FOLH1 and neoplasm: In view of the unique carboxypeptidase activity and restricted expression of the PSMA, we accomplished the synthesis of several PSMA-activated camptothecin pentapeptide prodrugs CPT-HT-J-ZLn, by introducing an oriented oligopeptide HT-J (Glu*Glu*Glu*Asp-Glu) (“*” mean the γ-glutamyl linkage; “-” mean the α-glutamyl linkage) to the 20-OH of CPT via carbonate linkers with different lengths, in order to improve their tumor targeting, stability, and aqueous solubility.