By Val R. Adams
A severe evaluation our present figuring out of camptothecins, their shortcomings, and of the probabilities for bettering their medical functionality. The authors speak about new camptothecin analog improvement, drug supply concerns for optimizing their anticancer task, and their capability use in various various cancers. extra chapters describe what's recognized in regards to 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 types in defining the anticancer capability of camptothecins, and the query of camptothecin resistance.
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Additional info for Camptothecins in Cancer Therapy (Cancer Drug Discovery and Development)
Fig. 4. Transformations of ring E in camptothecin. 43 44 Hecht Fig. 5. Structure of homocamptothecin (11). binary complex formed between the enzyme and DNA. The lactone (E-) ring does not undergo solvolysis readily, and ring opening is not readily reversed under physiological conditions. It is not clear to what extent the absence of reversible ring opening may contribute to the antitumor activity of the homocamptothecins, but derivatives have been prepared that exhibit strong antiproliferative activity (17,18).
Tables 1 and 3). However, ligation of inhibition of the gapped DNA substituted was effected only by CPT itself and by 20-deoxy CPT (21), the latter of which failed to inhibit any of the other ligation reactions. Thus it seems clear that differential inhibition of individual TOP-I-mediated transformations should be possible. 54 Hecht Table 3 Inhibition of the TOP-I-Mediated Ligation of Nicked and Gapped DNA Oligonucleotides by CPTs Extent of inhibition ligation (%) CPT analoga Nicked substrateb 1 21 22 23 24 62 5 21 37 32 a50 Gapped substrate 47 13 0 0 0 μM concentration.
Pourquier P, Pommier Y. 2001 Topoisomerase I-mediated DNA damage. Adv Cancer Res 80:189–216. 4. Wall ME, et al. The isolation and structure of camptothecin, a novel alkaloidal leukemia and tumor inhibitor from Camptotheca acuminata. J Am Chem Soc 1966;88:3888–3890. 5. Hsiang YH, Hertzberg, R, Hecht S, Liu LF. 1985 Camptothecin induces proteinlinked DNA breaks via mammalian DNA topoisomerase I. J Biol Chem 260:14873–14878. Chapter 2 / Topoisomerase–DNA–Drug X-Ray Structure 37 6. Nitiss JL, Wang JC.