2. Academic Validation
  3. Orally Bioavailable Quinoxaline Inhibitors of 15-Prostaglandin Dehydrogenase (15-PGDH) Promote Tissue Repair and Regeneration

Orally Bioavailable Quinoxaline Inhibitors of 15-Prostaglandin Dehydrogenase (15-PGDH) Promote Tissue Repair and Regeneration

  • J Med Chem. 2022 Nov 2. doi: 10.1021/acs.jmedchem.2c01299.
Bin Hu 1,  Kosuke Toda 2,  Xiaoyu Wang 1,  Monika I Antczak 1,  Julianne Smith 2,  Sophie Geboers 1,  Gen Nishikawa 2,  Hongyun Li 2,  Dawn Dawson 2,  Stephen Fink 2,  Amar B Desai 2,  Noelle S Williams 1,  Sanford D Markowitz 2 3 4,  Joseph M Ready 1
Affiliations

Affiliations

  • 1 Department of Biochemistry, UT Southwestern Medical Center, 5323 Harry Hines Blvd, Dallas, Teas75390-9038, United States.
  • 2 Case Comprehensive Cancer Center, Cleveland, Ohio44106-5065, United States.
  • 3 Department of Medicine, Case Western Reserve University, Cleveland, Ohio44106, United States.
  • 4 Seidman Cancer Center, University Hospitals of Cleveland, Cleveland, Ohio44106, United States.
PMID: 36322935 DOI: 10.1021/acs.jmedchem.2c01299
Abstract

15-Prostaglandin dehydrogenase (15-PGDH) regulates the concentration of prostaglandin E2 in vivo. Inhibitors of 15-PGDH elevate PGE2 levels and promote tissue repair and regeneration. Here, we describe a novel class of quinoxaline amides that show potent inhibition of 15-PGDH, good oral bioavailability, and protective activity in mouse models of ulcerative colitis and recovery from bone marrow transplantation.

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