Hexanoylation of a VPAC2 receptor-preferring ligand markedly increased its selectivity and potency
I Langer, F Gregoire, I Nachtergael, P De Neef… - Peptides, 2004 - Elsevier
We synthesized a VIP analog that combines mutations that decrease the affinity for the
VPAC1 receptor but maintain a high affinity for the VPAC2 receptor with an amino-terminal
hexanoylation that increases the affinity for the VPAC2 receptor with a limited decrease in
the affinity of the VPAC1 receptor. The resulting Hexanoyl [A19, K27, 28] VIP had the
expected properties of a high affinity for the VPAC2 receptor and a low affinity for the VPAC1
receptor and also a low affinity for the PAC1 and secretin receptors. With a 1000-fold …
VPAC1 receptor but maintain a high affinity for the VPAC2 receptor with an amino-terminal
hexanoylation that increases the affinity for the VPAC2 receptor with a limited decrease in
the affinity of the VPAC1 receptor. The resulting Hexanoyl [A19, K27, 28] VIP had the
expected properties of a high affinity for the VPAC2 receptor and a low affinity for the VPAC1
receptor and also a low affinity for the PAC1 and secretin receptors. With a 1000-fold …