NanoTAC is derived from the supramolecular self-assembly of drug conjugates composed of purposefully tailored components, including (i) a PROTAC constructed from the HK2-selective inhibitor lonidamine,44,45 a lysine residue serving as a four-atom linker46 and the E3 ligase VHL-recruiting peptide ALAPYIP;47–49 (ii) KRR, a substrate peptide for the cancer biomarker cathepsin B;50 and (iii) the clinically approved photosensitizer verteporfin (VPF), marketed under the trade name Visudyne®. Here, CTSB is linked to cancer.