Fig. 3: Imatinib traps ABCG2 in an inward conformation.
From: ABCG2 transports anticancer drugs via a closed-to-open switch
a Cryo-EM map of ABCG2 bound to imatinib. ABCG2 is in an inward facing conformation. TM5 is colored green, and imatinib is colored orange. Red dashed box indicates the position of bound imatinib. b Zoomed-in and rotated view of the highlighted area in (a) showing the cryo-EM map for imatinib. c View of the imatinib binding pocket from the extracellular space. Imatinib binds on the 2-fold axis between ABCG2 monomers and is sandwiched between Phe439 sidechains from each monomer.
