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Structure paper

TitleStructural Basis for the Modulation of Human KCNQ4 by Small-Molecule Drugs.
Journal, issue, pagesMol Cell, Vol. 81, Issue 1, Page 25-37.e4, Year 2021
Publish dateJan 7, 2021
AuthorsTian Li / Kun Wu / Zhenlei Yue / Yifei Wang / Fan Zhang / Huaizong Shen /
PubMed AbstractAmong the five KCNQ channels, also known as the K7 voltage-gated potassium (K) channels, KCNQ2-KCNQ5 control neuronal excitability. Dysfunctions of KCNQ2-KCNQ5 are associated with neurological ...Among the five KCNQ channels, also known as the K7 voltage-gated potassium (K) channels, KCNQ2-KCNQ5 control neuronal excitability. Dysfunctions of KCNQ2-KCNQ5 are associated with neurological disorders such as epilepsy, deafness, and neuropathic pain. Here, we report the cryoelectron microscopy (cryo-EM) structures of human KCNQ4 and its complexes with the opener retigabine or the blocker linopirdine at overall resolutions of 2.5, 3.1, and 3.3 Å, respectively. In all structures, a phosphatidylinositol 4,5-bisphosphate (PIP) molecule inserts its head group into a cavity within each voltage-sensing domain (VSD), revealing an unobserved binding mode for PIP. Retigabine nestles in each fenestration, inducing local shifts. Instead of staying within the central pore, linopirdine resides in a cytosolic cavity underneath the inner gate. Electrophysiological analyses of various mutants corroborated the structural observations. Our studies reveal the molecular basis for the modulatory mechanism of neuronal KCNQ channels and provide a framework for structure-facilitated drug discovery targeting these important channels.
External linksMol Cell / PubMed:33238160
MethodsEM (single particle)
Resolution2.5 - 3.3 Å
Structure data

30244

7byl

EMDB-30244, PDB-7byl:
Cryo-EM structure of human KCNQ4
Method: EM (single particle) / Resolution: 2.5 Å

30245

7bym

EMDB-30245, PDB-7bym:
Cryo-EM structure of human KCNQ4 with retigabine
Method: EM (single particle) / Resolution: 3.1 Å

30246

7byn

EMDB-30246, PDB-7byn:
Cryo-EM structure of human KCNQ4 with linopirdine
Method: EM (single particle) / Resolution: 3.3 Å

Chemicals

ChemComp-PT5:
[(2R)-1-octadecanoyloxy-3-[oxidanyl-[(1R,2R,3S,4R,5R,6S)-2,3,6-tris(oxidanyl)-4,5-diphosphonooxy-cyclohexyl]oxy-phospho / phospholipid*YM / Phosphatidylinositol 4,5-bisphosphate

ChemComp-K:
Unknown entry

ChemComp-HOH:
WATER / Water

ChemComp-FBX:
ethyl N-[2-azanyl-4-[(4-fluorophenyl)methylamino]phenyl]carbamate / Retigabine

ChemComp-FCC:
1-phenyl-3,3-bis(pyridin-4-ylmethyl)indol-2-one / Linopirdine

Source
  • homo sapiens (human)
  • aequorea victoria (jellyfish)
KeywordsMEMBRANE PROTEIN / KCNQ / Channel / Calmodulin / PIP2 / retigabine / linopirdine

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