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Evolutionary trace analysis of eukaryotic DNA topoisomerase I superfamily:Identification of novel antitumor drug binding site

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Science China(Life Sciences) 2005年第4期48卷 375-384页

作者： SONG Yunlong QI Yunpeng ZHANG Wannian SHENG Chunquan ZHANG Min YAO Jianzhong YU Jianxin MIAO Zhenyuan ZHOU Youjun ZHU Ju L(U)Jiaguo Department of Medicinal Chemistry School of PharmacySecond Military Medical UniversityShanghai 200433China

The studies of novel inhibitors of DNA topoisomerase I(Topo I)have already be-come very promising in cancer *** the new drug-binding residues is playing an important role in the design and optimization of Topo I *** designed com-pounds may have novel scaffolds,thus will be helpful to overcome the toxicities of current camptothecin(CPT)drugs.and may provide a solution to cross resistance with these ***-tiple sequence alignments were performed on eukaryotic DNA topoisomerase I superfamily and thus the evolutionary tree was *** Evolutionary Trace method was applied to iden-tify functionally important residues of human Topo *** has been demonstrated that class-specific hydrophobic residues Ala351,Met428,Pro431 are located around the 7,9-position of CPT,indi-cating suitable substitution of hydrophobic group on CPT will increase antitumor *** conservative residue Lys436 in the superfamily is of particular interest and new CPT derivatives designed based on this residue may greatly increase water solubility of such *** has also been demonstrated that the residues Asn352 and Arg364 were conservative in the superfamily,whose mutation will render CPT *** our molecular docking studies demonstrated they did not make any direct interaction with CPT,they are important drug-binding site residues for future design of novel non-camptothecin lead *** work provided a strong basis for the design and synthesis of novel highly potent CPT derivatives and virtual screening for novel lead compounds.

关键词： topoisomerase I binding site evolutionary trace camptothecin antineoplastic drugs.

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