Catch the kinase conformer.
Protein kinases exist in inactive and active states, but little attention has been paid to which state is or should be the target in drug discovery efforts. In this issue of Chemistry & Biology, Okram et al. tackle this issue and show that inhibitors can be designed specifically to bind to inactive Abl.
McInnes
Campbell
C
College of Pharmacy, University of South Carolina, Columbia, 29208, USA.
Mezna
Mokdad
M
Kontopidis
George
G
D018360:Crystallography, X-Ray; D008958:Models, Molecular; D011487:Protein Conformation; D011494:Protein Kinases / Q000737:chemistry*
D011494:Protein Kinases