Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, Research Support, Non-U.S. Gov’t, Journal of Medicinal Chemistry called An Exploration of Chemical Properties Required for Cooperative Stabilization of the 14-3-3 Interaction with NF-κB-Utilizing a Reversible Covalent Tethering Approach, Author is Wolter, Madita; Valenti, Dario; Cossar, Peter J.; Hristeva, Stanimira; Levy, Laura M.; Genski, Thorsten; Hoffmann, Torsten; Brunsveld, Luc; Tzalis, Dimitrios; Ottmann, Christian, which mentions a compound: 4045-24-3, SMILESS is COC1CCNCC1, Molecular C6H13NO, Name: 4-Methoxypiperidine.
Protein-protein modulation has emerged as a proven approach to drug discovery. While significant progress has been gained in developing protein-protein interaction (PPI) inhibitors, the orthogonal approach of PPI stabilization lacks established methodologies for drug design. Here, we report the systematic ”bottom-up” development of a reversible covalent PPI stabilizer. An imine bond was employed to anchor the stabilizer at the interface of the 14-3-3/p65 complex, leading to a mol. glue 24j (I) that elicited an 81-fold increase in complex stabilization. Utilizing protein crystallog. and biophys. assays, we deconvoluted how chem. properties of a stabilizer translate to structural changes in the ternary 14-3-3/p65/mol. glue complex. Furthermore, we explore how this leads to high cooperativity and increased stability of the complex.
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Reference:
Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem