Discovery of Non-prostanoid EP4 Agonists for the Treatment of Inflammatory Bowel Disease
was shown to induce hemodynamic changes in mouse, a known on-target effect of EP4 agonists in systemic circulation. High-throughput mutagenesis studies and computational modeling indicate that this series of agonists binds orthosterically to the PGE2 site in the EP4 receptor despite structural differentiation from prostanoids.
Authors
- R. M. Borzilleri
- Laura E. Armstrong (ORCID: https://orcid.org/0000-0002-7351-0701)
- Jenny Xie (ORCID: https://orcid.org/0000-0002-7083-4081)
- Mary T. Obermeier
- David Marcoux (ORCID: https://orcid.org/0000-0002-0295-7717)
- Purnima Khandelwal
- Heidi L. Perez (ORCID: https://orcid.org/0000-0003-3450-3434)
- Sunita Dewnani
- Yazh Muthukumar
- Steven A. Spronk (ORCID: https://orcid.org/0000-0002-2851-2572)
- K. Ghosh
- Brian J. Arey
- Trevor C. Sherwood (ORCID: https://orcid.org/0000-0003-3070-6373)
- Victor R. Guarino
- Alaric J. Dyckman (ORCID: https://orcid.org/0000-0002-1050-2077)
- William J. Pitts (ORCID: https://orcid.org/0000-0002-1034-6043)
- Samuel W. Gerritz (ORCID: https://orcid.org/0000-0002-8378-0393)
- Amy C. Hart (ORCID: https://orcid.org/0000-0002-3739-319X)
- Chi Shing Sum
- Mojgan Abousleiman
- Chandra Sekhar Bokka
- Tamara I. King (ORCID: https://orcid.org/0000-0001-8574-4292)
- Carolyn D. Dzierba (ORCID: https://orcid.org/0000-0001-5162-5295)
- Li Li (ORCID: https://orcid.org/0000-0002-7330-7308)
- Fei Yu (ORCID: https://orcid.org/0000-0003-4367-2707)
- Patrick J. Shaw
- Brian Anderson
- Hai-yun Xiao
- Mary Struthers
- M M Prack
- Carol Krause
- Tao Wang
- Julia Li
- Trevor Vernon
- Ramakrishna Chandran
- Margarita Garcia-Calvo
- Derek Holmes
- Riyaz Khan
Institutions
- Bristol-Myers Squibb (Germany) (DE)
- Bristol-Myers Squibb (India) (IN)
Publication Details
- Journal
- Journal of Medicinal Chemistry
- Published
- 2026-04-03
- DOI
- https://doi.org/10.1021/acs.jmedchem.6c00130
- Primary Topic
- Inflammatory mediators and NSAID effects
- Type
- article
- Field-Weighted Citation Impact
- 0.00