title: N-acyl phenylalanine analogues as potent small molecule VLA-4 antagonists.
abstract: We have identified a series of low molecular weight (Mr < 500) N-acylphenylalanines that are effective inhibitors of the VCAM-VLA-4 interaction. Investigation of the SAR of the N-acyl moiety led to the identification of N-benzylpyroglutamyl derivatives as being particularly potent.
authors.affiliation: Roche Research Center, Hoffmann-La Roche, Inc., Nutley, New Jersey 07110, USA.
authors.forename: L
authors.initials: L
authors.lastname: Chen
authors.forename: J W
authors.initials: JW
authors.lastname: Tilley
authors.forename: T N
authors.initials: TN
authors.lastname: Huang
authors.forename: D
authors.initials: D
authors.lastname: Miklowski
authors.forename: R
authors.initials: R
authors.lastname: Trilles
authors.forename: R W
authors.initials: RW
authors.lastname: Guthrie
authors.forename: K
authors.initials: K
authors.lastname: Luk
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: D000215:Acylation; D039041:Integrin alpha4beta1; D016023:Integrins / Q000037:antagonists & inhibitors*; D010649:Phenylalanine / Q000031:analogs & derivatives* / Q000494:pharmacology*; D016201:Receptors, Lymphocyte Homing / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D039041:Integrin alpha4beta1; D016023:Integrins; D016201:Receptors, Lymphocyte Homing; D010649:Phenylalanine