Editors' ChoiceFibrosis

Integrating integrin inhibition

Science Signaling  26 May 2015:
Vol. 8, Issue 378, pp. ec139
DOI: 10.1126/scisignal.aac6244

Integrins are a family of cell surface receptors that form cell-cell and cell–extracellular matrix contacts and, as such, are key targets in treating fibrotic disease. However, promiscuous pairing has limited our understanding of the contribution of individual integrin heterodimers. Now, Reed et al. have developed a specific small-molecule inhibitor of the integrin αvβ1, which is abundant on activated fibroblasts. This inhibitor decreased the severity of disease in mouse models of lung and liver fibrosis, in part through downstream effects on transforming growth factor–β. These data suggest that αvβ1 may be a viable target for fibrosis therapy.

N. I. Reed, H. Jo, C. Chen, K. Tsujino, T. D. Arnold, W. F. DeGrado, D. Sheppard, The αvβ1 integrin plays a critical in vivo role in tissue fibrosis. Sci. Transl. Med. 7, 288ra79 (2015). [Abstract]