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PROTACs As Potential Therapeutic Agents for Cancer Drug Resistance.

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Cancer drug resistance becomes the major challenging problem facing current clinical treatment faced by different kinds of therapies. Proteolysis targeting chimeras (PROTACs) as a novel and powerful strategy has attracted… Click to show full abstract

Cancer drug resistance becomes the major challenging problem facing current clinical treatment faced by different kinds of therapies. Proteolysis targeting chimeras (PROTACs) as a novel and powerful strategy has attracted great attentions both from academia and industry for their sensitivity to drug-resistant targets relying on their unique characteristics compared to traditional inhibitors. PROTACs exert their function by degrading the target protein instead of inhibiting targets. Thus, different kinds of resistance could be conquered by PROTACs such as target mutation or overexpression. Various resistant targets have been overcome by PROTACs including AR, ER, BTK, BET, and BCR-ABL. Though PROTACs have achieved some significant advances in settling the drug resistance, more cases are needed to prove the efficiency of PROTACs in addressing resistance hurdle in near future.

Keywords: drug resistance; drug; resistance; protacs; cancer drug

Journal Title: Biochemistry
Year Published: 2019

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