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Updated: Apr 17, 2026

Expression and Purification of the Human Lipid-sensitive Cation Channel TRPC3 for Structural Determination by Single-particle Cryo-electron Microscopy
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(-)-Englerin A is a potent and selective activator of TRPC4 and TRPC5 calcium channels

Yasemin Akbulut1, Hannah J Gaunt, Katsuhiko Muraki

  • 1Max-Planck-Institut für Molekulare Physiologie, Otto-Hahn-Strasse 11, 44227 Dortmund (Germany); Technische Universität Dortmund, Fakultät Chemie, Lehrbereich Chemische Biologie, Otto-Hahn-Strasse 6, 44227 Dortmund (Germany).

Angewandte Chemie (International Ed. in English)
|February 25, 2015
PubMed

Insights

A novel compound, (-)-englerin A, rapidly and selectively kills renal cancer cells by activating specific calcium channels (TRPC4/5). This discovery offers new avenues for developing targeted renal cancer therapies.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Current renal cell cancer therapies lack specificity and efficacy.
  • There is a critical need for novel pharmacological targets and treatment strategies.

Purpose of the Study:

  • To investigate the potential of sesquiterpene (-)-englerin A in targeting renal cancer cells.
  • To explore the mechanism of action of (-)-englerin A on calcium channels.

Main Methods:

  • Utilized (-)-englerin A, a sesquiterpene compound.
  • Investigated the activation of calcium-permeable nonselective transient receptor potential canonical (TRPC) channels, specifically TRPC4 and TRPC5.
  • Assessed the compound's effect on renal cancer cell viability.

Main Results:

  • (-)-Englerin A demonstrated rapid and selective killing of renal cancer cells.
  • The compound acts as a potent, selective, and direct stimulator of TRPC4 and TRPC5 channels.
  • A high-affinity extracellular binding site for (-)-englerin A on TRPC4/5 was identified.

Conclusions:

  • Activation of TRPC4/5 channels by (-)-englerin A presents a novel approach for renal cancer treatment.
  • This mechanism offers promising opportunities for future drug discovery in renal cancer therapy.
Keywords:
antitumor agentscalcium ionsion channelsnatural products

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