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This is by far the most-accepted mechanism to explain the action of anthracyclines as topoisomerase-II mediated toxicity is evident at clinically relevant drug concentrations. [ 19 ] [ 26 ] Topoisomerase-II is an enzyme that creates temporary double-stranded DNA (dsDNA) breaks and reseals them after managing torsion of DNA supercoils .
The calicheamicins are a class of enediyne antitumor antibiotics derived from the bacterium Micromonospora echinospora, [1] with calicheamicin γ1 being the most notable. [2] It was isolated originally in the mid-1980s from the chalky soil, or "caliche pits", located in Kerrville, Texas. The sample was collected by a scientist working for ...
Enediynes are most notable for their limited use as antitumor antibiotics (known as enediyne anticancer antibiotics). [1] They are efficient at inducing apoptosis in cells, but cannot differentiate cancerous cells from healthy cells. Consequently, research is being conducted to increase the specificity of enediyne toxicity.
Bizelesin is antineoplastic antibiotic which binds to the minor groove of DNA and induces interstrand cross-linking of DNA, thereby inhibiting DNA replication and RNA synthesis. Bizelesin also enhances p53 and p21 induction and triggers G2/M cell-cycle arrest, resulting in cell senescence without apoptosis.
The following is a list of antibiotics. ... Experimental, as antitumor antibiotics: ... liver toxicity. [7] Spiramycin: Rovamycine:
These antibiotics act via permeabilising the bacterial cell membrane, or neutralising is toxicity to cause cell death in bacteria. [5] Its predominant clinical use is as a topical medication, however successful laboratory trials are limited. A common polypeptide antibiotic is bacitracin, derived from the bacteria; Bacillus subtilis. [6]
Neothramycin shows weak antimicrobial activity compared to other pyrrolo(1,4)benzodiazepines. It also shows lower toxicity in mice. Neothramycin has been shown to exhibit activity against Yoshida sarcoma in rats, leukemia P388, sarcoma 180, Ehrlich Ascites carcinoma, Walker carcinosarcoma-256, and light activity against leukemia L-1210 in mice. [6]
The esperamicins are chromoprotein enediyne antitumor antibiotics of bacterial origin. Esperamicin A1 is the most well studied compound in this class. Esperamcin A1 and the related enediyne calicheamicin are the two most potent antitumor agents known. [1] The esperamicins are extremely toxic DNA splicing compounds. [2]