Targeting Hypoxia: Hypoxia-Activated Prodrugs in Cancer Therapy
Hypoxia is an important characteristic of most solid malignancies, and is closely related to tumor prognosis and therapeutic resistance. Hypoxia is one of the most important factors associated with resistance to conventional radiotherapy and chemotherapy. Therapies targeting tumor hypoxia have attra...
| Main Authors: | , , |
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| Format: | Article |
| Language: | English |
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Frontiers Media S.A.
2021-07-01
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| Series: | Frontiers in Oncology |
| Subjects: | |
| Online Access: | https://www.frontiersin.org/articles/10.3389/fonc.2021.700407/full |
| _version_ | 1818362496371654656 |
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| author | Yue Li Yue Li Yue Li Long Zhao Long Zhao Xiao-Feng Li Xiao-Feng Li |
| author_facet | Yue Li Yue Li Yue Li Long Zhao Long Zhao Xiao-Feng Li Xiao-Feng Li |
| author_sort | Yue Li |
| collection | DOAJ |
| description | Hypoxia is an important characteristic of most solid malignancies, and is closely related to tumor prognosis and therapeutic resistance. Hypoxia is one of the most important factors associated with resistance to conventional radiotherapy and chemotherapy. Therapies targeting tumor hypoxia have attracted considerable attention. Hypoxia-activated prodrugs (HAPs) are bioreductive drugs that are selectively activated under hypoxic conditions and that can accurately target the hypoxic regions of solid tumors. Both single-agent and combined use with other drugs have shown promising antitumor effects. In this review, we discuss the mechanism of action and the current preclinical and clinical progress of several of the most widely used HAPs, summarize their existing problems and shortcomings, and discuss future research prospects. |
| first_indexed | 2024-12-13T21:33:30Z |
| format | Article |
| id | doaj.art-1b7853fad6d64ad484fc31a37d9046ed |
| institution | Directory Open Access Journal |
| issn | 2234-943X |
| language | English |
| last_indexed | 2024-12-13T21:33:30Z |
| publishDate | 2021-07-01 |
| publisher | Frontiers Media S.A. |
| record_format | Article |
| series | Frontiers in Oncology |
| spelling | doaj.art-1b7853fad6d64ad484fc31a37d9046ed2022-12-21T23:30:45ZengFrontiers Media S.A.Frontiers in Oncology2234-943X2021-07-011110.3389/fonc.2021.700407700407Targeting Hypoxia: Hypoxia-Activated Prodrugs in Cancer TherapyYue Li0Yue Li1Yue Li2Long Zhao3Long Zhao4Xiao-Feng Li5Xiao-Feng Li6Department of Nuclear Medicine, The Second Clinical Medical College, Jinan University (Shenzhen People’s Hospital), Shenzhen, ChinaThe First Affiliated Hospital, Jinan University, Guangzhou, ChinaDepartment of Nuclear Medicine, The First Affiliated Hospital of Southern University of Science and Technology, Shenzhen, ChinaDepartment of Nuclear Medicine, The Second Clinical Medical College, Jinan University (Shenzhen People’s Hospital), Shenzhen, ChinaDepartment of Nuclear Medicine, The First Affiliated Hospital of Southern University of Science and Technology, Shenzhen, ChinaDepartment of Nuclear Medicine, The Second Clinical Medical College, Jinan University (Shenzhen People’s Hospital), Shenzhen, ChinaDepartment of Nuclear Medicine, The First Affiliated Hospital of Southern University of Science and Technology, Shenzhen, ChinaHypoxia is an important characteristic of most solid malignancies, and is closely related to tumor prognosis and therapeutic resistance. Hypoxia is one of the most important factors associated with resistance to conventional radiotherapy and chemotherapy. Therapies targeting tumor hypoxia have attracted considerable attention. Hypoxia-activated prodrugs (HAPs) are bioreductive drugs that are selectively activated under hypoxic conditions and that can accurately target the hypoxic regions of solid tumors. Both single-agent and combined use with other drugs have shown promising antitumor effects. In this review, we discuss the mechanism of action and the current preclinical and clinical progress of several of the most widely used HAPs, summarize their existing problems and shortcomings, and discuss future research prospects.https://www.frontiersin.org/articles/10.3389/fonc.2021.700407/fullhypoxiahypoxia-activated prodrugstirapazamineAQ4NPR-104EO9 |
| spellingShingle | Yue Li Yue Li Yue Li Long Zhao Long Zhao Xiao-Feng Li Xiao-Feng Li Targeting Hypoxia: Hypoxia-Activated Prodrugs in Cancer Therapy Frontiers in Oncology hypoxia hypoxia-activated prodrugs tirapazamine AQ4N PR-104 EO9 |
| title | Targeting Hypoxia: Hypoxia-Activated Prodrugs in Cancer Therapy |
| title_full | Targeting Hypoxia: Hypoxia-Activated Prodrugs in Cancer Therapy |
| title_fullStr | Targeting Hypoxia: Hypoxia-Activated Prodrugs in Cancer Therapy |
| title_full_unstemmed | Targeting Hypoxia: Hypoxia-Activated Prodrugs in Cancer Therapy |
| title_short | Targeting Hypoxia: Hypoxia-Activated Prodrugs in Cancer Therapy |
| title_sort | targeting hypoxia hypoxia activated prodrugs in cancer therapy |
| topic | hypoxia hypoxia-activated prodrugs tirapazamine AQ4N PR-104 EO9 |
| url | https://www.frontiersin.org/articles/10.3389/fonc.2021.700407/full |
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