Solution conformation of nociceptin.
Nociceptin, a novel heptadecapeptide, interacts with ORL1 a G protein-coupled receptor whose sequence is closely related to that of the kappa opioid receptor but has no opioid activity. We have investigated the conformational preferences of Nociceptin also in comparison to Dynorphin A. The N-terminal part of Nociceptin has the same conformational preferences of the message of endogenous opioids but the C-terminal part of the sequence is more flexible than the corresponding address of Dynorphin A. [Tyr1]-Nociceptin, while retaining nociceptive activity, has also an opioid activity comparable to that of enkephalins.
Salvadori
S
S
Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Italy.
Picone
D
D
Tancredi
T
T
Guerrini
R
R
Spadaccini
R
R
Lazarus
L H
LH
Regoli
D
D
Temussi
P A
PA
D000595:Amino Acid Sequence; D000818:Animals; D002531:Cerebellum / Q000187:drug effects / Q000378:metabolism; D004399:Dynorphins / Q000737:chemistry / Q000235:genetics / Q000494:pharmacology; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects / Q000378:metabolism; D066298:In Vitro Techniques; D007700:Kinetics; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D008969:Molecular Sequence Data; D018847:Opioid Peptides / Q000737:chemistry* / Q000235:genetics / Q000494:pharmacology; D011487:Protein Conformation; D017433:Protein Structure, Secondary; D051381:Rats; D011957:Receptors, Opioid / Q000819:agonists / Q000378:metabolism; D012996:Solutions; D013816:Thermodynamics; D000097629:Nociceptin
D004399:Dynorphins; D018847:Opioid Peptides; D011957:Receptors, Opioid; D012996:Solutions; D000097629:Nociceptin