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TitleOptical control of the cardiac rhythm with photoswitchable Na1.5 channel blockers.
Journal, issue, pagesNat Commun, Year 2026
Publish dateMar 10, 2026
AuthorsShiqi Liu / Weiqiang Guan / Zhangqiang Li / Wei Wang / Huifang Song / Jia'ao Li / Junjie Hou / Huan Wang / JingWei Xiong / Min Yang / Nieng Yan / Xin Tian / Houhua Li / Zhuo Huang /
PubMed AbstractVoltage-gated sodium channel Na1.5 is essential for cardiac excitability, mediating the rapid depolarization phase of the cardiac action potential (AP) and ensuring proper electrical conduction in ...Voltage-gated sodium channel Na1.5 is essential for cardiac excitability, mediating the rapid depolarization phase of the cardiac action potential (AP) and ensuring proper electrical conduction in the heart. Dysfunction of Na1.5 is implicated in life-threatening arrhythmias, making it a critical therapeutic target. Acting as a Na1.5 open-state blocker, quinidine demonstrates efficacy in arrhythmia treatment, but its low specificity restricts its clinical application. Here, we report an optopharmacological strategy that enables a precise and optical control of Na1.5 function by means of photoswitchable quinidine derivatives. Through systematic structural optimization, we identify azo-Q2a as a high-performance photoswitchable inhibitor, exhibiting low activity in the dark or under 480 nm light irradiation (trans isomer), while approximately 7-fold higher efficacy is observed under 365 nm light irradiation (cis isomer). Of note, azo-Q2a demonstrates exceptional selectivity for Na1.5 over cardiac ion channels and other Na1 subtypes, minimizing potential off-target effects. Furthermore, by solving the cryo-EM structure of the Na1.5 in complex with the cis-active isomer azo-Q2a (3.0 Å resolution), we reveal the essential binding site that is responsible for the optical control of Na1.5. Finally, azo-Q2a also attenuates the heart rate of living zebrafish larvae with light, showing its potential in cardiac-related research and treatment. Our work not only establishes azo-Q2a as a robust photoswitchable inhibitor for Na1.5 but also provides a structural blueprint for the rational design of next-generation optopharmacological antiarrhythmic agents.
External linksNat Commun / PubMed:41807386
MethodsEM (single particle)
Resolution3.0 Å
Structure data

64755

9v3s

EMDB-64755, PDB-9v3s:
Nav1.5 in complex with quinidine-azo
Method: EM (single particle) / Resolution: 3.0 Å

Chemicals

ChemComp-NAG:
2-acetamido-2-deoxy-beta-D-glucopyranose

PDB-1equ:
TYPE 1 17-BETA HYDROXYSTEROID DEHYDROGENASE EQUILIN COMPLEXED WITH NADP+

ChemComp-NA:
Unknown entry

Source
  • homo sapiens (human)
KeywordsMEMBRANE PROTEIN / Voltage-gated sodium channe Nav1.5

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