The design and synthesis of potent cyclic peptide VCAM–VLA-4 antagonists incorporating an achiral Asp-Pro mimetic

…, A Hanglow, K Rowan, V Schwinge, B Wolitzky

Index: Fotouhi, Nader; Joshi, Pramod; Fry, David; Cook, Charles; Tilley, Jefferson W.; Kaplan, Gerry; Hanglow, Angela; Rowan, Karen; Schwinge, Virginia; Wolitzky, Barry Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 11 p. 1171 - 1173

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Citation Number: 28

Abstract

Vascular cell adhesion molecule-l (VCAM-l), a member of the immunoglobulin (Ig) supergene family, is expressed on activated, but not resting, endothelium. The principal receptor for VCAM-1, the integrin very late antigen 4 (VLA-4, α 4 β 1 ), is expressed on many lymphocytes including circulating eosinophils, basophils, and monocytes, but not neutrophils. Antibodies to either protein are effective at inhibiting leukocyte infiltration and preventing tissue ...