Design of Short α-Helical Peptides for Transcriptional Inhibitor of Nuclear Receptor

摘要

We have synthesized short helical peptides, S_(3,7)S-1, R_(3,7)S-l, S_(3,7)R-1, and R_(3,7)R-1, containing an-LXXLL-coactivator binding motif. The preferred secondary structure of R_(3,7)R-1 was a (P) α-helix in both solution and the crystalline state. The four peptides were subjected to an hVDR inhibition assay using a receptor cofactor system.