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Molecular conformations, interactions, and properties associated with drug efficiency and clinical performance among VEGFR TK inhibitors Print
Monday, 17 September 2012 00:00

Pictured are crystals that contain VEGFR2 tyrosine kinase in complex with an inhibitor from a class of potent anticancer drugs. Michele McTigue et al. produced these and similar crystals to determine the structural basis for the significant variation in potency and clinical performance of members of this anticancer drug class. The authors found that conformations of an often-neglected kinase domain affect the efficiency with which inhibitors bind. Understanding the relationship between kinase conformation and inhibitor efficiency could help optimize drug design for in vivo performance. Article Link (PDF)

Image courtesy of Robert S. Kania.