Effects of D-amino acid substitution in dynorphin A (1-9) on binding at the mu-, delta- and kappa-sites.
Incorporation of D-Ala into position 2 of dynorphin A (1-9) (Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile-Arg) causes a loss of kappa-selectivity. Similarly, replacement of L-Arg by D-Arg also diminished kappa-selectivity. The combination of D-Ala in position 2 and D-Arg in positions 6, 7 and 9 further reduces kappa-binding. In experiments at 25 degrees C, D-Ala substitution leads to a stable peptide whereas D-Arg substitutions do not stabilize the peptides.
D000818:Animals; D004399:Dynorphins / Q000378:metabolism*; D006168:Guinea Pigs; D066298:In Vitro Techniques; D011957:Receptors, Opioid / Q000378:metabolism*; D017465:Receptors, Opioid, delta; D017473:Receptors, Opioid, kappa; D017450:Receptors, Opioid, mu; D013329:Structure-Activity Relationship
D011957:Receptors, Opioid; D017465:Receptors, Opioid, delta; D017473:Receptors, Opioid, kappa; D017450:Receptors, Opioid, mu; D004399:Dynorphins