Inhibition TOP1

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the briefly attached, covalently bonded top1-dna structure @ 3 end of cleaved dna single strand called top1-dna cleavage complex, or top1cc. top1cc specific target of top1 inhibitors. 1 of first inhibitors shown target top1 irinotecan. irinotecan analogue of cytotoxic natural alkaloid camptothecin, obtained chinese tree camptotheca acuminata. irinotecan effective through metabolic product sn-38. irinotecan , sn-38 act trapping subset of top1-dna cleavage complexes, guanine +1 in dna sequence. 1 irinotecan or sn-38 molecule stacks against base pairs flanking topoisomerase-induced cleavage site , poisons (inactivates) top1 enzyme. article camptothecin lists other analogues of camptothecin , article topoisomerase inhibitor lists other compounds inhibit top1.








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