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
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.