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Structure paper

TitleLigand activation mechanisms of human KCNQ2 channel.
Journal, issue, pagesNat Commun, Vol. 14, Issue 1, Page 6632, Year 2023
Publish dateOct 19, 2023
AuthorsDemin Ma / Yueming Zheng / Xiaoxiao Li / Xiaoyu Zhou / Zhenni Yang / Yan Zhang / Long Wang / Wenbo Zhang / Jiajia Fang / Guohua Zhao / Panpan Hou / Fajun Nan / Wei Yang / Nannan Su / Zhaobing Gao / Jiangtao Guo /
PubMed AbstractThe human voltage-gated potassium channel KCNQ2/KCNQ3 carries the neuronal M-current, which helps to stabilize the membrane potential. KCNQ2 can be activated by analgesics and antiepileptic drugs but ...The human voltage-gated potassium channel KCNQ2/KCNQ3 carries the neuronal M-current, which helps to stabilize the membrane potential. KCNQ2 can be activated by analgesics and antiepileptic drugs but their activation mechanisms remain unclear. Here we report cryo-electron microscopy (cryo-EM) structures of human KCNQ2-CaM in complex with three activators, namely the antiepileptic drug cannabidiol (CBD), the lipid phosphatidylinositol 4,5-bisphosphate (PIP), and HN37 (pynegabine), an antiepileptic drug in the clinical trial, in an either closed or open conformation. The activator-bound structures, along with electrophysiology analyses, reveal the binding modes of two CBD, one PIP, and two HN37 molecules in each KCNQ2 subunit, and elucidate their activation mechanisms on the KCNQ2 channel. These structures may guide the development of antiepileptic drugs and analgesics that target KCNQ2.
External linksNat Commun / PubMed:37857637 / PubMed Central
MethodsEM (single particle)
Resolution2.5 - 3.5 Å
Structure data

35877

8izy

EMDB-35877, PDB-8izy:
Human KCNQ2-CaM in complex with HN37
Method: EM (single particle) / Resolution: 2.5 Å

35879

8j00

EMDB-35879, PDB-8j00:
Human KCNQ2-CaM in complex with CBD
Method: EM (single particle) / Resolution: 3.0 Å

35880

8j01

EMDB-35880, PDB-8j01:
Human KCNQ2-CaM in complex with CBD and PIP2
Method: EM (single particle) / Resolution: 3.1 Å

35881

8j02

EMDB-35881, PDB-8j02:
Human KCNQ2(F104A)-CaM-PIP2-CBD complex in state II
Method: EM (single particle) / Resolution: 3.5 Å

35882

8j03

EMDB-35882, PDB-8j03:
Human KCNQ2(F104A)-CaM-PIP2-CBD complex in state I
Method: EM (single particle) / Resolution: 2.7 Å

35883

8j04

EMDB-35883, PDB-8j04:
Human KCNQ2-CaM-HN37 complex in the presence of PIP2
Method: EM (single particle) / Resolution: 2.7 Å

35884

8j05

EMDB-35884, PDB-8j05:
Human KCNQ2-CaM complex in the presence of PIP2
Method: EM (single particle) / Resolution: 2.7 Å

37270

8w4u

EMDB-37270, PDB-8w4u:
human KCNQ2-CaM in complex with PIP2 and HN37
Method: EM (single particle) / Resolution: 3.3 Å

Chemicals

ChemComp-9MF:
methyl N-[4-[(4-fluorophenyl)methyl-prop-2-ynyl-amino]-2,6-dimethyl-phenyl]carbamate

ChemComp-P0T:
cannabidiol / Cannabidiol

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

Source
  • homo sapiens (human)
KeywordsMEMBRANE PROTEIN / potassium voltage-gated channel / HN37 / CBD / PIP2

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