potent and selective _v_5 integrin inhibitor
selective in vitro tool compound
from internal integrin library and optimization
Eur. J. Med. Chem., Aug. 2, 2020
GlaxoSmithKline, Stevenage, UK
“compound 12” is a selective inhibitor of integrin αvβ5, a potential target for sepsis due to its potential role in regulating vascular leakage. Selectivity among integrin family members can be challenging to achieve and can have significant safety implications – hence, most integrin drugs have been selective biologics. Since the biological role of many integrins is still not fully understood, selective tool molecules like compound 12 can be very useful in early discovery.