1. Actinomycin D (AMD) is an anti-cancer drug, which binds to DNA and inhibits RNA synthesis.
2. We have crystallized AMD with a short DNA and proved the AMD binding mode (i.e., intercalation).
3. Structure of DNA-AMD complex determined by X-ray diffraction method.
4. On the basis of the structures, we designed modification and synthesized two potential AMD analogues, N8-AMD and F8-AMD. F8-AMD shows a strong selective anti-leukemia activity.
6. Structure of synthetic drug F8-AMD bound to DNA
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