Discovery and evaluation of potent, cysteine-based alpha4beta1 integrin antagonists

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* rela...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2000-05, Vol.10 (9), p.993-995
Hauptverfasser:	Archibald, S C, Head, J C, Linsley, J M, Porter, J R, Robinson, M K, Shock, A, Warrellow, G J
Format:	Artikel
Sprache:	eng
Schlagworte:	Cysteine - chemistry Cysteine - pharmacology Integrin alpha4beta1 Integrins - antagonists & inhibitors Interleukin-8 - pharmacology Protein Binding Receptors, Lymphocyte Homing - antagonists & inhibitors Structure-Activity Relationship Vascular Cell Adhesion Molecule-1 - metabolism
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Zusammenfassung:	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 CDThioPC related cyclic peptides.
ISSN:	0960-894X