Mutant-selective degradation by BRAF-targeting PROTACs
Hundreds of BRAF mutations have been identified in patients with cancer but currently approved drugs only target BRAF V600 mutants. Here, the authors develop a vemurafenib-based PROTAC that induces degradation of all classes of BRAF mutants without affecting wild-type RAF proteins.
| Main Authors: | , , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
Nature Portfolio
2021-02-01
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| Series: | Nature Communications |
| Online Access: | https://doi.org/10.1038/s41467-021-21159-7 |
| _version_ | 1818754050001207296 |
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| author | Shanique Alabi Saul Jaime-Figueroa Zhan Yao Yijun Gao John Hines Kusal T. G. Samarasinghe Lea Vogt Neal Rosen Craig M. Crews |
| author_facet | Shanique Alabi Saul Jaime-Figueroa Zhan Yao Yijun Gao John Hines Kusal T. G. Samarasinghe Lea Vogt Neal Rosen Craig M. Crews |
| author_sort | Shanique Alabi |
| collection | DOAJ |
| description | Hundreds of BRAF mutations have been identified in patients with cancer but currently approved drugs only target BRAF V600 mutants. Here, the authors develop a vemurafenib-based PROTAC that induces degradation of all classes of BRAF mutants without affecting wild-type RAF proteins. |
| first_indexed | 2024-12-18T05:17:05Z |
| format | Article |
| id | doaj.art-c199e2f0eb92437a873d93ab5b38d197 |
| institution | Directory Open Access Journal |
| issn | 2041-1723 |
| language | English |
| last_indexed | 2024-12-18T05:17:05Z |
| publishDate | 2021-02-01 |
| publisher | Nature Portfolio |
| record_format | Article |
| series | Nature Communications |
| spelling | doaj.art-c199e2f0eb92437a873d93ab5b38d1972022-12-21T21:19:45ZengNature PortfolioNature Communications2041-17232021-02-0112111110.1038/s41467-021-21159-7Mutant-selective degradation by BRAF-targeting PROTACsShanique Alabi0Saul Jaime-Figueroa1Zhan Yao2Yijun Gao3John Hines4Kusal T. G. Samarasinghe5Lea Vogt6Neal Rosen7Craig M. Crews8Department of PharmacologyMolecular, Cellular, and Developmental Biology, Yale UniversityProgram in Molecular Pharmacology, Memorial Sloan Kettering Cancer CenterProgram in Molecular Pharmacology, Memorial Sloan Kettering Cancer CenterMolecular, Cellular, and Developmental Biology, Yale UniversityMolecular, Cellular, and Developmental Biology, Yale UniversityMolecular, Cellular, and Developmental Biology, Yale UniversityProgram in Molecular Pharmacology, Memorial Sloan Kettering Cancer CenterDepartment of PharmacologyHundreds of BRAF mutations have been identified in patients with cancer but currently approved drugs only target BRAF V600 mutants. Here, the authors develop a vemurafenib-based PROTAC that induces degradation of all classes of BRAF mutants without affecting wild-type RAF proteins.https://doi.org/10.1038/s41467-021-21159-7 |
| spellingShingle | Shanique Alabi Saul Jaime-Figueroa Zhan Yao Yijun Gao John Hines Kusal T. G. Samarasinghe Lea Vogt Neal Rosen Craig M. Crews Mutant-selective degradation by BRAF-targeting PROTACs Nature Communications |
| title | Mutant-selective degradation by BRAF-targeting PROTACs |
| title_full | Mutant-selective degradation by BRAF-targeting PROTACs |
| title_fullStr | Mutant-selective degradation by BRAF-targeting PROTACs |
| title_full_unstemmed | Mutant-selective degradation by BRAF-targeting PROTACs |
| title_short | Mutant-selective degradation by BRAF-targeting PROTACs |
| title_sort | mutant selective degradation by braf targeting protacs |
| url | https://doi.org/10.1038/s41467-021-21159-7 |
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