With the rising global cancer burden, the dependency on chemotherapy also rises along with the complication of chemoresistance development. Studies on multi-drug resistant proteins provide a wide range of regulators, although the exact mechanism is not yet clearly understood. Epigenetic modifications play a vital role in the regulation of cellular processes and also in determining the efficacy of cancer therapy by modulating resistance development and tumor progression. Of the various epigenetic modifications, histone acetylation/deacetylation and DNA methylation are currently given more focus in evaluating their role in resistance development to doxorubicin. This chapter highlights the various studies conducted on the regulation of doxorubicin (dox) resistance based on these epigenetic modifications and the clinical trials conducted in evaluating its effectiveness as a potential combinational therapy.
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