Heterocyclic alpha-helix mimetics for targeting protein-protein interactions.
The design and synthesis of alpha-helix peptidomimetics using inverse electron demand Diels-Alder reactions is described. The potency of the resulting pyridazine-based library to disrupt the Bak/Bcl-X(L) interaction was tested using an in vitro fluorescence polarization assay.
Biros
Shannon M
SM
The Skaggs Institute for Chemical Biology, The Scripps Research Institute, Mail MB-26, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.
Moisan
Lionel
L
Mann
Enrique
E
Carella
Alexandre
A
Zhai
Dayong
D
Reed
John C
JC
Rebek
Julius
J
D006571:Heterocyclic Compounds / Q000737:chemistry*; D008958:Models, Molecular; D011485:Protein Binding; D017433:Protein Structure, Secondary; D050998:bcl-2 Homologous Antagonist-Killer Protein / Q000737:chemistry; D051020:bcl-X Protein / Q000737:chemistry
D006571:Heterocyclic Compounds; D050998:bcl-2 Homologous Antagonist-Killer Protein; D051020:bcl-X Protein