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Cancer Chemotherapy and Pharmacology

Erschienen in:

01.11.2006 | Short Communication

FK228 (depsipeptide): a HDAC inhibitor with pleiotropic antitumor activities

verfasst von: Panagiotis A. Konstantinopoulos, Gerasimos P. Vandoros, Athanasios G. Papavassiliou

Erschienen in: Cancer Chemotherapy and Pharmacology | Ausgabe 5/2006

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Abstract

Purpose: The fundamental role of epigenetic events in carcinogenesis has resulted in the evolution of epigenetic targeting as a new paradigm in anticancer therapeutics. Aberrant histone deacetylase (HDAC) activity has been documented in many human malignancies resulting in the repression of tumor suppressor genes and promotion of tumorigenesis. FK228, also known as depsipeptide, is a novel, natural, bicyclic tetrapeptide with significant antitumor properties which are mostly mediated by inhibition of HDACs. Results: FK228 induces the expression of genes linked to the inhibition of cell growth, induction of cell differentiation, promotion of apoptotic cell death and inhibition of angiogenesis. Conclusion: Its multitargeting properties, its ability to act on non-histone targets, its clinical activity and its acceptable side-effect profile render FK228 a very promising novel anticancer agent.

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Titel: FK228 (depsipeptide): a HDAC inhibitor with pleiotropic antitumor activities
verfasst von: Panagiotis A. Konstantinopoulos
Gerasimos P. Vandoros
Athanasios G. Papavassiliou
Publikationsdatum: 01.11.2006
Verlag: Springer-Verlag
Erschienen in: Cancer Chemotherapy and Pharmacology / Ausgabe 5/2006
Print ISSN: 0344-5704
Elektronische ISSN: 1432-0843
DOI: https://doi.org/10.1007/s00280-005-0182-5

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Springer Medizin

FK228 (depsipeptide): a HDAC inhibitor with pleiotropic antitumor activities

Abstract

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Springer Medizin

Abstract

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