definitely bind to topoisomerase I and stabilize DNA-topoisomerase I cleavable complex.
Cheng used a chemical linker to attach the camptothecins
to the polymer.
Prior to this discovery, most cancer drugs have targeted binding to the major groove in DNA leading to the successful introduction of several new classes of anticancer drugs, including topoisomerase inhibitors such as camptothecins
An up-to-date summary is offered including a discussion of topoisomerase I, along with an analysis of animal models for defining the anticancer potential of camptothecins
, and issues of camptothecin
Karenitecin is in the drug class known as camptothecins
and has been designed to avoid problems with oral bioavailability, unfavorable metabolism, toxicity and drug resistance that have been associated with other camptothecins
stop cells from completing mitosis, specifically in the S-phase.
Topoisomerase inhibitors that inhibit either topoisomerase I or II are used to treat a number of different tumor types: camptothecins
(topoisomerase I inhibitors) for colorectal cancer; anthracyclines (topoisomerase II inhibitors) for breast, ovarian, bladder cancer and Non Hodgkin's Lymphoma; etoposide (topoisomerase II inhibitor) for lung cancer.