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This chapter describes work that led to the identification of the target of praziquantel (PZQ) in parasitic flatworms. The molecular target of this drug is an ion channel of the transient receptor potential family, named TRPMPZQ. TRPMPZQ is activated by PZQ to cause a rapid depolarization of excitable cells in schistosomes, and the properties of this recently discovered ion channel align well with all known facets of PZQ action. The discovery of this elusive target has rapidly enabled progress to illuminate how PZQ works, understand scenarios in which PZQ is poorly effective, and unlock a new phase of target-based discovery to realize new anthelmintic chemotypes and useful tools for probing parasitic flatworm biology.

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The Molecular Drug Target of Praziquantel

  • 章节

  • 出版模式：

    开放获取

  • 发表日期：

    2026年

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  • Sang-Kyu Park,
  • Daniel J. Sprague,
  • Jonathan S. Marchant

摘要

This chapter describes work that led to the identification of the target of praziquantel (PZQ) in parasitic flatworms. The molecular target of this drug is an ion channel of the transient receptor potential family, named TRPMPZQ. TRPMPZQ is activated by PZQ to cause a rapid depolarization of excitable cells in schistosomes, and the properties of this recently discovered ion channel align well with all known facets of PZQ action. The discovery of this elusive target has rapidly enabled progress to illuminate how PZQ works, understand scenarios in which PZQ is poorly effective, and unlock a new phase of target-based discovery to realize new anthelmintic chemotypes and useful tools for probing parasitic flatworm biology.