Design and synthesis of highly potent and specific dynorphin derivatives for affinity labeling of kappa opioid receptors.
Dynorphin A derivatives containing S-(3-nitro-2-pyridinesulfenyl)-cysteine(Cys(Npys)) were designed and synthesized for affinity labeling of kappa opioid receptors. Derivatives with Cys(Npys) residue at the 8 position were highly potent and specific to kappa receptors and bound to receptors through disulfide bond formation.
Matsueda
R
R
New Lead Research Laboratories Sankyo Co. Ltd., Tokyo, Japan.
Koike
K
K
Takayanagi
I
I
D000345:Affinity Labels / Q000138:chemical synthesis*; D000595:Amino Acid Sequence; D000818:Animals; D015195:Drug Design; D004399:Dynorphins / Q000031:analogs & derivatives* / Q000138:chemical synthesis*; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008969:Molecular Sequence Data; D011817:Rabbits; D017473:Receptors, Opioid, kappa / Q000187:drug effects*
D000345:Affinity Labels; D017473:Receptors, Opioid, kappa; D004399:Dynorphins