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Small molecule inhibitors of 15-PGDH exploit a physiologic induced-fit closing system
oleh: Wei Huang, Hongyun Li, Janna Kiselar, Stephen P. Fink, Sagar Regmi, Alexander Day, Yiyuan Yuan, Mark Chance, Joseph M. Ready, Sanford D. Markowitz, Derek J. Taylor
Format: | Article |
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Diterbitkan: | Nature Portfolio 2023-02-01 |
Deskripsi
Inhibition of 15-prostaglandin dehydrogenase (15-PGDH) is a promising therapeutic target for regenerative medicine. We report the structure of 15-PGDH in complex with two different inhibitors. Unexpectedly, access to the binding pocket is regulated by a dynamic “lid” of the enzyme.