title: The design and synthesis of potent cyclic peptide VCAM-VLA-4 antagonists incorporating an achiral Asp-Pro mimetic.
abstract: The Asp-Pro sequence of the cyclic peptide Ac-HN-Tyr-Cys*-Asp-Pro-Cys*-OH (1) could be replaced with the achiral dipeptide mimetic 1-(2-aminoethyl)cyclpentylcarboxylic acid with retention of potent inhibition of the VCAM-VLA-4 interaction.
authors.affiliation: Roche Research Center, Hoffmann-La Roche Inc, Nutley, NJ 07110, USA. nader.fotouhi@roche.com
authors.forename: N
authors.initials: N
authors.lastname: Fotouhi
authors.forename: P
authors.initials: P
authors.lastname: Joshi
authors.forename: D
authors.initials: D
authors.lastname: Fry
authors.forename: C
authors.initials: C
authors.lastname: Cook
authors.forename: J W
authors.initials: JW
authors.lastname: Tilley
authors.forename: G
authors.initials: G
authors.lastname: Kaplan
authors.forename: A
authors.initials: A
authors.lastname: Hanglow
authors.forename: K
authors.initials: K
authors.lastname: Rowan
authors.forename: V
authors.initials: V
authors.lastname: Schwinge
authors.forename: B
authors.initials: B
authors.lastname: Wolitzky
mesh_terms: D001224:Aspartic Acid / Q000737:chemistry*; D015195:Drug Design; D039041:Integrin alpha4beta1; D016023:Integrins / Q000037:antagonists & inhibitors*; D018716:Molecular Mimicry; D010456:Peptides, Cyclic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011392:Proline / Q000737:chemistry*; D016201:Receptors, Lymphocyte Homing / Q000037:antagonists & inhibitors*; D019010:Vascular Cell Adhesion Molecule-1 / Q000187:drug effects*
chemical_list: D039041:Integrin alpha4beta1; D016023:Integrins; D010456:Peptides, Cyclic; D016201:Receptors, Lymphocyte Homing; D019010:Vascular Cell Adhesion Molecule-1; D001224:Aspartic Acid; D011392:Proline