Camptotheca Inhibition of the (irinotecan and acuminata nuclear protein topotecan) topoisomerase I.
Pommier, "Molecular and biological determinants of the cytotoxic actions of camptothecins
: perspective for the development of new topoisomerase I inhibitors," Annals of the New York Academy of Sciences, vol.
P-glycoprotein, identifies and ousts about 50% of all chemotherapeutic drugs including anthracyclines, vinca alkaloids, taxanes, epidophyllotoxins, mitomycins and camptothecins
out of the plasma membrane .
anthracyclines, Vinca alkaloids, taxanes, camptothecins
etc.), but also valuable lead compounds for the development of novel targeted chemotherapy approaches.
To date, it is known that, on simultaneous addition or right after the main drug, CAF diminishes the toxicity of the antitumour antibiotics doxorubicin [30, 31, 33, 37-39], mitoxantrone [32, 33, 37, 39], ellipticine [33, 38], amsacrine , camptothecins
[38, 40], and phenothiazine drugs  as well as the aromatic mutagen ethidium bromide and aromatic neurotoxin tetrahydropyridine .
Subsequently, the break is sealed and the linkage number is changed by 1, and permit essential cellular process (i.e DNA replication, recombination,repair and transcription )to occur.The camptothecins
definitely bind to topoisomerase I and stabilize DNA-topoisomerase I cleavable complex.
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
: a review of their chemotherapeutic potential.
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.
Circumvention of breast cancer resistance protein (BCRP)-mediated resistance to camptothecins
in vitro using non-substrate drugs or the BCRP inhibitor GF120918.