Targeting CDK4/6 for Anticancer Therapy
Cyclin-dependent kinase 4/6 (CDK4/6) are key regulators of the cell cycle and are deemed as critical therapeutic targets of multiple cancers. Various approaches have been applied to silence CDK4/6 at different levels, i.e., CRISPR to knock out at the DNA level, siRNA to inhibit translation, and drug...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-03-01
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| Series: | Biomedicines |
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| Online Access: | https://www.mdpi.com/2227-9059/10/3/685 |
| _version_ | 1797447045610471424 |
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| author | Jiating Qi Zhuqing Ouyang |
| author_facet | Jiating Qi Zhuqing Ouyang |
| author_sort | Jiating Qi |
| collection | DOAJ |
| description | Cyclin-dependent kinase 4/6 (CDK4/6) are key regulators of the cell cycle and are deemed as critical therapeutic targets of multiple cancers. Various approaches have been applied to silence CDK4/6 at different levels, i.e., CRISPR to knock out at the DNA level, siRNA to inhibit translation, and drugs that target the protein of interest. Here we summarize the current status in this field, highlighting the mechanisms of small molecular inhibitors treatment and drug resistance. We describe approaches to combat drug resistance, including combination therapy and PROTACs drugs that degrade the kinases. Finally, critical issues and perspectives in the field are outlined. |
| first_indexed | 2024-03-09T13:49:13Z |
| format | Article |
| id | doaj.art-8279621e40a0499887ba3e73dc7c6ff4 |
| institution | Directory Open Access Journal |
| issn | 2227-9059 |
| language | English |
| last_indexed | 2024-03-09T13:49:13Z |
| publishDate | 2022-03-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Biomedicines |
| spelling | doaj.art-8279621e40a0499887ba3e73dc7c6ff42023-11-30T20:53:26ZengMDPI AGBiomedicines2227-90592022-03-0110368510.3390/biomedicines10030685Targeting CDK4/6 for Anticancer TherapyJiating Qi0Zhuqing Ouyang1The Second Clinical College, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, ChinaDepartment of Pathogen Biology, School of Basic Medicine, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, ChinaCyclin-dependent kinase 4/6 (CDK4/6) are key regulators of the cell cycle and are deemed as critical therapeutic targets of multiple cancers. Various approaches have been applied to silence CDK4/6 at different levels, i.e., CRISPR to knock out at the DNA level, siRNA to inhibit translation, and drugs that target the protein of interest. Here we summarize the current status in this field, highlighting the mechanisms of small molecular inhibitors treatment and drug resistance. We describe approaches to combat drug resistance, including combination therapy and PROTACs drugs that degrade the kinases. Finally, critical issues and perspectives in the field are outlined.https://www.mdpi.com/2227-9059/10/3/685CDK4/6PROTACsmall molecular inhibitordrug resistancecancerpalbociclib |
| spellingShingle | Jiating Qi Zhuqing Ouyang Targeting CDK4/6 for Anticancer Therapy Biomedicines CDK4/6 PROTAC small molecular inhibitor drug resistance cancer palbociclib |
| title | Targeting CDK4/6 for Anticancer Therapy |
| title_full | Targeting CDK4/6 for Anticancer Therapy |
| title_fullStr | Targeting CDK4/6 for Anticancer Therapy |
| title_full_unstemmed | Targeting CDK4/6 for Anticancer Therapy |
| title_short | Targeting CDK4/6 for Anticancer Therapy |
| title_sort | targeting cdk4 6 for anticancer therapy |
| topic | CDK4/6 PROTAC small molecular inhibitor drug resistance cancer palbociclib |
| url | https://www.mdpi.com/2227-9059/10/3/685 |
| work_keys_str_mv | AT jiatingqi targetingcdk46foranticancertherapy AT zhuqingouyang targetingcdk46foranticancertherapy |