864926-75-0Relevant academic research and scientific papers
Thiophene inhibitors of PDE4: Crystal structures show a second binding mode at the catalytic domain of PDE4D2
Nankervis, Jacob L.,Feil, Susanne C.,Hancock, Nancy C.,Zheng, Zhaohua,Ng, Hooi-Ling,Morton, Craig J.,Holien, Jessica K.,Ho, Patricia W.M.,Frazzetto, Mark M.,Jennings, Ian G.,Manallack, David T.,John Martin,Thompson, Philip E.,Parker, Michael W.
, p. 7089 - 7093 (2012/01/06)
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.
