Literature DB >> 21974949

Discovery of a new class of glucosylceramide synthase inhibitors.

Elena Koltun1, Steven Richards, Vicky Chan, Jason Nachtigall, Hongwang Du, Kevin Noson, Adam Galan, Naing Aay, Art Hanel, Amanda Harrison, Jeff Zhang, Kwang-Ai Won, Danny Tam, Fawn Qian, Tao Wang, Patricia Finn, Kathleen Ogilvie, Jon Rosen, Raju Mohan, Christopher Larson, Peter Lamb, John Nuss, Patrick Kearney.   

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.
Copyright © 2011 Elsevier Ltd. All rights reserved.

Entities:  

Mesh:

Substances:

Year:  2011        PMID: 21974949     DOI: 10.1016/j.bmcl.2011.09.037

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  Attenuation of acetic acid-induced gastric ulcer formation in rats by glucosylceramide synthase inhibitors.

Authors:  Manabu Nakashita; Hidekazu Suzuki; Soichiro Miura; Takao Taki; Keita Uehara; Tohru Mizushima; Hiroshi Nagata; Toshifumi Hibi
Journal:  Dig Dis Sci       Date:  2012-08-24       Impact factor: 3.199

2.  Novel compounds that reverse the disease phenotype in Type 2 Gaucher disease patient-derived cells.

Authors:  Wayne Childers; Rong Fan; Rogelio Martinez; Dennis J Colussi; Edward Melenski; Yuxiao Liu; John Gordon; Magid Abou-Gharbia; Marlene A Jacobson
Journal:  Bioorg Med Chem Lett       Date:  2019-11-11       Impact factor: 2.823

Review 3.  The development and use of small molecule inhibitors of glycosphingolipid metabolism for lysosomal storage diseases.

Authors:  James A Shayman; Scott D Larsen
Journal:  J Lipid Res       Date:  2014-02-17       Impact factor: 5.922

  3 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.