NB1011
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Thymidylate Synthase Inhibitor -> NB1011
NB1011 Definition
A small molecule phosphoramidate derivative of (E)-5-(2-bromovinyl)-2'-deoxyuridine with potential antineoplastic activity. Selectively active against tumor cells expressing high levels of thymidylate synthase (TS), BVdU pronucleotide analogue NB1011 is converted intracellularly by TS to bromovinyldeoxyuridine monophosphate (BVdUMP) which competes with the natural substrate, deoxyuridine monophosphate, for binding to TS. Unlike TS inhibitors, this agent is a reversible substrate for TS catalysis. Thus, TS retains activity and converts BVdUMP into cytotoxic metabolites. As key enzyme in the de novo synthesis of dTMP, TS is an enzyme critical to DNA biosynthesis and is overexpressed in many solid tumors.
NB1011 Synonyms
Brivudine Phosphoramidate, (E)-5-(2-Bromovinyl)-2'-deoxy-5'-uridyl Phenyl L-methoxyalaninylphosphoramidate, BVDU Prodrug, BVdU Phosphoramidate, NB101.1, NB1011, Thymectacin
Terms in NB1011 category
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