Selective, tight-binding inhibitors of integrin α4β1 that inhibit allergic airway responses

…, CE Hammond, S Kalkunte, LL Chen…

Index: Lin, Ko-Chung; Ateeq, Humayun S.; Hsiung, Sherry H.; Chong, Lillian T.; Zimmerman, Craig N.; Castro, Alfredo; Lee, Wen-Cherng; Hammond, Charles E.; Kalkunte, Sandhya; Chen, Ling-Ling; Pepinsky, R. Blake; Leone, Diane R.; Sprague, Andrew G.; Abraham, William M.; Gill, Alan; Lobb, Roy R.; Adams, Steven P. Journal of Medicinal Chemistry, 1999 , vol. 42, # 5 p. 920 - 934

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Citation Number: 216

Abstract

Integrin α4β1 mediates leukocyte recruitment, activation, mediator release, and apoptosis inhibition, and it plays a central role in inflammatory pathophysiology. High-affinity, selective inhibitors of α4β1, based on the Leu-Asp-Val (LDV) sequence from the alternatively spliced connecting segment-1 (CS-1) peptide of cellular fibronectin, are described that employ a novel N-terminal peptide “cap” strategy. One inhibitor, BIO-1211, was~ 106-fold more ...

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