Dimeric beta-turn peptidomimetics as ligands for the neurotrophin receptor TrkC.
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 beta-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.
Zhang
A J
AJ
Texas A&M University, Chemistry Department, College Station, TX 77842-3012, USA.
Khare
S
S
Gokulan
K
K
Linthicum
D S
DS
Burgess
K
K
D002460:Cell Line / Q000187:drug effects; D020650:Combinatorial Chemistry Techniques; D019281:Dimerization; D006801:Humans; D007700:Kinetics; D008024:Ligands; D018716:Molecular Mimicry; D020933:Neurotrophin 3 / Q000737:chemistry; D010455:Peptides / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology*; D017433:Protein Structure, Secondary; D020812:Receptor, trkC / Q000235:genetics / Q000378:metabolism*; D017475:Receptors, Nerve Growth Factor / Q000235:genetics / Q000378:metabolism; D013329:Structure-Activity Relationship; D014162:Transfection
D008024:Ligands; D020933:Neurotrophin 3; D010455:Peptides; D017475:Receptors, Nerve Growth Factor; D020812:Receptor, trkC