Targeting prostate cancer cells with a multivalent PSMA inhibitor-guided streptavidin conjugate

A series of spacer-varied biotinylated PSMA inhibitors were synthesized and evaluated, which exhibited spacer length-dependent effects on inhibitory potency, mode of inhibition. Moreover, only one of them can be used to form a complex with Cy5-streptavidin for fluorescence imaging of prostate cancer cells.