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14-3-3σ and Its Modulators in Cancer

School of Pharmaceutical Sciences, Universiti Sains Malaysia, Gelugor 11800, Penang, Malaysia
Author to whom correspondence should be addressed.
Pharmaceuticals 2020, 13(12), 441;
Received: 4 November 2020 / Revised: 30 November 2020 / Accepted: 1 December 2020 / Published: 3 December 2020
(This article belongs to the Section Medicinal Chemistry)
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. View Full-Text
Keywords: protein-protein interaction (PPI); 14-3-3σ; dimer; stabilizer; inhibitor; cancer protein-protein interaction (PPI); 14-3-3σ; dimer; stabilizer; inhibitor; cancer
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MDPI and ACS Style

Aljabal, G.; Yap, B.K. 14-3-3σ and Its Modulators in Cancer. Pharmaceuticals 2020, 13, 441.

AMA Style

Aljabal G, Yap BK. 14-3-3σ and Its Modulators in Cancer. Pharmaceuticals. 2020; 13(12):441.

Chicago/Turabian Style

Aljabal, Ghazi, and Beow K. Yap 2020. "14-3-3σ and Its Modulators in Cancer" Pharmaceuticals 13, no. 12: 441.

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