Remarkable Synergy When Combining EZH2 Inhibitors with YM155 Is H3K27me3-Independent
Targeting multiple molecules in the same biological network may maximize therapeutic efficacy. In this study, we identified a 27-gene module that is highly expressed in solid tumors, encoding actionable targets including EZH2 and BIRC5. The combination of EZH2 inhibitors and a BIRC5 inhibitor, YM155...
| Main Authors: | , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-12-01
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| Series: | Cancers |
| Subjects: | |
| Online Access: | https://www.mdpi.com/2072-6694/15/1/208 |
| _version_ | 1797626147958161408 |
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| author | Jun Yang Andrew M. Davidoff |
| author_facet | Jun Yang Andrew M. Davidoff |
| author_sort | Jun Yang |
| collection | DOAJ |
| description | Targeting multiple molecules in the same biological network may maximize therapeutic efficacy. In this study, we identified a 27-gene module that is highly expressed in solid tumors, encoding actionable targets including EZH2 and BIRC5. The combination of EZH2 inhibitors and a BIRC5 inhibitor, YM155, results in a remarkable synergistic effect. The action of EZH2 inhibitors in this process is independent of the histone methyltransferase activity of polycomb repressive complex 2. Our study reveals a potential therapeutic approach for treating solid tumors by simultaneously targeting EZH2 and BIRC5. |
| first_indexed | 2024-03-11T10:06:22Z |
| format | Article |
| id | doaj.art-e6ad75c466434b63b7e359731ece6ad0 |
| institution | Directory Open Access Journal |
| issn | 2072-6694 |
| language | English |
| last_indexed | 2024-03-11T10:06:22Z |
| publishDate | 2022-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Cancers |
| spelling | doaj.art-e6ad75c466434b63b7e359731ece6ad02023-11-16T15:03:05ZengMDPI AGCancers2072-66942022-12-0115120810.3390/cancers15010208Remarkable Synergy When Combining EZH2 Inhibitors with YM155 Is H3K27me3-IndependentJun Yang0Andrew M. Davidoff1Department of Surgery, St. Jude Children’s Research Hospital, Memphis, TN 38105, USADepartment of Surgery, St. Jude Children’s Research Hospital, Memphis, TN 38105, USATargeting multiple molecules in the same biological network may maximize therapeutic efficacy. In this study, we identified a 27-gene module that is highly expressed in solid tumors, encoding actionable targets including EZH2 and BIRC5. The combination of EZH2 inhibitors and a BIRC5 inhibitor, YM155, results in a remarkable synergistic effect. The action of EZH2 inhibitors in this process is independent of the histone methyltransferase activity of polycomb repressive complex 2. Our study reveals a potential therapeutic approach for treating solid tumors by simultaneously targeting EZH2 and BIRC5.https://www.mdpi.com/2072-6694/15/1/208EZH2BIRC5YM155EPZ5687EPZ6438GSK343 |
| spellingShingle | Jun Yang Andrew M. Davidoff Remarkable Synergy When Combining EZH2 Inhibitors with YM155 Is H3K27me3-Independent Cancers EZH2 BIRC5 YM155 EPZ5687 EPZ6438 GSK343 |
| title | Remarkable Synergy When Combining EZH2 Inhibitors with YM155 Is H3K27me3-Independent |
| title_full | Remarkable Synergy When Combining EZH2 Inhibitors with YM155 Is H3K27me3-Independent |
| title_fullStr | Remarkable Synergy When Combining EZH2 Inhibitors with YM155 Is H3K27me3-Independent |
| title_full_unstemmed | Remarkable Synergy When Combining EZH2 Inhibitors with YM155 Is H3K27me3-Independent |
| title_short | Remarkable Synergy When Combining EZH2 Inhibitors with YM155 Is H3K27me3-Independent |
| title_sort | remarkable synergy when combining ezh2 inhibitors with ym155 is h3k27me3 independent |
| topic | EZH2 BIRC5 YM155 EPZ5687 EPZ6438 GSK343 |
| url | https://www.mdpi.com/2072-6694/15/1/208 |
| work_keys_str_mv | AT junyang remarkablesynergywhencombiningezh2inhibitorswithym155ish3k27me3independent AT andrewmdavidoff remarkablesynergywhencombiningezh2inhibitorswithym155ish3k27me3independent |