title: The discovery of non-basic atrial natriuretic peptide clearance receptor antagonists. Part 1.
abstract: The cyclic peptide ANP 4-23 and the linear peptide analogue AP-811 have been shown to be selective ANP-CR antagonists. Via alanine scanning and truncation studies we sought to determine which residues in these molecules were important in their binding to the clearance receptor and the relationship between these two molecules. These studies show that several modifications to these compounds are possible which improve physical properties of these molecules while retaining high affinity for the ANP-CR.
authors.affiliation: Department of Chemistry, AstraZeneca Pharmaceuticals, Wilmington, DE 19850-5437, USA. chris.veale@astrazeneca.com
authors.forename: C A
authors.initials: CA
authors.lastname: Veale
authors.forename: V C
authors.initials: VC
authors.lastname: Alford
authors.forename: D
authors.initials: D
authors.lastname: Aharony
authors.forename: D L
authors.initials: DL
authors.lastname: Banville
authors.forename: R A
authors.initials: RA
authors.lastname: Bialecki
authors.forename: F J
authors.initials: FJ
authors.lastname: Brown
authors.forename: J R
authors.initials: JR
authors.lastname: Damewood
authors.forename: C L
authors.initials: CL
authors.lastname: Dantzman
authors.forename: P D
authors.initials: PD
authors.lastname: Edwards
authors.forename: R T
authors.initials: RT
authors.lastname: Jacobs
authors.forename: R C
authors.initials: RC
authors.lastname: Mauger
authors.forename: M M
authors.initials: MM
authors.lastname: Murphy
authors.forename: W
authors.initials: W
authors.lastname: Palmer
authors.forename: K K
authors.initials: KK
authors.lastname: Pine
authors.forename: W L
authors.initials: WL
authors.lastname: Rumsey
authors.forename: L E
authors.initials: LE
authors.lastname: Garcia-Davenport
authors.forename: A
authors.initials: A
authors.lastname: Shaw
authors.forename: G B
authors.initials: GB
authors.lastname: Steelman
authors.forename: J M
authors.initials: JM
authors.lastname: Surian
authors.forename: E P
authors.initials: EP
authors.lastname: Vacek
mesh_terms: D000595:Amino Acid Sequence; D009320:Atrial Natriuretic Factor / Q000378:metabolism*; D008969:Molecular Sequence Data; D017461:Receptors, Atrial Natriuretic Factor / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D009320:Atrial Natriuretic Factor; D017461:Receptors, Atrial Natriuretic Factor