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.
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 humanmalignancies 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.
Authors: Angelika Danielsson; Helena Dzojic; Victoria Rashkova; Wing-Shing Cheng; Magnus Essand Journal: PLoS One Date: 2011-02-17 Impact factor: 3.240
Authors: Simon J Cooper; Christina A von Roemeling; Kylie H Kang; Laura A Marlow; Stefan K Grebe; Michael E Menefee; Han W Tun; Gerardo Colon-Otero; Edith A Perez; John A Copland Journal: Mol Cancer Ther Date: 2012-07-23 Impact factor: 6.261
Authors: Wei Zhang; Michael Peyton; Yang Xie; Junichi Soh; John D Minna; Adi F Gazdar; Eugene P Frenkel Journal: J Thorac Oncol Date: 2009-02 Impact factor: 15.609