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Structure paper

TitleGABA receptor signalling mechanisms revealed by structural pharmacology.
Journal, issue, pagesNature, Year 2019
Publish dateJan 2, 2019
AuthorsSimonas Masiulis / Rooma Desai / Tomasz Uchański / Itziar Serna Martin / Duncan Laverty / Dimple Karia / Tomas Malinauskas / Jasenko Zivanov / Els Pardon / Abhay Kotecha / Jan Steyaert / Keith W Miller / A Radu Aricescu
External linksPubMed:30602790 / Publisher's page
KeywordsMEMBRANE PROTEIN / GABAAR / PTX / Membrane / Channel / Nanobody / Megabody / Cys-loop / PLGIC / Inhibition / Signalling / CNS / Neurons / Chloride / Ion / GABA / Picrotoxin / BCC / Bicuculline / Antagonist / Membrane protein / pLGIC / Cys-loop receptor
MethodsEM (single particle)
Resolution3.04 - 3.69 A
Structure data

EMDB-0275:
CryoEM structure of human full-length alpha1beta3gamma2L GABA(A)R in complex with picrotoxin and megabody Mb38.

EMDB-0280:
CryoEM structure of human full-length alpha1beta3gamma2L GABA(A)R in complex with bicuculline and megabody Mb38.

EMDB-0282:
CryoEM structure of human full-length heteromeric alpha1beta3gamma2L GABA(A)R in complex with alprazolam (Xanax), GABA and megabody Mb38.

EMDB-0283:
CryoEM structure of human full-length alpha1beta3gamma2L GABA(A)R in complex with diazepam (Valium), GABA and megabody Mb38.

EMDB-0279:
CryoEM structure of human full-length heteromeric alpha1beta3gamma2L GABA(A)R in complex with picrotoxin, GABA and megabody Mb38.

PDB-6hug:
CryoEM structure of human full-length alpha1beta3gamma2L GABA(A)R in complex with picrotoxin and megabody Mb38.

PDB-6huj:
CryoEM structure of human full-length heteromeric alpha1beta3gamma2L GABA(A)R in complex with picrotoxin, GABA and megabody Mb38.

PDB-6huk:
CryoEM structure of human full-length alpha1beta3gamma2L GABA(A)R in complex with bicuculline and megabody Mb38.

PDB-6huo:
CryoEM structure of human full-length heteromeric alpha1beta3gamma2L GABA(A)R in complex with alprazolam (Xanax), GABA and megabody Mb38.

PDB-6hup:
CryoEM structure of human full-length alpha1beta3gamma2L GABA(A)R in complex with diazepam (Valium), GABA and megabody Mb38.

Chemicals

ChemComp-PIO:
[(2R)-2-octanoyloxy-3-[oxidanyl-[(1R,2R,3S,4R,5R,6S)-2,3,6-tris(oxidanyl)-4,5-diphosphonooxy-cyclohexyl]oxy-phosphoryl]oxy-propyl] octanoate

ChemComp-NAG:
N-ACETYL-D-GLUCOSAMINEN-Acetylglucosamine

ChemComp-BMA:
BETA-D-MANNOSE

ChemComp-MAN:
ALPHA-D-MANNOSE

ChemComp-RI5:
(1aR,2aR,3S,6R,6aS,8aS,8bR,9R)-2a-hydroxy-8b-methyl-9-(prop-1-en-2-yl)hexahydro-3,6-methano-1,5,7-trioxacyclopenta[ij]cyclopropa[a]azulene-4,8(3H)-dionePicrotoxin

ChemComp-ABU:
GAMMA-AMINO-BUTANOIC ACID

ChemComp-H0Z:
bicuculline methochloride

ChemComp-08H:
8-chloro-1-methyl-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepineAlprazolam

ChemComp-DZP:
7-CHLORO-1-METHYL-5-PHENYL-1,3-DIHYDRO-2H-1,4-BENZODIAZEPIN-2-ONE

Source
  • Homo sapiens (human)
  • Lama glama (llama)
  • Bos taurus (cattle)
  • bos taurus (cattle)
  • homo sapiens (human)
  • lama glama (llama)

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