NMR Solution Structure of the Antitumor Compound PT523 and NADPH in the Ternary Complex with Human Dihydrofolate Reductase

The antitumor compound PT523 [N α-(4-amino-4-deoxypteroyl)-N δ-hemiphthaloyl-l-ornithine] was found to have an inhibition constant (K i) of 0.35 ± 0.10 pM against human dihydrofolate reductase (hDHFR), 15-fold lower than that of the classical antifolate drug methotrexate (MTX). The structure of PT52...

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Veröffentlicht in:	Biochemistry (Easton) 1997-04, Vol.36 (15), p.4399-4411
Hauptverfasser:	Johnson, Jason M, Meiering, Elizabeth M, Wright, Joel E, Pardo, Jorge, Rosowsky, Andre, Wagner, Gerhard
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic Agents - chemistry Binding Sites Crystallography, X-Ray Folic Acid Antagonists - chemistry Humans Kinetics Ligands Magnetic Resonance Spectroscopy Methotrexate - chemistry NADP - chemistry Ornithine - analogs & derivatives Ornithine - chemistry Protein Conformation Pterins - chemistry Tetrahydrofolate Dehydrogenase - chemistry
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