Despite the enormous number of anticancer drugs presently available in the clinic, treatment failure due to drug
resistance is very frequent. The identification of mechanisms of resistance to different drugs is necessary, in order to identify
ways to prevent and circumvent such resistance. Indeed, the identification of novel therapeutic targets to overcome cancer
drug resistance remains one of the major challenges in drug discovery and development. The methods employed to
identify drug resistance mechanisms and novel therapeutic targets depend greatly on the establishment of cancer drug
resistant cell lines. The establishment of such drug resistant cell lines is laborious and time-consuming and various
different approaches have been described. This manuscript reviews the methodologies that have been used to create
cancer drug resistant cell lines and to identify their mechanisms of resistance. In addition, this review highlights the most
frequent drug resistance mechanisms found in cancer cells.
Keywords: Acquired drug resistance, anticancer drugs, cancer drug resistance, drug resistant cancer cell lines, isogenic cell
lines, mechanisms of drug resistance, multidrug resistance.
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