Abstract
A series of simple N-(glyoxyl)pipecolate esters were synthesized as mimics of the FKBP12- binding domain portion of FK506. Compounds which were effective inhibitors of the prolyl isomerase activity of FKBP12 were extraordinarily potent neurotrophic agents in vitro, and were effective in a mouse model of Parkinson's Disease. These results suggest that FKBP12 ligands have therapeutic utility in neurodegenerative diseases.
Original language | English (US) |
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Pages (from-to) | 1785-1790 |
Number of pages | 6 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 7 |
Issue number | 13 |
DOIs | |
State | Published - Jul 8 1997 |
Externally published | Yes |
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry