Structural Biochemistry/Amsacrine

Amsacrine Description 300px|thumb|Amsacrine C21H19N3O3S Amsacrine is a potent intercalating antineoplastic agent. It is effective in the treatment of adult acute leukemias and malignant lymphomas, but not effective in the treatment of solid tumors. It is frequently used in combination with other antineoplastic agents in chemotherapy. Usage Injectable (Intravenous Route) Side Effects Black stools cough or hoarseness fever or chills painful or difficult urination pinpoint red spots on skin sores, ulcers, or white spots on lips, tongue, or inside mouth Abdominal pain or tenderness blurred vision fast, pounding, or irregular heartbeat or pulse palpitations seizures yellow eyes or skin Mechanism of Actions 300px|thumb|Inhibition of Topisomerase 300px|thumb|Complex of DNA-Topoisomerase is destroyed The DNA is wound around basic proteins called histones and is tighly coiled or supercoiled. Sequences of DNA must be unwound or relaxed before they can be processed by DNA processing enzymes. Topoisomerase II or TopoII is one enzyme that can process DNA. TopoII temporarily breaks the DNA strand and allows both ends to freely rotate within the enzyme. This allows the DNA to unwind. After the DNA is processed, the enzyme then reconnects the two ends. Amsacrine kills cancerous cells by inhibiting the Topo II enzyme. It stabilizes the enzyme with the broken DNA strand complex long enough for the enzyme-DNA complex to break down completely. When the DNA is destroyed, the cancerous cells will be eventually killed. References "Amsacrine." Scott Hamilton CARES Initiative. N.p.. Web. 07 Dec 2012. <http://chemocare.com/chemotherapy/drug-info/Amsacrine.aspx> Grove, WR, CL Fortner, and PH Wiernik. "Clinical Pharmacy." Clinical Pharmacy. Jul-Aug. (1982): 320-26. Print.