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TitleModulation of the human GlyT1 by clinical drugs and cholesterol.
Journal, issue, pagesNat Commun, Vol. 16, Issue 1, Page 2412, Year 2025
Publish dateMar 11, 2025
AuthorsNa Li / Yiqing Wei / Renjie Li / Yufei Meng / Jun Zhao / Qinru Bai / Gang Wang / Yan Zhao /
PubMed AbstractGlycine transporter 1 (GlyT1) is a key player in shaping extracellular glutamatergic signaling processes and holds promise for treating cognitive impairments associated with schizophrenia by ...Glycine transporter 1 (GlyT1) is a key player in shaping extracellular glutamatergic signaling processes and holds promise for treating cognitive impairments associated with schizophrenia by inhibiting its activity and thus enhancing the function of NMDA receptors. Despite its significant role in physiological and pharmacology, its modulation mechanism by clinical drugs and internal lipids remains elusive. Here, we determine cryo-EM structures of GlyT1 in its apo state and in complex with clinical trial drugs iclepertin and sarcosine. The GlyT1 in its apo state is determined in three distinct conformations, exhibiting a conformational equilibrium of the transport cycle. The complex structures with inhibitor iclepertin and sarcosine elucidate their unique binding poses with GlyT1. Three binding sites of cholesterol are determined in GlyT1, two of which are conformation-dependent. Transport kinetics studies reveal that a delicate binding equilibrium for cholesterol is crucial for the conformational transition of GlyT1. This study significantly enhances our understanding of the physiological and pharmacological aspects of GlyT1.
External linksNat Commun / PubMed:40069141 / PubMed Central
MethodsEM (single particle)
Resolution2.9 - 6.2 Å
Structure data

61226

9j8b

EMDB-61226, PDB-9j8b:
Human Glycine Transporter 1 in the Apo State with an Inward-Facing Conformation
Method: EM (single particle) / Resolution: 3.9 Å

61227

9j8c

EMDB-61227, PDB-9j8c:
Human Glycine Transporter 1 in the Sarcosine-Bound State with an Occluded Conformation
Method: EM (single particle) / Resolution: 2.9 Å

61228

9j8d

EMDB-61228, PDB-9j8d:
Human Glycine Transporter 1 in the Iclepertin-Bound State with an Inward-Facing Conformation
Method: EM (single particle) / Resolution: 3.0 Å

EMDB-61580: Human Glycine Transporter 1 in the Apo State with an Outward-Facing Conformation
Method: EM (single particle) / Resolution: 6.05 Å

EMDB-61581: Human Glycine Transporter 1 in the Apo State with an Occluded Conformation
Method: EM (single particle) / Resolution: 6.2 Å

Chemicals

ChemComp-SAR:
SARCOSINE

ChemComp-CLR:
CHOLESTEROL

ChemComp-CL:
Unknown entry

ChemComp-NA:
Unknown entry

ChemComp-HOH:
WATER

PDB-1ebx:
Unknown entry

Source
  • homo sapiens (human)
KeywordsMEMBRANE PROTEIN / human glycine transporter 1 / GlyT1 / apo / sarcosine / iclepertin

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