Beta-casomorphins: substitution of phenylalanine with beta-homo phenylalanine increases the mu-type opioid receptor affinity.
Two analogues of bovine beta-casomorphin-7 and beta-casomorphin-5 containing a beta-homo phenylalanine in substitution of the phenylalanine in position 3 were synthesised and tested for their mu-opioid receptor affinity. The modification enhanced the mu receptor affinity 5-fold in the case of modified beta-CM-7 and 2-fold for modified beta-CM-5 when compared to the natural peptides.
Longobardo
L
L
Dipartinento di Scienza degli Alimenti, Università di Napoli Federico II, Portici, Italy. luilongo@unina.it
Melck
D
D
Siciliano
R
R
Santini
A
A
Di Marzo
V
V
Cammarota
G
G
D000595:Amino Acid Sequence; D000818:Animals; D002417:Cattle; D004723:Endorphins / Q000737:chemistry / Q000378:metabolism*; D010649:Phenylalanine / Q000737:chemistry*; D011485:Protein Binding; D051381:Rats; D017450:Receptors, Opioid, mu / Q000378:metabolism*
D004723:Endorphins; D017450:Receptors, Opioid, mu; D010649:Phenylalanine; C021968:beta-casomorphins