Precision medicine is in an urgent need for public healthcare. Among the past
several decades, the flourishing development in nanotechnology significantly advances
the realization of precision nanomedicine. Comparing to well-documented nanoparticlebased
strategy, in this review, we focus on the strategy using enzyme instructed selfassembly
(EISA) in biological milieu for theranostics purpose. In principle, the design of
small molecules for EISA requires two aspects: (1) the substrate of enzyme of interest;
and (2) self-assembly potency after enzymatic conversion. This strategy has shown its irreplaceable
advantages in nanomedicne, specifically for cancer treatments and Vaccine
Adjuvants. Interestingly, all the reported examples rely on only one kind of enzymehydrolase.
Therefore, we envision that the application of EISA strategy just begins and
will lead to a new paradigm in nanomedicine.
