Structure–Activity Relationship of PAD4 Inhibitors and Their Role in Tumor Immunotherapy
Protein arginine deiminase 4 (PAD4) plays an important role in cancer progression by participating in gene regulation, protein modification, and neutrophil extracellular trap (NET) formation. Many reversible and irreversible PAD4 inhibitors have been reported recently. In this review, we summarize t...
| Main Authors: | , , , , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2024-02-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/16/3/335 |
| _version_ | 1797239667077152768 |
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| author | Yijiang Jia Renbo Jia Ayijiang Taledaohan Yanming Wang Yuji Wang |
| author_facet | Yijiang Jia Renbo Jia Ayijiang Taledaohan Yanming Wang Yuji Wang |
| author_sort | Yijiang Jia |
| collection | DOAJ |
| description | Protein arginine deiminase 4 (PAD4) plays an important role in cancer progression by participating in gene regulation, protein modification, and neutrophil extracellular trap (NET) formation. Many reversible and irreversible PAD4 inhibitors have been reported recently. In this review, we summarize the structure–activity relationships of newly investigated PAD4 inhibitors to bring researchers up to speed by guiding and describing new scaffolds as optimization and development leads for new effective, safe, and selective cancer treatments. In addition, some recent reports have shown evidence that PAD4 inhibitors are expected to trigger antitumor immune responses, regulate immune cells and related immune factors, enhance the effects of immune checkpoint inhibitors, and enhance their antitumor efficacy. Therefore, PAD4 inhibitors may potentially change tumor immunotherapy and provide an excellent direction for the development and clinical application of immunotherapy strategies for related diseases. |
| first_indexed | 2024-04-24T17:55:10Z |
| format | Article |
| id | doaj.art-8ba5686945744ddda3d025bc7aa8ccf8 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-04-24T17:55:10Z |
| publishDate | 2024-02-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-8ba5686945744ddda3d025bc7aa8ccf82024-03-27T13:59:38ZengMDPI AGPharmaceutics1999-49232024-02-0116333510.3390/pharmaceutics16030335Structure–Activity Relationship of PAD4 Inhibitors and Their Role in Tumor ImmunotherapyYijiang Jia0Renbo Jia1Ayijiang Taledaohan2Yanming Wang3Yuji Wang4Department of Medicinal Chemistry, School of Pharmaceutical Sciences of Capital Medical University, 10 Xi Tou Tiao, You An Men, Beijing 100069, ChinaDepartment of Medicinal Chemistry, School of Pharmaceutical Sciences of Capital Medical University, 10 Xi Tou Tiao, You An Men, Beijing 100069, ChinaDepartment of Medicinal Chemistry, School of Pharmaceutical Sciences of Capital Medical University, 10 Xi Tou Tiao, You An Men, Beijing 100069, ChinaSchool of Life Sciences, Henan University, Kaifeng 475004, ChinaDepartment of Medicinal Chemistry, School of Pharmaceutical Sciences of Capital Medical University, 10 Xi Tou Tiao, You An Men, Beijing 100069, ChinaProtein arginine deiminase 4 (PAD4) plays an important role in cancer progression by participating in gene regulation, protein modification, and neutrophil extracellular trap (NET) formation. Many reversible and irreversible PAD4 inhibitors have been reported recently. In this review, we summarize the structure–activity relationships of newly investigated PAD4 inhibitors to bring researchers up to speed by guiding and describing new scaffolds as optimization and development leads for new effective, safe, and selective cancer treatments. In addition, some recent reports have shown evidence that PAD4 inhibitors are expected to trigger antitumor immune responses, regulate immune cells and related immune factors, enhance the effects of immune checkpoint inhibitors, and enhance their antitumor efficacy. Therefore, PAD4 inhibitors may potentially change tumor immunotherapy and provide an excellent direction for the development and clinical application of immunotherapy strategies for related diseases.https://www.mdpi.com/1999-4923/16/3/335reviewPAD4PAD4 inhibitorstructure–activity relationshipantitumor immunitycombination therapy strategies |
| spellingShingle | Yijiang Jia Renbo Jia Ayijiang Taledaohan Yanming Wang Yuji Wang Structure–Activity Relationship of PAD4 Inhibitors and Their Role in Tumor Immunotherapy Pharmaceutics review PAD4 PAD4 inhibitor structure–activity relationship antitumor immunity combination therapy strategies |
| title | Structure–Activity Relationship of PAD4 Inhibitors and Their Role in Tumor Immunotherapy |
| title_full | Structure–Activity Relationship of PAD4 Inhibitors and Their Role in Tumor Immunotherapy |
| title_fullStr | Structure–Activity Relationship of PAD4 Inhibitors and Their Role in Tumor Immunotherapy |
| title_full_unstemmed | Structure–Activity Relationship of PAD4 Inhibitors and Their Role in Tumor Immunotherapy |
| title_short | Structure–Activity Relationship of PAD4 Inhibitors and Their Role in Tumor Immunotherapy |
| title_sort | structure activity relationship of pad4 inhibitors and their role in tumor immunotherapy |
| topic | review PAD4 PAD4 inhibitor structure–activity relationship antitumor immunity combination therapy strategies |
| url | https://www.mdpi.com/1999-4923/16/3/335 |
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