發明
中華民國
096146086
I 433672
吲唑化合物
國立臺灣大學
2014/04/11
腫瘤的淋巴管新生(Lymphangiogenesis)被認為是癌細胞轉移的重要途徑之一,因此C型血管內皮生長因子(VEGF-C)及其受體血管內皮生長因子受體-3 (VEGFR-3)的訊息被認為是抑制癌細胞轉移之標靶治療的重要標的;本技術團隊成功開發一種新的多學科綜合方法,快速合成一系列之小分子吲唑化合物,用以開發以VEGFR-3為標的癌症治療藥物,同時並已成功的發展出可快速且大量的篩選具抑制VEGFR3活性化合物的技術平臺-激脢受體活化酵素連結免疫吸附分析法(KIRA-ELISA),篩選具有抑制VEGFR-3訊息傳導中止淋巴管增生,進而降低癌細胞淋巴轉移之後選藥物,目前所開發之小分子吲唑化合物及其衍生物,已獲得美國新物質專利,將轉移給財團法人生物技術中心,共同進行後續的臨床藥物試驗與開發。 Tumor lymphangiogenesis is considered to be one important pathway to contribute cancer metastasis. Thus, VEGF-C/ VEGFR-3 signaling pathway as an important target for anticancer therapeutics designed to limit metastatic spread. Our research team successfully developed a new multidisciplinary synthetic approach to synthesis of indazole compound library for developed VEGFR-3 specific inhibitors as the candidate drug of targeted cancer therapies. Moreover, we also developed a high-throughput platform as KIRA-ELISA to screen indazole compounds with activity to suppress VEGFR-3 signaling then decreased lymphangiogenesis and tumor metastasis. Current, the small molecule of indazole compounds and their derivatives exhibited a inhibitory potency on tumor growth, metastasis, recurrence and increased survival rate. These indazole compounds have received U.S. patent and it well transfer to Development Center for Biotechnology (DCB) for drug development and clinical testing in cancer treatmen.
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