7F8X
Crystal structure of the cholecystokinin receptor CCKAR in complex with NN9056
Summary for 7F8X
| Entry DOI | 10.2210/pdb7f8x/pdb |
| Descriptor | Cholecystokinin receptor type A,Endolysin, ASP-SMF-NLE-GLY-TRP-NLE-OEM-MEA-NH2 (NN9056) (2 entities in total) |
| Functional Keywords | g protein-coulped receptor, structural protein |
| Biological source | Homo sapiens (human) More |
| Total number of polymer chains | 2 |
| Total formula weight | 61583.62 |
| Authors | |
| Primary citation | Zhang, X.,He, C.,Wang, M.,Zhou, Q.,Yang, D.,Zhu, Y.,Feng, W.,Zhang, H.,Dai, A.,Chu, X.,Wang, J.,Yang, Z.,Jiang, Y.,Sensfuss, U.,Tan, Q.,Han, S.,Reedtz-Runge, S.,Xu, H.E.,Zhao, S.,Wang, M.W.,Wu, B.,Zhao, Q. Structures of the human cholecystokinin receptors bound to agonists and antagonists. Nat.Chem.Biol., 17:1230-1237, 2021 Cited by PubMed Abstract: Cholecystokinin receptors, CCKR and CCKR, are important neurointestinal peptide hormone receptors and play a vital role in food intake and appetite regulation. Here, we report three crystal structures of the human CCKR in complex with different ligands, including one peptide agonist and two small-molecule antagonists, as well as two cryo-electron microscopy structures of CCKR-gastrin in complex with G and G, respectively. These structures reveal the recognition pattern of different ligand types and the molecular basis of peptide selectivity in the cholecystokinin receptor family. By comparing receptor structures in different conformational states, a stepwise activation process of cholecystokinin receptors is proposed. Combined with pharmacological data, our results provide atomic details for differential ligand recognition and receptor activation mechanisms. These insights will facilitate the discovery of potential therapeutics targeting cholecystokinin receptors. PubMed: 34556863DOI: 10.1038/s41589-021-00866-8 PDB entries with the same primary citation |
| Experimental method | X-RAY DIFFRACTION (3 Å) |
Structure validation
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