Involvement of amino acids 361 to 364 of human topoisomerase I in camptothecin resistance and enzyme catalysis

Camptothecins are antineoplastic drugs that specifically target the enzyme DNA topoisomerase I. Prior work has identified a human topoisomerase I mutation, F361S, that confers resistance to camptothecin. We now demonstrate that substitutions in the 361–364 region can alter DNA cleavage/ligation by t...

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Veröffentlicht in:	Biochemical pharmacology 1997-04, Vol.53 (7), p.1019-1027
Hauptverfasser:	Li, Xi-Guang, Paul, Haluska, Yaw-Huei, Hsiang, Ajit, K.Bharti, Donald, W.Kufe, Leroy, F.Liu, Eric, H.Rubin
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic agents Antineoplastic Agents, Phytogenic - pharmacology Binding Sites Biological and medical sciences camptothecin Camptothecin - pharmacology Catalysis DNA - metabolism DNA binding DNA cleavage DNA Damage DNA Topoisomerases, Type I - biosynthesis DNA Topoisomerases, Type I - genetics DNA Topoisomerases, Type I - metabolism drug resistance Drug Resistance - genetics enzyme mutations General aspects Genetic Vectors Humans Medical sciences Mutation Pharmacology. Drug treatments topoisomerase
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