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Structure paper

TitleMechanisms of Channel Block in Calcium-Permeable AMPA Receptors.
Journal, issue, pagesNeuron, Vol. 99, Issue 5, Page 956-968.e4, Year 2018
Publish dateSep 5, 2018
AuthorsEdward C Twomey / Maria V Yelshanskaya / Alexander A Vassilevski / Alexander I Sobolevsky /
PubMed AbstractAMPA receptors mediate fast excitatory neurotransmission and are critical for CNS development and function. Calcium-permeable subsets of AMPA receptors are strongly implicated in acute and chronic ...AMPA receptors mediate fast excitatory neurotransmission and are critical for CNS development and function. Calcium-permeable subsets of AMPA receptors are strongly implicated in acute and chronic neurological disorders. However, despite the clinical importance, the therapeutic landscape for specifically targeting them, and not the calcium-impermeable AMPA receptors, remains largely undeveloped. To address this problem, we used cryo-electron microscopy and electrophysiology to investigate the mechanisms by which small-molecule blockers selectively inhibit ion channel conductance in calcium-permeable AMPA receptors. We determined the structures of calcium-permeable GluA2 AMPA receptor complexes with the auxiliary subunit stargazin bound to channel blockers, including the orb weaver spider toxin AgTx-636, the spider toxin analog NASPM, and the adamantane derivative IEM-1460. Our structures provide insights into the architecture of the blocker binding site and the mechanism of trapping, which are critical for development of small molecules that specifically target calcium-permeable AMPA receptors.
External linksNeuron / PubMed:30122377 / PubMed Central
MethodsEM (single particle)
Resolution3.9 - 4.8 Å
Structure data

7959

6dlz

EMDB-7959, PDB-6dlz:
Open state GluA2 in complex with STZ after micelle signal subtraction
Method: EM (single particle) / Resolution: 3.9 Å

7960

6dm0

EMDB-7960, PDB-6dm0:
Open state GluA2 in complex with STZ and blocked by IEM-1460, after micelle signal subtraction
Method: EM (single particle) / Resolution: 4.4 Å

7961

6dm1

EMDB-7961, PDB-6dm1:
Open state GluA2 in complex with STZ and blocked by NASPM, after micelle signal subtraction
Method: EM (single particle) / Resolution: 4.2 Å

7962

6o9g

EMDB-7962, PDB-6o9g:
Open state GluA2 in complex with STZ and blocked by AgTx-636, after micelle signal subtraction
Method: EM (single particle) / Resolution: 4.6 Å

Chemicals

ChemComp-GLU:
GLUTAMIC ACID / Glutamic acid

ChemComp-CYZ:
CYCLOTHIAZIDE / Cyclothiazide

ChemComp-GZD:
N,N,N-trimethyl-5-({[(3s,5s,7s)-tricyclo[3.3.1.1~3,7~]decan-1-yl]methyl}amino)pentan-1-aminium

ChemComp-GYY:
N-[3-({4-[(3-aminopropyl)amino]butyl}amino)propyl]-2-(naphthalen-1-yl)acetamide

ChemComp-LU7:
N~1~-{5-[(3-{[3-(L-arginylamino)propyl]amino}propyl)amino]pentyl}-N~2~-[(2,4-dihydroxyphenyl)acetyl]-L-aspartamide

Source
  • rattus norvegicus (Norway rat)
  • homo sapiens (human)
KeywordsTRANSPORT PROTEIN / Ion channel

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