What is the target of camptothecin?
Camptothecins selectively target topoisomerase I (Top1) by trapping the catalytic intermediate of the Top1-DNA reaction, the cleavage complex. Hence, camptothecins represent a paradigm for targeting macromolecular interactions.
What is the function of camptothecin?
Camptothecin, an quinolone alkaloid, is used as a chemotherapeutic agent in the treatment of leukemia (Jones et al., 1997). Camptothecin complexes with type I DNA topoisomerase inhibiting both cleavage and religation reactions of DNA replication thus arresting growth of L.
What is the mechanism of camptothecins?
The primary mechanism of cell killing by CPT is S-phase-specific killing through potentially lethal collisions between advancing replication forks and topo-I cleavable complexes.
What class of drug is camptothecins?
Drug type: Irinotecan is an anti-cancer ("antineoplastic" or "cytotoxic") chemotherapy drug. This medication is classified as a "plant alkaloid" and "topoisomerase I inhibitor." (For more detail, see "How this drug works" section below).
What is the use of camptothecin?
The camptothecin topoisomerase I-targeting agents are new class of antitumor drugs with demonstrated clinical activity in human malignancies, such as colorectal cancer and ovarian cancer.
What is the source of camptothecin?
Camptothecin (CPT) (Figure 1A) is a pentacyclic alkaloid that was first isolated from stem wood of Camptotheca acuminata by botanists working in the USDA's Plant Introduction Division in the mid-1950s [1]. Camptotheca acuminata is a tree native to China and its bark is a recognized Chinese traditional medicine.
What is the biological source of camptothecin?
Camptothecin is an alkaloid first isolated from the stem wood of the tree Camptotheca acuminata (Nyssaceae), and has potent antitumor activity. Camptothecin acts by inhibiting the enzyme topoisomerase-I, which is responsible for relaxing supercoils that are generated during transcription and DNA replication.