Enzyme-catalyzed therapeutic agent (ECTA) design: activation of the antitumor ECTA compound NB1011 by thymidylate synthase11Abbreviations: BVdU, (E)-5-(2-bromovinyl)-2′-deoxyuridine; BVdUMP, (E)-5-(2-bromovinyl)-2′-deoxyuridine 5′-monophosphate; NB1011, (E)-5-(2-bromovinyl)-2′-deoxy-5′-uridyl phenyl l-methoxyalaninylphosphoramidate; COSY, correlated spectroscopy; DCI, direct current ionization; DMF, N,N-dimethylformamide; dUMP, 2′-deoxyuridine 5′-monophosphate; ECTA, enzyme-catalyzed therapeutic agent; 5-FU, 5-fluorouracil; 5-FdUMP, 5-fluoro-2′-deoxyuridine 5′-monophosphate; RFU, relative fluorescence units; THF, N5,N10-methylene tetrahydrofolate; TBDMS, tert-butyldimethylsilyl; and TS, thymidylate synthase (EC 2.1.1.45).

Author:

Lackey David B.,Groziak Michael P.,Sergeeva Maria,Beryt Malgorzata,Boyer Christopher,Stroud Robert M.,Sayre Peter,Park John W.,Johnston Patrick,Slamon Dennis,Shepard H.Michael,Pegram Mark

Publisher

Elsevier BV

Subject

Pharmacology,Biochemistry

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