By Val R. Adams

A severe overview our present knowing of camptothecins, their shortcomings, and of the probabilities for making improvements to their medical functionality. The authors speak about new camptothecin analog improvement, drug supply matters for optimizing their anticancer task, and their power use in numerous diverse cancers. extra chapters describe what's identified 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 strength of camptothecins, and the query of camptothecin resistance.

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120. Pickart CM. 1997 Targeting of substrates to the 26S proteasome. FASEB J 11:1055–1066. 121. Hershko A, Ciechanover A, Varshavsky A. 2000 The ubiquitin system. Nat Med 6:1073–1081. 122. Melchior F. 2000 Sumo nonclassical ubiquitin. Annu Rev Cell Dev Biol 16: 591–626. 123. Schwienhorst I, Johnson ES, Dohmen RJ. 2000 SUMO conjugation and deconjugation. Mol Gen Genet 263:771–786. 124. Yeh ET, Gong L, Kamitani T. 2000 Ubiquitin-like proteins: new wines in new bottles. Gene 248:1–14. 125. Kretz-Remy C, Tanguay RM.

018 µM fagaronine, respectively. Reprinted with permission from Chem Res Toxicol 1993;6:813–818. Copyright 1993 American Chemical Society. aging that only those benzophenanthridine alkaloids found to stabilize the covalent binary complex formed from TOP-I and DNA in vitro had been identified in earlier studies as agents having antitumor activity in experimental animal models. 3. OTHER THERAPEUTIC STRATEGIES INVOLVING TOP-I Although the focus of activity in developing inhibitors of TOP-I function has involved compounds that stabilize the enzyme-DNA covalent binary complex, other strategies for enzyme inhibition can be readily envisioned.

The hydroxyl of Thr718 makes a hydrogen bond contact with the nonbridging phosphodiester oxygen of guanosine at position +1 of the cleaved strand (+1G). Arg364 makes a hydrogen bond contact with N3 of adenosine at position –1 of the uncleaved strand (–1A). Lys532 makes a hydrogen bond with the oxygen of thymidine at position –1 (–1T). Lys374 and the main chain nitrogens of 362 and 363 make hydrogen bond contacts Chapter 2 / Topoisomerase–DNA–Drug X-Ray Structure 27 with the nonbridging phosphodiester of the uncleaved strand (0P).

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