6awn

From Proteopedia

X-ray structure of the S439T human serotonin transporter complexed with paroxetine at the central site

Structural highlights

6awn is a 3 chain structure with sequence from Homo sapiens and Mus musculus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:	X-ray diffraction, Resolution 3.62Å
Ligands:	8PR, CL, CLR, LMT, NA, NAG
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

A0A0F7R1P3_MOUSE

Publication Abstract from PubMed

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.

Structural basis for recognition of diverse antidepressants by the human serotonin transporter.,Coleman JA, Gouaux E Nat Struct Mol Biol. 2018 Feb;25(2):170-175. doi: 10.1038/s41594-018-0026-8. Epub, 2018 Jan 29. PMID:29379174^[1]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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Citations

19 reviews cite this structure

Monoamine transporters: structure, intrinsic dynamics and allosteric regulation.

Cheng et al. (2019)

18 more

44 other articles

No citations found

References

↑ Coleman JA, Gouaux E. Structural basis for recognition of diverse antidepressants by the human serotonin transporter. Nat Struct Mol Biol. 2018 Feb;25(2):170-175. doi: 10.1038/s41594-018-0026-8. Epub, 2018 Jan 29. PMID:29379174 doi:http://dx.doi.org/10.1038/s41594-018-0026-8

1 Structural highlights
2 Function
3 Publication Abstract from PubMed
4 See Also
5 References

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PDB ID 6awn

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Categories: Homo sapiens | Large Structures | Mus musculus | Coleman JA | Gouaux E

6awn

From Proteopedia

X-ray structure of the S439T human serotonin transporter complexed with paroxetine at the central site

Structural highlights

Function

Publication Abstract from PubMed

See Also

References

Contents

Proteopedia Page Contributors and Editors (what is this?)

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