Novel Pyrrolopyrimidine-Based alpha-Helix Mimetics: Cell-Permeable Inhibitors of Protein-Protein Interactions
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- Title
- Novel Pyrrolopyrimidine-Based alpha-Helix Mimetics: Cell-Permeable Inhibitors of Protein-Protein Interactions
- Authors
- Lee, JH; Zhang, Q; Jo, S; Chai, SC; Oh, M; Im, W; Lu, H; Lim, HS
- Date Issued
- 2011-02-02
- Publisher
- American Chemical Society
- Abstract
- There is considerable interest in developing non-peptidic, small-molecule alpha-helix mimetics to disrupt alpha-helix-mediated protein protein interactions. Herein, we report the design of a novel pyrrolopyrimidine-based scaffold for such alpha-helix mimetics with increased conformational rigidity. We also developed a facile solid-phase synthetic route that is amenable to divergent synthesis of a large library. Using a fluorescence polarization-based assay, we identified cell-permeable, dual MDMX/MDM2 inhibitors, demonstrating that the designed molecules can act as alpha-helix mimetics.
- Keywords
- SMALL-MOLECULE INHIBITORS; STRUCTURE-BASED DESIGN; BETA(3)-PEPTIDE INHIBITORS; P53 PATHWAY; IN-VIVO; MDMX; AFFINITY; ANTAGONISTS; SCAFFOLDS; LIBRARIES
- URI
- https://oasis.postech.ac.kr/handle/2014.oak/16856
- DOI
- 10.1021/JA108230S
- ISSN
- 0002-7863
- Article Type
- Article
- Citation
- JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, vol. 133, no. 4, page. 676 - 679, 2011-02-02
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- There are no files associated with this item.
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