Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 4045-24-3, is researched, SMILESS is COC1CCNCC1, Molecular C6H13NOJournal, 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, the main research direction is reversible covalent PPI stabilizer NFkB p65 complex mol glue.Related Products of 4045-24-3.
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