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Fig. 8.2
Amino acid changes to KP-10 at the C-terminus affect receptor binding. (
a
) KP-10
binds strongly to GPR54 with an IC
50
of 7.7 nM. (
b
) Peptide 208, with a glycine at position 5
binds the receptor with an IC
50
of 120 nM and effectively displaces the labelled ligand by 75% at
10
M (
d
) D -Trp
8
retains a binding affi nity with an IC
50
of 6 nM similar to KP-10. Amino acid structure of the
peptides is also shown
μ
M. (
c
) Replacement of Phe
6
with D -Phe
6
signifi cantly reduces the IC
50
to 4.3
μ
had been hypothesised that these residues were involved in binding to the receptor due
to the high level of conservation of these residues between vertebrate species and the
RFamide motif within this family; peptides 208, 209, 210, 211, 212, 213 and 288
(Figs.
8.2
and
8.3
).
In order to increase the fl exibility of the peptide and make substitutions poten-
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