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Novel Pyrrolopyrimidine-Based α-Helix Mimetics: Cell- Permeable Inhibitors of Protein-Protein Interactions
Lee, Ji Hoon Zhang, Qi Jo, Sunhwan Chai, Sergip Oh, Misook Im, Wonpil Lu, Hua Lim, Hyun-Suk
Lee, Ji Hoon
Zhang, Qi
Jo, Sunhwan
Chai, Sergip
Oh, Misook
Im, Wonpil
Lu, Hua
Lim, Hyun-Suk
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Abstract
There is considerable interest in developing nonpeptidic, small molecule α-helix mimetics to disrupt α-helix-mediated protein-protein interactions. Herein, we report the design of a novel pyrrolopyrimidine-based scaffold for such α-helix mimetics with increased conformational rigidity. We also developed a facile solid phase synthetic route, which 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 α-helix mimetics.
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This document is the Accepted Manuscript version of a Published Work that appeared in final form in the Journal of the American Chemical Society, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see http://doi.org/10.1021/ja108230s.
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2011-02-02
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American Chemical Society
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JoS_2011.pdf
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Lee, J. H., Zhang, Q., Jo, S., Chai, S. C., Oh, M., Im, W., … Lim, H.-S. (2011). Novel Pyrrolopyrimidine-Based α-Helix Mimetics: Cell-Permeable Inhibitors of Protein-Protein Interactions. Journal of the American Chemical Society, 133(4), 676–679. http://doi.org/10.1021/ja108230s