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Structure paper

TitleTransport mechanism and pharmacology of the human GlyT1.
Journal, issue, pagesCell, Vol. 187, Issue 7, Page 1719-1732.e14, Year 2024
Publish dateMar 28, 2024
AuthorsYiqing Wei / Renjie Li / Yufei Meng / Tuo Hu / Jun Zhao / Yiwei Gao / Qinru Bai / Na Li / Yan Zhao /
PubMed AbstractThe glycine transporter 1 (GlyT1) plays a crucial role in the regulation of both inhibitory and excitatory neurotransmission by removing glycine from the synaptic cleft. Given its close association ...The glycine transporter 1 (GlyT1) plays a crucial role in the regulation of both inhibitory and excitatory neurotransmission by removing glycine from the synaptic cleft. Given its close association with glutamate/glycine co-activated NMDA receptors (NMDARs), GlyT1 has emerged as a central target for the treatment of schizophrenia, which is often linked to hypofunctional NMDARs. Here, we report the cryo-EM structures of GlyT1 bound with substrate glycine and drugs ALX-5407, SSR504734, and PF-03463275. These structures, captured at three fundamental states of the transport cycle-outward-facing, occluded, and inward-facing-enable us to illustrate a comprehensive blueprint of the conformational change associated with glycine reuptake. Additionally, we identified three specific pockets accommodating drugs, providing clear insights into the structural basis of their inhibitory mechanism and selectivity. Collectively, these structures offer significant insights into the transport mechanism and recognition of substrate and anti-schizophrenia drugs, thus providing a platform to design small molecules to treat schizophrenia.
External linksCell / PubMed:38513663
MethodsEM (single particle)
Resolution2.58 - 3.35 Å
Structure data

37492

8wfi

EMDB-37492, PDB-8wfi:
human glycine transporter 1 in complex with glycine in occluded conformation
Method: EM (single particle) / Resolution: 2.58 Å

37493

8wfj

EMDB-37493, PDB-8wfj:
human glycine transporter 1 in complex with ALX-5407 in inward facing conformation
Method: EM (single particle) / Resolution: 3.35 Å

37494

8wfk

EMDB-37494, PDB-8wfk:
human glycine transporter 1 in complex with SSR504734 in outward facing conformation
Method: EM (single particle) / Resolution: 3.22 Å

37495

8wfl

EMDB-37495, PDB-8wfl:
human glycine transporter 1 in complex with PF-03463275 in outward facing conformation
Method: EM (single particle) / Resolution: 3.03 Å

Chemicals

ChemComp-GLY:
GLYCINE / Glycine

ChemComp-CL:
Unknown entry / Chloride

ChemComp-NA:
Unknown entry

ChemComp-HOH:
WATER / Water


ChemComp, No image

ChemComp-W5F:
Unknown entry


ChemComp, No image

ChemComp-W5O:
Unknown entry


ChemComp, No image

ChemComp-W5X:
Unknown entry

Source
  • homo sapiens (human)
KeywordsMEMBRANE PROTEIN / GlyT1 / glycine / ALX-5407 / inward-open / SSR504734 / PF03463275

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