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Small-molecule inhibitors of 14-3-3 protein–protein interactions could serve as valuable chemical biology tools and starting points for drug development. The article by Zhao et al. (1) described FOBISIN101 (1) (Fig. 1A), a pyridoxal-phosphate (PLP) derivative that inhibits 14-3-3 protein–protein interactions. The authors provided a crystal structure of 14-3-3ζ with PLP covalently bound to K120 [Protein Data Bank (PDB) ID code 3RDH] lacking the p-amino-benzoate moiety. As a mechanism, they propose X-ray–induced cleavage of the N=N bond. They suggest this mechanism could serve as a radiation-triggered anticancer prodrug concept.pnas;109/18/E1051/FIG01F1fig01Fig. 1.(A) PLP derivatives 1 (FOBISIN101) and 2. The PLP part is highlighted...
| Authors: | Lars Röglin; Philipp Thiel; Oliver Kohlbacher; Christian Ottmann | |
| Journal: | Proceedings of the National Academy of Sciences current issue | |
| Volume: | 109 | |
| Issue: | 18 | |
| Year: | 2012 | |
| Pages: | E1051 | |
| DOI: | 10.1073/pnas.1116592109 | |
| Publication date: | 01-05-2012 |
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