title: Kappa agonist CovX-Bodies.
abstract: Small peptidic kappa agonists were covalently linked to the reactive lysine of the CovX antibody to create compounds having potent activity at the kappa receptor with greatly extended half-life when compared to the parent peptide as exemplified by compound 20.
authors.affiliation: Worldwide Medicinal Chemistry, Pfizer Ramsgate Road, Sandwich, Kent CT13 9NJ, UK. lee.roberts@pfizer.com
authors.forename: Lee R
authors.initials: LR
authors.lastname: Roberts
authors.forename: Kevin
authors.initials: K
authors.lastname: Brady
authors.forename: Amy
authors.initials: A
authors.lastname: Brown
authors.forename: Doreen
authors.initials: D
authors.lastname: Davey
authors.forename: Lijin
authors.initials: L
authors.lastname: Feng
authors.forename: Hanhua
authors.initials: H
authors.lastname: Huang
authors.forename: Dingguo
authors.initials: D
authors.lastname: Liu
authors.forename: Laia
authors.initials: L
authors.lastname: Malet
authors.forename: Gordon
authors.initials: G
authors.lastname: McMurray
authors.forename: Anne
authors.initials: A
authors.lastname: Phelan
authors.forename: Ken
authors.initials: K
authors.lastname: Saunders
authors.forename: Abhijit
authors.initials: A
authors.lastname: Bhat
mesh_terms: D000700:Analgesics / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000906:Antibodies / Q000737:chemistry; D019390:Arrestins / Q000378:metabolism; D001384:Azetidines / Q000737:chemistry; D045744:Cell Line, Tumor; D016503:Drug Delivery Systems; D006207:Half-Life; D006801:Humans; D018796:Immunoconjugates / Q000737:chemistry* / Q000494:pharmacology; D008024:Ligands; D018847:Opioid Peptides / Q000138:chemical synthesis* / Q000494:pharmacology; D021381:Protein Transport / Q000187:drug effects; D051381:Rats; D017473:Receptors, Opioid, kappa / Q000819:agonists* / Q000378:metabolism; D054852:Small Molecule Libraries / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D000071557:beta-Arrestins
chemical_list: C116379:2-azetidinone; D000700:Analgesics; D000906:Antibodies; D019390:Arrestins; D001384:Azetidines; D018796:Immunoconjugates; D008024:Ligands; D018847:Opioid Peptides; D017473:Receptors, Opioid, kappa; D054852:Small Molecule Libraries; D000071557:beta-Arrestins