Author/Authors :
Theodore M. Kamenecka، نويسنده , , You-Jung Park، نويسنده , , Linus S. Lin، نويسنده , , Stephen de Laszlo، نويسنده , , Ermengilda D. McCauley، نويسنده , , Gail Van Riper، نويسنده , , Linda Egger، نويسنده , , Usha Kidambi، نويسنده , , Richard A. Mumford، نويسنده , , Sharon Tong، نويسنده , , Wei Tang، نويسنده , , Adria Colletti، نويسنده , , Yohannes Teffera، نويسنده , , Ralph Stearns، نويسنده , , Malcolm MacCoss، نويسنده , , John A. Schmidt، نويسنده , , William K. Hagmann، نويسنده ,
Abstract :
VLA-4 (α4β1, very late activating antigen-4), a key cell surface integrin plays an important role in inflammation by promoting leukocyte attachment and extravasation from the vasculature into the peripheral tissues. As such, VLA-4 antagonists may be useful in the treatment, prevention, and suppression of diseases where cell adhesion and migration are important such as asthma, rheumatoid arthritis, and multiple sclerosis. Herein, we report on the discovery, synthesis, and biological evaluation of amidines as small molecule antagonists of VLA-4.
Keywords :
VLA-4 , integrin , asthma , e-mail: theodore_kamenecka@merck.com , fax: +1-8582025752 , Inflammation.* Corresponding author. Tel.: +1-8582025449
