Design of a Hyperpolarized Molecular Probe for Detection of Aminopeptidase N Activity

Aminopeptidase N (APN) is an important enzyme that is involved in tumor angiogenesis. Detection of APN activity can thus lead to early diagnosis and elucidation of tumor development. Although some molecular probes for APN have been developed, the detection of APN activity in opaque biological samples remains a challenge. To this end, we designed a hyperpolarized NMR probe [1‐13C]Ala‐NH2 which satisfies the prerequisites for APN detection, namely, sufficient retention of the hyperpolarized state, a high reactivity to APN, and an APN‐induced chemical shift change. The [1‐13C]Ala‐NH2 probe allowed sensitive detection of APN activity using 13C NMR spectroscopy. Rational design: A hyperpolarized NMR probe [1‐13C]Ala‐NH2 was designed. The probe satisfies the prerequisites for aminopeptidase N (APN) detection, namely, sufficient retention of the hyperpolarized state, high reactivity towards APN, and an APN‐induced chemical shift change. The probe allowed sensitive detection of APN activity using 13C NMR spectroscopy.