title: Discovery and evaluation of potent, cysteine-based alpha4beta1 integrin antagonists.
abstract: Acyclic, disulphide derivatives of cysteine have been identified as moderately potent antagonists of alpha4beta1-mediated leukocyte cell adhesion to VCAM. This communication describes how they were discovered from a simple L-cystine derivative and using the structure-activity data of C*DThioPC* related cyclic peptides.
authors.affiliation: Celltech Chiroscience, Slough, UK.
authors.forename: S C
authors.initials: SC
authors.lastname: Archibald
authors.forename: J C
authors.initials: JC
authors.lastname: Head
authors.forename: J M
authors.initials: JM
authors.lastname: Linsley
authors.forename: J R
authors.initials: JR
authors.lastname: Porter
authors.forename: M K
authors.initials: MK
authors.lastname: Robinson
authors.forename: A
authors.initials: A
authors.lastname: Shock
authors.forename: G J
authors.initials: GJ
authors.lastname: Warrellow
mesh_terms: D003545:Cysteine / Q000737:chemistry* / Q000494:pharmacology; D039041:Integrin alpha4beta1; D016023:Integrins / Q000037:antagonists & inhibitors*; D016209:Interleukin-8 / Q000494:pharmacology; D011485:Protein Binding; D016201:Receptors, Lymphocyte Homing / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D019010:Vascular Cell Adhesion Molecule-1 / Q000378:metabolism
chemical_list: D039041:Integrin alpha4beta1; D016023:Integrins; D016209:Interleukin-8; D016201:Receptors, Lymphocyte Homing; D019010:Vascular Cell Adhesion Molecule-1; D003545:Cysteine