LFA-1 inhibitors could give potential help against Cancer

The stages of colon cancer (Credit: thecolorectalinstitute.com)Researchers have described a number of novel molecules that can stop the growth of colon cancer and its spread in the liver.

This research has been published online in the Journal of Medicinal Chemistry.

Researchers have checked these molecules (novel family of integrin leukocyte function associated antigen 1 (LFA-1) inhibitors) in the laboratory mice. (LFA-1 binds with intercellular adhesion molecule 1 (ICAM-1) and plays an important role in cancer and other diseases). These molecules interfere with the adhesion of the tumor cells to the other cells of the organism thereby stop the growth of the tumors and its spread and rapid increase in the other organs.

“In this project we first designed inhibitors to cell adhesion involved in the metastasis of murine melanomas, and then undertook the chemical synthesis of these molecules, testing their biological potential and activity.” Dr. Fernando Cossío, UPV/EHU professor and co-founder of Ikerchem S. L., as well as President of the Executive Committee of Ikerbasque, said in a statement.

“What was surprising was that our calculations predicted that, by introducing relatively small changes, we would be able to generate new molecules with the capacity to inhibit cell adhesion involved in another type of cancer. This prediction was confirmed by the experiments, suggesting that these techniques of chemical design and synthesis could be extended to other related therapeutic targets.” Dr. Fernando added.

“Besides its relevance in the control of cancer and metastasis, this research highlights that, in the Basque Country, there are research teams at academic centres and in companies with the necessary experience and skill to tackle multidisciplinary projects of biomedical relevance, combining synthetic and computational chemistry with the structural analysis of the mechanism and the biological validation of the molecules generated”, Dr. Francisco Blanco, Ikerbasque lecturer and researcher at CIC bioGUNE, said.


San Sebastián, E., Zimmerman, T., Zubia, A., Vara, Y., Martin, E., Sirockin, F., Dejaegere, A., Stote, R., Lopez, X., Pantoja-Uceda, D., Valcárcel, M., Mendoza, L., Vidal-Vanaclocha, F., Cossío, F., & Blanco, F. (2013). Design, Synthesis, and Functional Evaluation of Leukocyte Function Associated Antigen-1 Antagonists in Early and Late Stages of Cancer Development Journal of Medicinal Chemistry, 56 (3), 735-747 DOI: 10.1021/jm3016848


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