By Val R. Adams
A severe evaluation our present realizing of camptothecins, their shortcomings, and of the probabilities for making improvements to their medical functionality. The authors talk about new camptothecin analog improvement, drug supply concerns for optimizing their anticancer job, and their power use in numerous diversified 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 power of camptothecins, and the query of camptothecin resistance.
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Additional resources for Camptothecins in Cancer Therapy
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Topotecan intercalates the cleaved DNA and is tightly sandwiched between the upstream and downstream base pairs. 34 Burgin et al. binding events would have to be rendered ineffective before a significant effect on relaxation could be observed. It logically follows that large concentrations of inhibitors will be required to observe an effect on plasmid relaxation. Thus it has been a mystery how camptothecins stabilize the nicked complex but prevent DNA relaxation, because nicked DNA should be able to rotate and allow DNA relaxation (30).
139. Liu LF, Desai SD, Li TK, Mao Y, Sun M, Sim SP. 2000 Mechanism of action of camptothecin. Ann N Y Acad Sci 922:1–10. 140. Desai SD, Mao Y, Sun M, Li TK, Wu J, Liu LF. 2000 Ubiquitin, SUMO-1 and UCRP in camptothecin sensitivity and resistance. 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.
Camptothecins in Cancer Therapy by Val R. Adams