Enzyme-catalyzed therapeutic agent (ECTA) design: activation of the antitumor ECTA compound NB1011 by thymidylate synthase 1 1 Abbreviations: 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, N 5,N 10-methylene tetrahydrofolate; TBDMS, tert-butyldimethylsilyl; and TS, thymidylate synthase (EC 2.1.1.45).
Titel:
Enzyme-catalyzed therapeutic agent (ECTA) design: activation of the antitumor ECTA compound NB1011 by thymidylate synthase 1 1 Abbreviations: 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, N 5,N 10-methylene tetrahydrofolate; TBDMS, tert-butyldimethylsilyl; and TS, thymidylate synthase (EC 2.1.1.45).
Auteur:
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