New templates for syntheses of ring-fused,C(10) beta-turn peptidomimetics leading to the first reported small-molecule mimic of neurotrophin-3 |
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| Authors: | Pattarawarapan Mookda Zaccaro Maria Clara Saragovi Uri H Burgess Kevin |
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| Affiliation: | Department of Chemistry, Texas A&M University, P.O. Box 30012, College Station, Texas 77842-3012, USA. |
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| Abstract: | beta-Turn peptidomimetics 1 were designed to mimic hot spots of neurotrophin-3 (NT-3) and others. Solid-phase syntheses of these were developed, though limitations were encountered with scale-up. Consequently, an alternative design with 2 was investigated. 1 and 2 favored distorted type I beta-turn conformations in solution. It was found that peptidomimetic 2b has NT-3-like neurotrophic activity in cell survival assays, selectively binds the NT-3 receptor TrkC, and induces the tyrosine phosphorylation of the TrkC receptor. |
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