Identification and development of novel compounds for the treatment of human cancers

作者: Steven Spencer Carey

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摘要: Although some progress has been made in the treatment of cancer over last sixty years, majority chemotherapeutics fallen short. Because general chemotherapies that target DNA replication have only a limited efficacy and significant non-target side-effects, new paradigm for drug development adopted. Using molecular targeted approach, gene protein targets identified are specific to these already begun. In this study, compounds interact with two key targets, Gquadruplex c-Myc promoter p-glycoprotein, investigated. By developing such compounds, improvements is anticipated an aspiration decreased mortality attributable cancer. Formation secondary structures, as G-quadruplex, NHE III1 region shown repress transcription. oncogene overexpressed variety cancers, stabilization G-quadruplex by small molecules would be advantageous treatment. Fluorescence Resonance Energy Transfer, Taq Polymerase Stop assays confirmation, group were stabilize structure. colon model, decrease expression. Also, exposure 48 hours results induction caspase-3, indicative apoptosis. Furthermore, surface plasmon resonance suggests compound-induced can prevent sustained binding regulatory NM23-H2

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