Glioblastoma multiforme is the most common and lethal brain *** current standard of care includes Temozolomide(TMZ)***,inherent and acquired resistance to TMZ thwart successful *** direct repair protein methylguanine ...
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Glioblastoma multiforme is the most common and lethal brain *** current standard of care includes Temozolomide(TMZ)***,inherent and acquired resistance to TMZ thwart successful *** direct repair protein methylguanine DNA methyltransferase(MGMT)removes the cytotoxic O6-methylguanine(O6-MeG)lesion delivered by TMZ and so its expression by tumours confers *** mismatch repair(MMR)is essential to process O6-MeG adducts and MMR-deficiency leads to tolerance of lesions,resistance to TMZ and further DNA *** this article,two strategies to overcome TMZ resistance are discussed:(1)synthesis of imidazotetrazine analogues-designed to retain activity in the presence of MGMT or loss of MMR;(2)preparation of imidazotetrazine-nanoparticles to deliver TMZ preferably to the brain and tumour *** promising results encourage belief in a future where better prognoses exist for patients diagnosed with this devastating disease.
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