camptothecins

camp·to·the·cins

(kamp'tō-thek'inz),
1. Antitumor agents acting as topoisomerase inhibitors; include irinotecan and topotecan.
2. A semisynthetic drug derived from camptothecin.

camptothecins

A new class of cytotoxic anticancer drugs based on the plant alkaloid camptothecin found in the wood, bark and fruit of the tree Camptotheca acuminata . Camptopthecins attack the enzyme TOPOISOMERASE. The class includes the drugs TOPOTECAN and IRINOTECAN both of which are showing promising results in the treatment of small cell lung cancer and ovarian cancer.
References in periodicals archive ?
Camptothecins 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 [50].
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 [34], camptothecins [38, 40], and phenothiazine drugs [41] as well as the aromatic mutagen ethidium bromide [42]and aromatic neurotoxin tetrahydropyridine [43].
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 and anthracyclines.
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 resistance.
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.
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.