發明
中華民國
107129529
I 699202
有機鉑複合物和其藥物組合物以及hTop 2 core-DNA-有機鉑複合物晶體的製備方法
國立臺灣大學
2020/07/21
The 4 most critical advancements we have achieved are (i) establishment of hTop2 isozyme-specific assaying platforms using different biochemical, cellular and pharmacological approaches, (ii) Animal models for determination of anticancer efficacy, (iii) structure determination of both hTop2α and hTop2β in complexes with DNA, (iv) Unique drug-replacement structure platform for lead compound validation and optimization. Structural analyses not only reveal the molecular basis of drug action, but also allow the formulation of design guidelines for the advanced development of isoform-specific hTop2-targeting antineoplastic agents. In this project, we plan and seek to further examine the anticancer efficacy of our leads, 4th generation optimized leads and carry out pharmacological, toxicological and safety assessments of our leads and with the following specific aims: 1. To further establish the anticancer efficacy and/or reduced side effects of our optimized leads. 2. To validate MOA, improve isozyme selectivity and optimize leads. The choice of SCLC treatment has always been only chemotherapy drugs, although the Atezolizumab was approved in 2019 but still needs to be used in conjunction with Etoposide. However, these topoisomerase inhibitors cause many side effects. (e.g., etoposide-, doxorubicin-associated bone marrow suppression, hepatotoxicity, cardiotoxicity and 2nd malignancies)
產學合作總中心
33669945
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主辦單位:國家科學及技術委員會 執行單位:台灣經濟研究院 網站維護:台灣經濟研究院