Anindya Roy, Lei Shi, Ashley Chang, Xianchi Dong, Andres Fernandez, John C Kraft, Jing Li, Viet Q Le, Rebecca Viazzo Winegar, Gerald Maxwell Cherf, Dean Slocum, P Daniel Poulson, Garrett E Casper, Mary L Vallecillo-Zúniga, Jonard Corpuz Valdoz, Marcos C Miranda, Hua Bai, Yakov Kipnis, Audrey Olshefsky, Tanu Priya, Lauren Carter, Rashmi Ravichandran, Cameron M Chow, Max R Johnson, Suna Cheng, McKaela Smith, Catherine Overed-Sayer, Donna K Finch, David Lowe, Asim K Bera, Gustavo Matute-Bello, Timothy P Birkland, Frank DiMaio, Ganesh Raghu, Jennifer R Cochran, Lance J Stewart, Melody G Campbell, Pam M Van Ry, Timothy Springer, David Baker
The RGD (Arg-Gly-Asp)-binding integrins αvβ6 and αvβ8 are clinically validated cancer and fibrosis targets of considerable therapeutic importance. Compounds that can discriminate between homologous αvβ6 and αvβ8 and other RGD integrins, stabilize specific conformational states, and have high thermal stability could have considerable therapeutic utility. Existing small molecule and antibody inhibitors do not have all these properties, and hence new approaches are needed...
September 13, 2023: Nature Communications