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Expert Opin Drug Discov. 2013 Sep;8(9):1135-51. doi: 10.1517/17460441.2013.807248. Epub 2013 Jun 6.

Novel approaches to glioma drug design and drug screening.

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  • 1Department of Pharmaceutical Sciences, College of Pharmacy, The University of Tennessee Health Science Center, 847 Monroe Avenue, Room 327, 881 Madison, Room 435, Memphis, TN 38163, USA. spatil3@uthsc.edu



Gliomas are considered the most malignant form of brain tumors, and ranked among the most aggressive human cancers. Despite advance standard therapy the prognosis for patients with gliomas remains poor. Chemotherapy has played an important role as an adjuvant in treating gliomas. The efficacy of the chemotherapeutic drug is limited due to poor drug delivery and the inherent chemo- and radio-resistance. Challenges of the brain cancer therapy in clinical settings are; i) to overcome the chemo- and radio-resistance, ii) to improve drug delivery to tumors and iii) the development of effective drug screening procedures.


In this review, the authors discuss clinically important chemotherapeutic agents used for treating malignant gliomas along with novel drug design approaches. The authors, furthermore, discuss the in vitro and in vivo drug screening procedures for the development of novel drug candidates.


The development of novel and highly potent chemotherapeutic agents for both glioma and glioma stem cells (GSCs) is highly important for future brain cancer research. Thus, research efforts should be directed towards developing innovative molecularly targeted antiglioma agents in order to reduce the toxicity and drug resistance which are associated with current forms of therapy. Development of novel pre-clinical drug screening procedures is also very critical for the overall success of brain cancer therapies in clinical settings.

[PubMed - indexed for MEDLINE]
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