Qin, Lihong; Mao, Huiwen; Wang, Jianguo; Wang, Yuanyaun; Khan, Salman A.; Zhang, Ying; Qiu, Hong; Jiang, Longwei; He, Lingfeng; Zhang, Yan; Jia, Shaochang published the artcile< A novel polymerase β inhibitor from phage displayed peptide library augments the anti-tumour effects of temozolomide on colorectal cancer>, Category: esters-buliding-blocks, the main research area is temozolomide 10D anticancer polymerasebeta colorectal cancer phage display library; CRC; DNA repair; Inhibitor; Polβ; TMZ.
The therapeutic efficacy of TMZ, a common used drug for chemotherapy, is limited by the resistance from colorectal cancer cells. Base excision repair (BER) pathway has been identified as one of the reasons for drug resistance. By blocking Polβ-dependent BER (Base Excision Repair) pathway, the efficacy of TMZ treatment can be improved greatly. Several Polβ inhibitors that have been identified could not become approved drugs due to lack of potency or specificity. To find therapeutic candidates with exquisite specificity and high affinity to Polβ, phage display technol. was used in the current research. We screened out a candidate Polβ inhibitor, 10 D, that can inhibit the activity of Polβand SP-BER (Short-Patch Base excision Repair) pathway. Co-treatment with 10 D enhanced the sensitivity of colorectal cancer (CRC) cells to TMZ both in vitro and in vivo. Our data suggested that the novel Polβ inhibitor we identified can improve TMZ efficacy and optimize CRC chemotherapy.
Journal of Chemotherapy (Abingdon, United Kingdom) published new progress about Colorectal neoplasm. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Category: esters-buliding-blocks.
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