DUPA(OtBu)-OH

DUPA(OtBu)-OH is a DUPA precursor. DUPA is used as the targeting moiety to actively deliver Docetaxel (DTX) for treatment of Prostate-Specific Membrane Antigen (PSMA) expressing prostate cancer.

Signaling Pathways >> Others >> Others

Research Areas >> Cancer

DUPA(OtBu)-OH (DUPA precursor 17) is a 2-[3-(1,3-dicarboxypropyl)ureido]pentanedioic acid (DUPA) reagent[1]. The targeting ligand DUPA enhances the transport capability and selectivity of Paclitaxel (PTX) to tumor cells via prostate-specific membrane antigen (PSMA) mediated endocytosis. Besides, DUPA is conjugated with PTX via a disulfide bond, which facilitates the rapid and differential drug release in tumor cells[2].

DUPA-targeted Docetaxel (DTX) conjugate with longer spacer has no toxicity in major organs of treated mice[3].

[1]. Roy J, et al. DUPA conjugation of a cytotoxic indenoisoquinoline topoisomerase I inhibitor for selectiveprostate cancer cell targeting. J Med Chem. 2015 Apr 9;58(7):3094-103.

[2]. Lv Q, et al. Prostate-Specific Membrane Antigen Targeted Therapy of Prostate Cancer Using a DUPA-Paclitaxel Conjugate. Mol Pharm. 2018 May 7;15(5):1842-1852.

[3]. Peng ZH, et al. Spacer length impacts the efficacy of targeted docetaxel conjugates in prostate-specificmembrane antigen expressing prostate cancer. J Drug Target. 2013 Dec;21(10):968-80.

Captisol | Cyclosporin A | H2DCFDA | 0MPTP hydrochloride | GW4869 | Etomoxir | TD139 | Mitoquinone mesylate | GSK2795039 | JC-1 | BAPTA-AM | AP 20187 | Setanaxib (GKT137831) | D-Luciferin | Crotaline