Chen et al. provide cryo-EM structures of ABC transporter ABCC4 in human platelets and, through a combination of structural and biochemical assays, demonstrate that platelet agonist TXA2 and antagonist aspirin are substrates of ABCC4 and reveal a specific transmembrane substrate-binding pocket of ABCC4. They also found that dipyridamole is a strong competitive inhibitor against ABCC4, which supports the co-administration of dipyridamole with aspirin in clinic.
- Yu Chen
- Liang Wang
- Yuxing Chen
