Inside job: Ligand-receptor pharmacology beneath the plasma membrane

Joseph J. Babcock, Min Li

Research output: Contribution to journalReview articlepeer-review

6 Scopus citations


Most drugs acting on the cell surface receptors are membrane permeable and thus able to engage their target proteins in different subcellular compartments. However, these drugs' effects on cell surface receptors have historically been studied on the plasma membrane alone. Increasing evidence suggests that small molecules may also modulate their targeted receptors through membrane trafficking or organelle-localized signaling inside the cell. These additional modes of interaction have been reported for functionally diverse ligands of GPCRs, ion channels, and transporters. Such intracellular drug-target engagements affect cell surface expression. Concurrent intracellular and cell surface signaling may also increase the complexity and therapeutic opportunities of small molecule modulation. Here we discuss examples of ligand-receptor interactions that are present in both intra- and extracellular sites, and the potential therapeutic opportunities presented by this phenomenon.

Original languageEnglish (US)
Pages (from-to)859-869
Number of pages11
JournalActa Pharmacologica Sinica
Issue number7
StatePublished - Jul 2013
Externally publishedYes


  • GPCR
  • endoplasmic reticulum
  • ion channel
  • ligand-receptor interaction
  • phamacological chaperone
  • transporter

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)


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