ACS meetings content online

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>> Tuesday, May 25, 2010

It’s good news for those who had missed the opportunity to attend American Chemical Society (ACS) meeting in San Francisco, CA (Spring 2010),  Washington, D. C and Boston MA (Fall 2010). ACS has provided the contents from the meetings online. It’s great to see and hear the presentation with a sip of coffee just sitting in front of your computer. They have synchronized the audio with power point slide. Great job indeed!


Voreloxin: DNA intercalating topoisomerase II poison

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>> Tuesday, May 18, 2010

As we know, topoisomerases are the nuclear enzymes that change the topology of DNA by transiently breaking one or two strands of DNA. They have important role in number of vital cellular processes like replication, transcription, recombination, repair, chromatin assembly, and chromosome segregation. Many anticancer drugs that target topoisomerase have been developed. For instance, Camptothecin and Etoposide, well known anticancer agents, inhibit topo I and topo II respectively.
Voreloxin, Topo II poison
Recently, Voreloxin, a quinolone derivative, which is completing phase 2 clinical trials for acute myeloid leukemia (AML) and platinum-resistant ovarian cancer, has been reported as a DNA intercalating topo II poison.
Discovery of Voreloxin has occurred while optimizing the class of compounds bearing a 1, 8 –naphthyridine core. Voreloxin has no antibacterial activity, but interestingly shows potent cytotoxicity towards eukaryotic cancer cell lines. Moreover, its activity was not affected by common mechanism of drug resistance, including P-gp overexpression, when evaluated in etoposide and anthracycline-resistant nonclinical models. Authors claimed Voreloxin as a first-in-class topo II poison and inhibitor that  intercalates DNA and induces site selective DNA DSB, G2 arrest, and apoptosis.




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