Ontology highlight
ABSTRACT:
SUBMITTER: Ruan B
PROVIDER: S-EPMC2224212 | biostudies-literature | 2008 Jan
REPOSITORIES: biostudies-literature
Ruan Benfang B Pong Kevin K Jow Flora F Bowlby Mark M Crozier Robert A RA Liu Danni D Liang Shi S Chen Yi Y Mercado Mary Lynn ML Feng Xidong X Bennett Frann F von Schack David D McDonald Leonard L Zaleska Margaret M MM Wood Andrew A Reinhart Peter H PH Magolda Ronald L RL Skotnicki Jerauld J Pangalos Menelas N MN Koehn Frank E FE Carter Guy T GT Abou-Gharbia Magid M Graziani Edmund I EI
Proceedings of the National Academy of Sciences of the United States of America 20071227 1
Rapamycin is an immunosuppressive immunophilin ligand reported as having neurotrophic activity. We show that modification of rapamycin at the mammalian target of rapamycin (mTOR) binding region yields immunophilin ligands, WYE-592 and ILS-920, with potent neurotrophic activities in cortical neuronal cultures, efficacy in a rodent model for ischemic stroke, and significantly reduced immunosuppressive activity. Surprisingly, both compounds showed higher binding selectivity for FKBP52 versus FKBP12 ...[more]