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Discovery of a new class of glucosylceramide synthase inhibitors |
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| Authors: | Koltun Elena Richards Steven Chan Vicky Nachtigall Jason Du Hongwang Noson Kevin Galan Adam Aay Naing Hanel Art Harrison Amanda Zhang Jeff Won Kwang-Ai Tam Danny Qian Fawn Wang Tao Finn Patricia Ogilvie Kathleen Rosen Jon Mohan Raju Larson Christopher Lamb Peter Nuss John Kearney Patrick |
| Affiliation: | Exelixis, 210 E. Grand Avenue, South San Francisco, CA 94005, USA. |
| Abstract: | A novel series of potent inhibitors of glucosylceramide synthase are described. The optimization of biochemical and cellular potency as well as ADME properties led to compound 23c. Broad tissue distribution was obtained following oral administration to mice. Thus 23c could be another useful tool compound for studying the effects of GCS inhibition in vitro and in vivo. |
| Keywords: | Glucosylceramide synthase inhibitor GCS Diabetes Gaucher disease Cancer Inflammation |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |