Dimeric β-turn peptidomimetics as ligands for the neurotrophin receptor TrkC

AJ Zhang, S Khare, K Gokulan, DS Linthicum… - Bioorganic & medicinal …, 2001 - Elsevier
Bioorganic & medicinal chemistry letters, 2001Elsevier
Twelve dimeric peptidomimetics 1 were prepared via a divergent–convergent strategy.
These peptidomimetics incorporated the same amino acids as i+ 1 and i+ 2 residues in key
β-turns of the neurotrophin NT-3. Cytosensor microphysiometry was used to gauge the
effects of the dimers 1 on cells that overexpress the NT-3 receptor, TrkC. Increases in
extracellular acidification rates were observed for some monomers 3, but the active dimers
gave greater effects.
Twelve dimeric peptidomimetics 1 were prepared via a divergent–convergent strategy. These peptidomimetics incorporated the same amino acids as i+1 and i+2 residues in key β-turns of the neurotrophin NT-3. Cytosensor microphysiometry was used to gauge the effects of the dimers 1 on cells that overexpress the NT-3 receptor, TrkC. Increases in extracellular acidification rates were observed for some monomers 3, but the active dimers gave greater effects.
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