Two disparate ligand-binding sites in the human P2Y1 receptor

@article{Zhang2015TwoDL,
  title={Two disparate ligand-binding sites in the human P2Y1 receptor},
  author={Dandan Zhang and Zhang-Guo Gao and K. Zhang and E. Kiselev and S. Crane and Jiang Wang and S. Paoletta and C. Yi and Limin Ma and Wenru Zhang and G. Han and Hong Liu and V. Cherezov and V. Katritch and H. Jiang and R. Stevens and K. Jacobson and Qiang Zhao and B. Wu},
  journal={Nature},
  year={2015},
  volume={520},
  pages={317-321}
}
In response to adenosine 5′-diphosphate, the P2Y1 receptor (P2Y1R) facilitates platelet aggregation, and thus serves as an important antithrombotic drug target. Here we report the crystal structures of the human P2Y1R in complex with a nucleotide antagonist MRS2500 at 2.7 Å resolution, and with a non-nucleotide antagonist BPTU at 2.2 Å resolution. The structures reveal two distinct ligand-binding sites, providing atomic details of P2Y1R's unique ligand-binding modes. MRS2500 recognizes a… Expand
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