title: Synthesis and erythropoietin receptor binding affinities of N,N-disubstituted amino acids.
abstract: N,N-Dicinnamyl, N-benzyl-N-cinnamyl, and N,N-dibenzyl amino acids were prepared and evaluated in an EPO binding assay. Several derivatives of aspartic acid, glutamic acid, and lysine exhibited moderate (10-50 microM) affinity for EBP; 'dimerization' of the most potent analogues by coupling with linear diamines led to EPO competitors having 1-2 microM binding affinities.
authors.affiliation: The R. W. Johnson Pharmaceutical Research Institute, Raritan, NJ 08869, USA. pconnoll@prius.jnj.com
authors.forename: P J
authors.initials: PJ
authors.lastname: Connolly
authors.forename: S K
authors.initials: SK
authors.lastname: Wetter
authors.forename: W V
authors.initials: WV
authors.lastname: Murray
authors.forename: D L
authors.initials: DL
authors.lastname: Johnson
authors.forename: F J
authors.initials: FJ
authors.lastname: McMahon
authors.forename: F X
authors.initials: FX
authors.lastname: Farrell
authors.forename: J
authors.initials: J
authors.lastname: Tullai
authors.forename: L K
authors.initials: LK
authors.lastname: Jolliffe
mesh_terms: D000596:Amino Acids / Q000138:chemical synthesis* / Q000378:metabolism; D019281:Dimerization; D017467:Receptors, Erythropoietin / Q000378:metabolism*
chemical_list: D000596:Amino Acids; D017467:Receptors, Erythropoietin