کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2007780 | 1066386 | 2009 | 7 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: A peptidomimetic of NT-3 acts as a TrkC antagonist A peptidomimetic of NT-3 acts as a TrkC antagonist](/preview/png/2007780.png)
Neurotrophins are a family of growth factors that regulate the peripheral and central nervous system. We designed and tested a mini-library of small molecules peptidomimetics based on β-turns of the neurotrophin growth factor polypeptides NT-3, which is the natural ligand for TrkC receptors. Biological studies identified a peptidomimetic 2Cl that exhibited selective antagonism of TrkC. 2Cl reduces TrkC activation and signaling promoted by NT-3, and selectively blocks ligand-dependent cell survival. 2Cl also blocks ligand-independent TrkC activation and signals that take place when the receptor is over-expressed. This work adds to our understanding of how the neurotrophins function through Trk receptors, and demonstrates that peptidomimetics can be designed to selectively disturb neurotrophin–receptor interactions, and receptor activation.
Journal: Peptides - Volume 30, Issue 10, October 2009, Pages 1833–1839