Bivalent diketopiperazine-based tropomysin receptor kinase C (TrkC) antagonists.
Bivalent molecules containing two beta-turn mimics with side chains that correspond to hot-spots on the neurotrophin NT-3 were prepared. Binding assays showed the mimetics to be selective TrkC ligands, and biological assays showed one mimetic to be an antagonist of the TrkC receptor.
Liu
Jing
J
Department of Chemistry, Texas A&M University, Box 30012, College Station, Texas 77842-3012, USA.
Brahimi
Fouad
F
Saragovi
H Uri
HU
Burgess
Kevin
K
D020816:Amino Acid Motifs; D000818:Animals; D002470:Cell Survival / Q000187:drug effects; D054659:Diketopiperazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D051379:Mice; D041681:NIH 3T3 Cells; D020933:Neurotrophin 3 / Q000378:metabolism; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D020812:Receptor, trkC / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015398:Signal Transduction
D054659:Diketopiperazines; D020933:Neurotrophin 3; D047428:Protein Kinase Inhibitors; D020812:Receptor, trkC