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AntiCancer Screens

TopoGEN offers powerful and tractable services to identify Topoisomerase-targeting drugs.

In Situ Screens

TopoGEN offers powerful and tractable services to quantify the ability of your front line anticancer drug to specifically target endogenous topoisomerase action in cells.

Anit-Infective Screens

TopoGEN offers powerful and tractable services to identify Gyrase and Topoisomerase IV targeting antibiotics.

Customer Extracts

TopoGEN can quantify total topoisomerase I, IIactivity levels in your extracts

Western Blotting Services

TopoGEN can quantify topoisomerase I, IIa and IIb levels in your extracts using Westerns

Bio-Correlations

TopoGEN offers powerful and tractable services to assist.

Reviews

“The genomic era has shifted anticancer drug development from its traditional mode concentrated on natural product cytotoxic agents to mechanism-based drug design focused on signal transduction pathways. Yet traditional cytotoxic chemotherapies continue to have an important role in the armamentarium. This is particularly true when one considers that important elements of solid tumor physiology – acidosis and hypoxia – have rarely been incorporated into algorithms for anticancer drug development. It is now well established that a majority of solid tumors exist in an acidic and hypoxic microenvironment that promotes resistance to radiation and chemotherapies apart from any drug-induced target mutations or efflux protein pumps. The acidic extracellular environment leads to a pH gradient unique to tumor cells. This gradient will favor uptake and retention of small molecule drugs that are weak acids. The converse is true for weak bases. The camptothecin class of topoisomerase I inhibitors is one example of a natural product cytotoxic that can exploit the tumor pH gradient. Screening of compounds based on selective activity at acidic pH (pH modulation), rather than potency, reveals analogs that are over ten times more active under the acidic conditions prevalent in vivo. Thus, knowledge of the tumor metabolic phenotype gained at the beginning of the 20(th) century can lead to more effective anticancer drugs in the new millennium.”

Adams DJ

Department of Medicine, Duke University Medical Center, Durham, NC 27710, USA. , Curr Med Chem Anti-Canc Agents. 2005 Jan;5(1):1-13.

“Non-small cell lung cancer (NSCLC) is an aggressive disease that is generally resistant to chemotherapy. As a result, the prognosis for patients with NSCLC is poor. Currently, platinum-based regimens are the standard of care for patients with advanced NSCLC. However, these regimens are associated with severe and often cumulative hematologic and nonhematologic toxicities, limiting dose intensity. Therefore, novel chemotherapeutic agents and combination regimens may improve the outcome for these patients. A variety of new agents and combinations have been investigated in the treatment of NSCLC. However, to date, no clearly superior single-agent or combination regimen has emerged. Topotecan (Hycamtin; GlaxoSmithKline; Philadelphia, PA), a topoisomerase I inhibitor, is currently approved for the treatment of patients with relapsed small cell lung cancer (SCLC) and is associated with manageable, noncumulative, hematologic toxicities.

Stewart DJ.

The University of Texas M.D. Anderson Cancer Center, 1515 Holcombe Boulevard, Box 0432, Houston, Texas 77030, USA. , Oncologist. 2004;9 Suppl 6:43-52.

“Natural and synthetic indolocarbazole compounds have triggered considerable interest since the discovery in 1986 of the inhibitory properties of staurosporine toward protein kinase C (PKC). Later, it has been shown that indolocarbazole compounds may inhibit various kinases, such as cyclin dependent-kinases and/or topoisomerase I, someones behave only as DNA intercalators. In this review are presented various indolocarbazole compounds bearing a sugar moiety and their biological targets. The relevance of these targets to develop indolocarbazole compounds as potential antitumor agents is discussed.”

Prudhomme M.

Laboratoire SEESIB, UMR 6504 CNRS, Universite Blaise Pascal, 24, Avenue des Landais, 63177 Aubiere, France., Curr Med Chem Anti-Canc Agents. 2004 Nov;4(6):509-21.Biological targets of antitumor indolocarbazoles bearing a sugar moiety.