears that clinical responses are influenced both by epigenetic alterations and by apoptosis induction. To maximize the clinical efficacy of azacytidine and decitabine it will be important to understand the molecular changes induced by these drugs. In this review, we examine the pharmacological properties of azanucleosides and their interactions with various cellular pathways. Because azacytidine and decitabine are prodrugs, an understanding of the cellular mechanisms mediating transmembrane transport and metabolic activation will be critically important for optimizing patient responses. We also discuss the mechanism of DNA methyltransferase inhibition and emphasize the need for the identification of predictive biomarkers for the further advancement of epigenetic therapies. © 2008 Wiley‐Liss, Inc.

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Metadata

Authors
Stresemann, C., & Lyko, F.
Venue
International Journal of Cancer
Publisher
Wiley
Published
2008-04-24
Volume
123
Issue
1
Pages
8-13
ISSN
  • 0020-7136 (ISSN-L)
  • 1097-0215
OpenAlex
W2017394727
Cited by
949
References
3
FWCI
13.40
Type
journal article
Language
en
Open access
closed

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CoChat. (2026). Citation check: Modes of action of the DNA methyltransferase inhibitors azacytidine and decitabine. https://app.cochat.ai/papers/10.1002/ijc.23607
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Stresemann, C., & Lyko, F. (2008). Modes of action of the DNA methyltransferase inhibitors azacytidine and decitabine. International Journal of Cancer. https://doi.org/10.1002/ijc.23607

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