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- W3004733782 abstract "C-terminal binding proteins (CtBP1 & 2) are co-transcriptional factors that have been implicated in progression of a broad range of cancers. CtBP possesses a D-isomer specific 2-hydroxyacid dehydrogenase (D2-HDH) domain that binds NAD(H) and provides an attractive target for small molecule intervention. We have previously demonstrated that NAD(H) triggers assembly of CtBP1 and CtBP2 into structurally very similar tetramers, strongly suggesting that this tetrameric form is the co-transcriptionally active species. Using multi-angle light scattering (MALS) to test various NAD(H) moieties, we find that AMP and ADP, but not adenosine, nicotinamide and nicotinamide mononucleotide promote tetramer formation, demonstrating that the adenosine phosphate plays a central role in tetrameric assembly. Crystal structures with bound AMP show a direct structural role of this phosphate in stabilizing a key interaction across the tetrameric interface. Most importantly, these results indicate that development of inhibitors that extend into the nicotinamide pocket, including the regions bound to the nicotinamide ribose and phosphate, should inhibit NAD(H) binding and interfere with tetrameric assembly. We are using these results to guide our development of anti-neoplastic CtBP specific inhibitors." @default.
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- W3004733782 date "2020-02-01" @default.
- W3004733782 modified "2023-10-18" @default.
- W3004733782 title "Illuminating the Structural Determinants for Tetrameric Assembly of Oncogenic CtBP to Guide Inhibitor Design" @default.
- W3004733782 doi "https://doi.org/10.1016/j.bpj.2019.11.430" @default.
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