Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1372160 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
Abstract
PDE4 inhibitors have been identified as therapeutic targets for a variety of conditions, particularly inflammatory diseases. We have serendipitously identified a novel class of phosphodiesterase 4 (PDE4) inhibitor during a study to discover antagonists of the parathyroid hormone receptor. X-ray crystallographic studies of PDE4D2 complexed to four potent inhibitors reveal the atomic details of how they inhibit the enzyme and a notable contrast to another recently reported thiophene-based inhibitor.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Jacob L. Nankervis, Susanne C. Feil, Nancy C. Hancock, Zhaohua Zheng, Hooi-Ling Ng, Craig J. Morton, Jessica K. Holien, Patricia W.M. Ho, Mark M. Frazzetto, Ian G. Jennings, David T. Manallack, T. John Martin, Philip E. Thompson, Michael W. Parker,