TABLE 1

Sequences and modifications of the helix 9 peptides

ET residues are underlined. In peptides 6, 7, and 8, Nle was substituted for Met165 to avoid sulfur oxidation.

PeptideSequenceModification
1EFDRRWRQWRELWLRModified sequence except for ET residues, designed by PB
1AAAc-EFDRRWRQWRELWLR-NH2(AA) Acetylated and amidated peptide 1
2DFEERRRQWLILYRModified sequence except for ET residues, designed by PB
2AAAc-DFEERRRQWLILYR-NH2(AA) Acetylated and amidated peptide 2
3EEYFKRRWEQWYKLYModified sequence except for ET residues, designed by PB
4YFNRFLQWKWLEUnmodified GRK6 α9 (166–177)
5Ac-FFDRFLQWKWLE-NH2Acetylated and amidated GRK5 α9 (166–177)
6Ac-SNleFFDRFLQWKWLER-NH2Acetylated and amidated GRK5 α9 (164-M165Nle-178)
7Ac-SNleFFDRELQWKWLER-NH2Glu170 side chain–Lys174 side chain bridge
8Ac-SNleFEDRFKQWKWLER-NH2Glu167 side chain–Lys171 side chain bridge
  • PB, peptide builder.