The central dogma of the action of current anticancer drugs is that the drug tightly binds to its molecular target for inhibition. The reliance on tight ligand-receptor binding, however, is also the major root of drug resistance in cancer therapy. In this talk, we highlight enzyme-instructed self-assembly (EISA)—the integration of enzymatic transformation and molecular self-assembly—as a multi-step process for the development of cancer therapy. Using apoptosis as an example, we illustrate that the combination of enzymatic transformation and self-assembly, in fact, is an inherent feature of apoptosis. After the introduction of EISA of small molecules in the context of supramolecular hydrogelation, we describe several key studies to underscore the promises of EISA for developing cancer therapy. Particularly, we will discuss that EISA allows one to develop approaches to target “undruggable” targets or “untargetable” features of cancer cells and provides the opportunity for simultaneously interacting with multiple targets. We will highlight developing anticancer medicine that inhibit multiple hallmark capabilities of cancer without inducing drug resistance.

Enzyme-instructed self-assembly in cellular milieu: Bioinspired targeting of cancer cells without drug resistance

253rd National Meeting (2017)

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