6AWQ
Anomalous chloride signal reveals the position of sertraline complexed with the serotonin transporter at the central site
Summary for 6AWQ
| Entry DOI | 10.2210/pdb6awq/pdb |
| Descriptor | Sodium-dependent serotonin transporter, 8B6 antibody FAB heavy chain, 8B6 antibody FAB light chain, ... (8 entities in total) |
| Functional Keywords | neurotransmitter transporter, antidepressant, transport protein |
| Biological source | Homo sapiens (Human) More |
| Total number of polymer chains | 3 |
| Total formula weight | 111478.33 |
| Authors | Coleman, J.A.,Gouaux, E. (deposition date: 2017-09-06, release date: 2017-10-25, Last modification date: 2023-10-04) |
| Primary citation | Coleman, J.A.,Gouaux, E. Structural basis for recognition of diverse antidepressants by the human serotonin transporter. Nat. Struct. Mol. Biol., 25:170-175, 2018 Cited by PubMed Abstract: Selective serotonin reuptake inhibitors are clinically prescribed antidepressants that act by increasing the local concentrations of neurotransmitters at synapses and in extracellular spaces via blockade of the serotonin transporter. Here we report X-ray structures of engineered thermostable variants of the human serotonin transporter bound to the antidepressants sertraline, fluvoxamine, and paroxetine. The drugs prevent serotonin binding by occupying the central substrate-binding site and stabilizing the transporter in an outward-open conformation. These structures explain how residues within the central site orchestrate binding of chemically diverse inhibitors and mediate transporter drug selectivity. PubMed: 29379174DOI: 10.1038/s41594-018-0026-8 PDB entries with the same primary citation |
| Experimental method | X-RAY DIFFRACTION (4.046 Å) |
Structure validation
Download full validation report
