Shared class A GPCR activation path
Class A GPCRs share a conserved residue-contact rearrangement pathway from ligand pocket to G-protein site.
Source
Common activation mechanism of class A GPCRs
What they did
Quantified residue–residue contact scores across inactive/active structures and identified conserved switching/repacking contacts.
What they found
A 34-residue-pair pathway across layers; comparisons used 142 inactive and 27 active structures (p<0.001).
The limits
What it doesn't show
Does not replace ligand-specific pharmacology for every receptor.
Key terms
- GPCR
- G protein–coupled receptor.
- Class A
- Largest rhodopsin-like GPCR family.
- RRCS
- Residue–residue contact score.
- Transmission switch
- Conserved contact set linking pocket to core.
- Microswitch
- Local motif rewiring during activation.
- Active vs inactive
- Conformational states relative to G-protein coupling.
Flashcards
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Residue pairs:
Common questions
Pathway size?
34 residue pairs (35 residues).
Inactive structures?
142.
Active structures?
27.
First common step?
Transmission switch + Na⁺ pocket changes.
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