Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1375845 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
Abstract
Ortho-biphenyl carboxamides, originally prepared as inhibitors of microsomal triglyceride transfer protein (MTP) have been identified as novel inhibitors of the Hedgehog signaling pathway. Structure–activity relationship studies for this class of compounds reduced MTP inhibitory activity and led to low nanomolar Hedgehog inhibitors. Binding assays revealed that the compounds act as antagonists of Smoothened and show cross-reactivity for both the human and mouse receptor.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Stefan Peukert, Rishi K. Jain, Adrian Geisser, Yingchuan Sun, Rui Zhang, Aaron Bourret, Adam Carlson, Jennifer DaSilva, Arun Ramamurthy, Joseph F. Kelleher,