Allosteric activation of the glutamate receptor mGlu2 by the serotonin receptor 5-HT2A - PubMed
3 hours ago
- #Allosteric Modulation
- #GPCR
- #Receptor Heteromerization
- The study explores the allosteric activation of the glutamate receptor mGlu2 by the serotonin receptor 5-HT2A.
- GPCR dimers and oligomers allow cells to integrate multiple signals, but their allosteric interaction mechanisms are unclear.
- Using molecular dynamics, nanobody-based sensors, and resonance energy transfer assays, the study demonstrates that 5-HT2A acts as a positive allosteric modulator by stabilizing mGlu2's active conformation.
- Cysteine cross-linking experiments and mGlu2 sensors reveal the molecular basis for this allosteric modulation, which is also mediated by other GPCRs.
- The findings provide insights into the allosteric control of GPCR activity through heteromerization with another receptor.