Tretazicar
Created:
4/18/17
Submitted:
10/6/26
Published:
10/7/26
89105-bas-color-print_cautionAtoms shown as ball-and-stick (geometry appears faceted on screen; apply smooth normals in Blender or similar to improve visualization; generally smooth when 3D printed) with standard colors. 3D printable, with caution, using certain 3D printers.
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Description
Tretazicar is a prodrug of a bifunctional alkylating, dinitrobenzamide derivative with antineoplastic activity. Tretazicar can be activated by the human enzyme quinone oxidoreductase 2 (NQO2) in the presence of the cosubstrate caricotamide, an analogue of the natural cosubstrate dihydronicotinamide riboside (NRH), which acts as an electron donor. The resulting active, but short-lived metabolite, dinitrobenzamide, leads to DNA replication inhibition and the induction of apoptosis in NQO2 expressing cancer cells. Due to the lack of the natural cosubstrate NRH, NQO2 expression is normally latent but is upregulated in certain types of tumor cells.
