The discovery and development of IP3 receptor modulators: an update

Jessica Gambardella, Marco B. Morelli, Xujun Wang, Vanessa Castellanos, Pasquale Mone, Gaetano Santulli

Research output: Contribution to journalReview articlepeer-review

14 Scopus citations


Introduction: Inositol 1,4,5-trisphosphate receptors (IP3Rs) are intracellular calcium (Ca2+) release channels located on the endoplasmic/sarcoplasmic reticulum. The availability of the structure of the ligand-binding domain of IP3Rs has enabled the design of compatible ligands, but the limiting step remains their actual effectiveness in a biological context. Areas covered: This article summarizes the compelling literature on both agonists and antagonists targeting IP3Rs, emphasizing their strengths and limitations. The main challenges toward the discovery and development of IP3 receptor modulators are also described. Expert opinion: Despite significant progress in recent years, the pharmacology of IP3R still has major drawbacks, especially concerning the availability of specific antag onists. Moreover, drugs specifically targeting the three different subtypes of IP3R are especially needed.

Original languageEnglish (US)
Pages (from-to)709-718
Number of pages10
JournalExpert Opinion on Drug Discovery
Issue number6
StatePublished - 2021


  • 2-APB
  • Adenophostin
  • IP3
  • IP3R
  • ITPR
  • drug design
  • structure
  • xestospongin

ASJC Scopus subject areas

  • Drug Discovery


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