Camptothecins in Cancer Therapy (Cancer Drug Discovery and by Val R. Adams

By Val R. Adams

A severe evaluate our present realizing of camptothecins, their shortcomings, and of the chances for bettering their scientific functionality. The authors talk about new camptothecin analog improvement, drug supply concerns for optimizing their anticancer task, and their capability use in various assorted cancers. extra chapters describe what's identified concerning the biochemistry, the pharmacology, and the chemistry of the camptothecins, together with the mechanism of topoisomerase and the way camptothecins poison this enzyme, using animal versions in defining the anticancer strength of camptothecins, and the query of camptothecin resistance.

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The transformations involved in the use of nicked and gapped DNA oligonucleotide substrates are shown in Fig. 12. Also illustrated in this figure is TOP-I-mediated ligation of the nicked substrate. As shown in Fig. 12, ligation could occur across one- or three-nucleotide gaps produced by the enzyme and was influenced by the complementarity of the nucleotide at the 5v-end of the acceptor oligonucleotide to the nucleotide downstream from the cleavage site on the nonscissile strand. The model duplexes were subsequently used to test the inhibitory properties of CPT analogues, most of which had been shown to stabilize the covalent TOP-I–DNA binary complex formed from B-DNA duplexes (8,56).

Tamura H, Kohchi C, Yamada R, et al. 1991 Molecular cloning of a cDNA of a camptothecin-resistant human DNA topoisomerase I and identification of mutation sites. Nucleic Acids Res 19:69–75. 19. Fertala J, Vance JR, Pourquier P, Pommier Y, Bjornsti M-A. 2000 Substitutions of Ans-726 in the active site of yeast DNA topoisomerase I define novel mechanisms of stabilizing the covalent enzyme-DNA intermediate. J Biol Chem 275:15246–15253. 20. Jaxel C, Kohn KW, Wani MC, Wall ME, Pommier Y. 1989 Structure-activity study of the actions of camptothecin derivatives on mammalian topoisomerase I: evidence for a specific receptor site and a relation to antitumor activity.

Ann N Y Acad Sci 922:306–308. 141. Desai SD, Li TK, Rodriguez-Bauman A, Rubin E, Liu LF. 2001 Ubiquitin/26S proteasome-mediated degradation of topoisomerase I as a resistance mechanism to camptothecin in tumor cells. Cancer Res 61:5926–5932. 142. Desai SD, Zhang H, Rodriguez-Bauman A, Yang JM, Wu X, Gounder MK, et al. 2003 Transcription-dependent degradation of topoisomerase I-DNA covalent complexes. Mol Cell Biol 23:2341–2350. 143. Eder JP, Rubin E, Stone R, Bryant M, Xi G-X, Supko J, et al. 1996 Trials of 9amino-20(S)-camptothecin in Boston.

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