Tethered agonists: A new mechanism underlying adhesion G protein-coupled receptor activation

Torsten Schöneberg, Ines Liebscher, Rong Luo, Kelly R. Monk, Xianhua Piao

Research output: Contribution to journalArticlepeer-review

14 Scopus citations


The family of adhesion G protein-coupled receptors (aGPCRs) comprises 33 members in the human genome, which are subdivided into nine subclasses. Many aGPCRs undergo an autoproteolytic process via their GPCR Autoproteolysis-INducing (GAIN) domain during protein maturation to generate an N- and a C-terminal fragments, NTF and CTF, respectively. The NTF and CTF are non-covalently reassociated on the plasma membrane to form a single receptor unit. How aGPCRs are activated upon ligand binding remains one of the leading questions in the field of aGPCR research. Recent work from our labs and others shows that ligand binding can remove the NTF from the plasma membrane-bound CTF, exposing a tethered agonist which potently activates downstream signaling.

Original languageEnglish (US)
Pages (from-to)220-223
Number of pages4
JournalJournal of Receptors and Signal Transduction
Issue number3
StatePublished - Sep 11 2015
Externally publishedYes


  • G proteincoupled signaling
  • adhesion GPCR
  • tethered agonist

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Cell Biology


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