Cruentaren A 类似物的优化和研究-猫眼课题宝

Cruentaren A 类似物的优化和研究

批准号：

10078544

负责人：

Brian S J Blagg

金额：

$35.3万

依托单位：

UNIVERSITY OF NOTRE DAME

依托单位国家：

美国

项目类别：

财政年份：

2018

资助国家：

美国

项目状态：

已结题

起止时间：

2018-01-01 至 2022-06-30

来源：

https://reporter.nih.gov/project-details/10078544

关键词：

Animal Cancer Model Antineoplastic Agents Binding Binding Sites Cancer cell line Cardiotoxicity Cell Line Cell model Client Clinical Clinical Trials Complex Data Development Dose Energy Metabolism Enzymes Exhibits Frequencies Generations Goals HSP 90 inhibition Heat shock proteins Heat-Shock Response Hepatotoxicity In Vitro Individual Investigation Lead Malignant Neoplasms Maximum Tolerated Dose Methods Molecular Chaperones Molecular Conformation N-terminal Natural Products Normal Cell Pathway interactions Patients Peripheral Nervous System Diseases Pharmaceutical Preparations Preclinical Drug Development Production Protein Isoforms Proteins Reporting Schedule Signal Transduction Structure Structure-Activity Relationship Time Toxic effect Translating Translations Warburg Effect analog anticancer activity antitumor agent base cancer cell cancer therapy clinical application clinical candidate in vitro activity in vivo in vivo Model in vivo evaluation inhibitor/antagonist nanomolar neoplastic cell novel novel anticancer drug novel lead compound overexpression pre-clinical preclinical development preclinical evaluation protein degradation protein folding research clinical testing side effect small molecule tumor

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中文摘要

翻译

摘要开发治疗癌症的新方法是非常必要的。在此应用程序中，我们标识了一个大环小分子，对癌细胞和正常细胞表现出高的区分选择性，目的是开发这种分子的更简化的类似物，努力使效率最大化，同时减少步骤的总数，这将可能导致临床上有用的分子治疗癌症。此外, 我们的目标是询问这些化合物在细胞和动物癌症模型中表现出的活性，目的是提供临床前数据，以支持使用此类化合物进行翻译开发。

英文摘要

Abstract The development of new methods to treat cancer is greatly needed. In this application, we have identified a macrocyclic small molecule that exhibits high differential selectivity for cancer cells vs. normal cells and aim to develop more simplified analogs of this molecule in an effort to maximize efficiency as well as to decrease the overall number of steps, which will likely lead to clinically useful molecules for the treatment of cancer. In addition, we aim to interrogate the activity manifested by these compounds in both cellular and animal models of cancer, with the goal of providing preclinical data to support the use of such compounds for translational development.

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