14-3-3σ and Its Modulators in Cancer
14-3-3σ is an acidic homodimer protein with more than one hundred different protein partners associated with oncogenic signaling and cell cycle regulation. This review aims to highlight the crucial role of 14-3-3σ in controlling tumor growth and apoptosis and provide a detailed discussion on the str...
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| Format: | Article |
| Language: | English |
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MDPI AG
2020-12-01
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| Series: | Pharmaceuticals |
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| Online Access: | https://www.mdpi.com/1424-8247/13/12/441 |
| _version_ | 1797545850427146240 |
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| author | Ghazi Aljabal Beow Keat Yap |
| author_facet | Ghazi Aljabal Beow Keat Yap |
| author_sort | Ghazi Aljabal |
| collection | DOAJ |
| description | 14-3-3σ is an acidic homodimer protein with more than one hundred different protein partners associated with oncogenic signaling and cell cycle regulation. This review aims to highlight the crucial role of 14-3-3σ in controlling tumor growth and apoptosis and provide a detailed discussion on the structure–activity relationship and binding interactions of the most recent 14-3-3σ protein-protein interaction (PPI) modulators reported to date, which has not been reviewed previously. This includes the new fusicoccanes stabilizers (FC-NAc, DP-005), fragment stabilizers (TCF521-123, TCF521-129, AZ-003, AZ-008), phosphate-based inhibitors (IMP, PLP), peptide inhibitors (2a–d), as well as inhibitors from natural sources (85531185, 95911592). Additionally, this review will also include the discussions of the recent efforts by a different group of researchers for understanding the binding mechanisms of existing 14-3-3σ PPI modulators. The strategies and state-of-the-art techniques applied by various group of researchers in the discovery of a different chemical class of 14-3-3σ modulators for cancer are also briefly discussed in this review, which can be used as a guide in the development of new 14-3-3σ modulators in the near future. |
| first_indexed | 2024-03-10T14:21:52Z |
| format | Article |
| id | doaj.art-e95310b31dc648118435c7006dfe02ea |
| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-03-10T14:21:52Z |
| publishDate | 2020-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceuticals |
| spelling | doaj.art-e95310b31dc648118435c7006dfe02ea2023-11-20T23:21:36ZengMDPI AGPharmaceuticals1424-82472020-12-01131244110.3390/ph1312044114-3-3σ and Its Modulators in CancerGhazi Aljabal0Beow Keat Yap1School of Pharmaceutical Sciences, Universiti Sains Malaysia, Gelugor 11800, Penang, MalaysiaSchool of Pharmaceutical Sciences, Universiti Sains Malaysia, Gelugor 11800, Penang, Malaysia14-3-3σ is an acidic homodimer protein with more than one hundred different protein partners associated with oncogenic signaling and cell cycle regulation. This review aims to highlight the crucial role of 14-3-3σ in controlling tumor growth and apoptosis and provide a detailed discussion on the structure–activity relationship and binding interactions of the most recent 14-3-3σ protein-protein interaction (PPI) modulators reported to date, which has not been reviewed previously. This includes the new fusicoccanes stabilizers (FC-NAc, DP-005), fragment stabilizers (TCF521-123, TCF521-129, AZ-003, AZ-008), phosphate-based inhibitors (IMP, PLP), peptide inhibitors (2a–d), as well as inhibitors from natural sources (85531185, 95911592). Additionally, this review will also include the discussions of the recent efforts by a different group of researchers for understanding the binding mechanisms of existing 14-3-3σ PPI modulators. The strategies and state-of-the-art techniques applied by various group of researchers in the discovery of a different chemical class of 14-3-3σ modulators for cancer are also briefly discussed in this review, which can be used as a guide in the development of new 14-3-3σ modulators in the near future.https://www.mdpi.com/1424-8247/13/12/441protein-protein interaction (PPI)14-3-3σdimerstabilizerinhibitorcancer |
| spellingShingle | Ghazi Aljabal Beow Keat Yap 14-3-3σ and Its Modulators in Cancer Pharmaceuticals protein-protein interaction (PPI) 14-3-3σ dimer stabilizer inhibitor cancer |
| title | 14-3-3σ and Its Modulators in Cancer |
| title_full | 14-3-3σ and Its Modulators in Cancer |
| title_fullStr | 14-3-3σ and Its Modulators in Cancer |
| title_full_unstemmed | 14-3-3σ and Its Modulators in Cancer |
| title_short | 14-3-3σ and Its Modulators in Cancer |
| title_sort | 14 3 3σ and its modulators in cancer |
| topic | protein-protein interaction (PPI) 14-3-3σ dimer stabilizer inhibitor cancer |
| url | https://www.mdpi.com/1424-8247/13/12/441 |
| work_keys_str_mv | AT ghazialjabal 1433sanditsmodulatorsincancer AT beowkeatyap 1433sanditsmodulatorsincancer |