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© 2020 WILEY-VCH Verlag GmbH Co. KGaA, Weinheim.Severe side effects and poor therapeutic efficacy are the main drawbacks of current anticancer drugs. These problems can be mitigated by targeting, but the targeting efficacy of current drugs is poor and urgently needs improvement. Taking this into consideration, this review first summarizes the current targeting strategies for cancer therapy in terms of cancer tissue and organelles. Then, we analyse the systematic targeting of anticancer drugs and conclude that a typical journey for