DUPA, belongs to a class of glutamate ureas, is used as the targeting moiety in drug conjugate to selectively deliver cytotoxic drugs to prostate cancer cells[1][2].
DUPA is used as the targeting moiety to actively deliver Docetaxel (DTX) for treatment of prostate-specific membrane antigen (PSMA) expressing prostate cancer[1]. The DUPA-indenoisoquinoline conjugate exhibits an IC50 in the low nanomolar range in 22RV1 cell cultures[2].
The DUPA-indenoisoquinoline conjugate induces a complete cessation of tumor growth with no toxicity, as determined by loss of body weight and death of treated mice[2].
[1]. Peng ZH, et al. Spacer length impacts the efficacy of targeted docetaxel conjugates in prostate-specific membrane antigen expressing prostate cancer. J Drug Target. 2013 Dec;21(10):968-80. [2]. Roy J, et al. DUPA conjugation of a cytotoxic indenoisoquinoline topoisomerase I inhibitor for selective prostate cancer cell targeting. J Med Chem. 2015 Apr 9;58(7):3094-103.