Case Study: The Discovery of Potent LFA‐1 Antagonists

Russell L Dedrick, Patricia Walicke, Marvin Garovoy, Anti-adhesion antibodies efalizumab, a humanized anti-CD11a monoclonal antibody. Transplant Immunology. ,vol. 9, pp. 181- 186 ,(2002) , 10.1016/S0966-3274(02)00029-1

Gabriele Weitz-Schmidt, Karl Welzenbach, Volker Brinkmann, Tetsji Kamata, Joerg Kallen, Christian Bruns, Sylvain Cottens, Yoshikazu Takada, Ulrich Hommel, Statins selectively inhibit leukocyte function antigen-1 by binding to a novel regulatory integrin site. Nature Medicine. ,vol. 7, pp. 687- 692 ,(2001) , 10.1038/89058

N M Dahms, G W Hart, Influence of quaternary structure on glycosylation. Differential subunit association affects the site-specific glycosylation of the common beta-chain from Mac-1 and LFA-1. Journal of Biological Chemistry. ,vol. 261, pp. 13186- 13196 ,(1986) , 10.1016/S0021-9258(18)69289-0

Mélanie R. Tardif, Michel J. Tremblay, Regulation of LFA-1 activity through cytoskeleton remodeling and signaling components modulates the efficiency of HIV type-1 entry in activated CD4+ T lymphocytes. Journal of Immunology. ,vol. 175, pp. 926- 935 ,(2005) , 10.4049/JIMMUNOL.175.2.926

Mark E. Labadia, Deborah Durham Jeanfavre, Maurice M. Morelock, Gary O. Caviness, Molecular Regulation of the Interaction Between Leukocyte Function-Associated Antigen-1 and Soluble ICAM-1 by Divalent Metal Cations Journal of Immunology. ,vol. 161, pp. 836- 842 ,(1998)

M Champe, W A Werther, S J O'Connor, P W Berman, T N Gonzalez, J A Fox, T Hotaling, S McCabe, B Chan, L G Presta, P M Jardieu, Humanization of an anti-lymphocyte function-associated antigen (LFA)-1 monoclonal antibody and reengineering of the humanized antibody for binding to rhesus LFA-1. Journal of Immunology. ,vol. 157, pp. 4986- 4995 ,(1996)

Kathleen Last-Barney, Walter Davidson, Mario Cardozo, Leah L. Frye, Christine A. Grygon, Jerry L. Hopkins, Deborah D. Jeanfavre, Susan Pav, Chungeng Qian, James M. Stevenson, Liang Tong, Renee Zindell, Terence A. Kelly, Binding site elucidation of hydantoin-based antagonists of LFA-1 using multidisciplinary technologies: evidence for the allosteric inhibition of a protein--protein interaction. Journal of the American Chemical Society. ,vol. 123, pp. 5643- 5650 ,(2001) , 10.1021/JA0104249

Martin Winn, Edward B. Reilly, Gang Liu, Jeffrey R. Huth, Hwan-Soo Jae, Jennifer Freeman, Zhonghua Pei, Zhili Xin, John Lynch, Jeff Kester, Thomas W. von Geldern, Sandra Leitza, Peter DeVries, Robert Dickinson, Donna Mussatto, Gregory F. Okasinski, Discovery of novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intercellular adhesion molecule-1 interaction. 4. Structure-activity relationship of substituents on the benzene ring of the cinnamide. Journal of Medicinal Chemistry. ,vol. 44, pp. 4393- 4403 ,(2001) , 10.1021/JM0103108

G. Song, Y. Yang, J.-h. Liu, J. M. Casasnovas, M. Shimaoka, T. A. Springer, J.-h. Wang, An atomic resolution view of ICAM recognition in a complex between the binding domains of ICAM-3 and integrin αLβ2 Proceedings of the National Academy of Sciences of the United States of America. ,vol. 102, pp. 3366- 3371 ,(2005) , 10.1073/PNAS.0500200102

A. Kuek, B. L Hazleman, A. J K Ostor, Immune-mediated inflammatory diseases (IMIDs) and biologic therapy: a medical revolution. Postgraduate Medical Journal. ,vol. 83, pp. 251- 260 ,(2007) , 10.1136/PGMJ.2006.052688