Literature DB >> 16185865

Rapamycin analogs with reduced systemic exposure.

Rolf Wagner1, Karl W Mollison, Luping Liu, Cynthia L Henry, Teresa A Rosenberg, Nwe Bamaung, Noah Tu, Paul E Wiedeman, Yatsun Or, Jay R Luly, Benjamin C Lane, James Trevillyan, Yung-Wu Chen, Thomas Fey, Gin Hsieh, Kennan Marsh, Merrill Nuss, Peer B Jacobson, Denise Wilcox, Richard P Carlson, George W Carter, Stevan W Djuric.   

Abstract

The synthesis and biological activities of rapamycin (I) analogs modified at the C-40 position are reported. Emphasis placed on compounds that potentially have an improved safety profile on account of their shorter in vivo half-life when compared with rapamycin.

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Year:  2005        PMID: 16185865     DOI: 10.1016/j.bmcl.2005.06.106

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


  4 in total

1.  Light regulation of protein dimerization and kinase activity in living cells using photocaged rapamycin and engineered FKBP.

Authors:  Andrei V Karginov; Yan Zou; David Shirvanyants; Pradeep Kota; Nikolay V Dokholyan; Douglas D Young; Klaus M Hahn; Alexander Deiters
Journal:  J Am Chem Soc       Date:  2010-12-16       Impact factor: 15.419

2.  Autophagy activation by rapamycin reduces severity of experimental osteoarthritis.

Authors:  Beatriz Caramés; Akihiko Hasegawa; Noboru Taniguchi; Shigeru Miyaki; Francisco J Blanco; Martin Lotz
Journal:  Ann Rheum Dis       Date:  2011-11-14       Impact factor: 19.103

3.  Rapamycin-induced autophagy activity promotes bone fracture healing in rats.

Authors:  G E Yang; Xunhong Duan; Dasheng Lin; Ten Li; Deqing Luo; Lei Wang; Kejian Lian
Journal:  Exp Ther Med       Date:  2015-07-27       Impact factor: 2.447

4.  Site-specific bioalkylation of rapamycin by the RapM 16-O-methyltransferase.

Authors:  Brian J C Law; Anna-Winona Struck; Matthew R Bennett; Barrie Wilkinson; Jason Micklefield
Journal:  Chem Sci       Date:  2015-03-02       Impact factor: 9.825

  4 in total

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