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Shared class A GPCR activation path
Class A GPCRs share a conserved residue-contact rearrangement pathway from ligand pocket to G-protein site.
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Pathway contacts?
34 residue pairs.
Source: Common activation mechanism of class A GPCRs · DOI · quote verified
Metric?
RRCS / ΔRRCS contact scores.
Source: Common activation mechanism of class A GPCRs · DOI · quote verified
Layer 1 idea?
Transmission switch + Na⁺ pocket.
Source: Common activation mechanism of class A GPCRs · DOI · quote verified
Stats?
p<0.001 active vs inactive.
Source: Common activation mechanism of class A GPCRs · DOI · quote verified
Receptor class?
Class A GPCRs.
Source: Common activation mechanism of class A GPCRs · DOI · quote verified
Endpoint?
G-protein-competent cytosolic interface.
Source: Common activation mechanism of class A GPCRs · DOI · quote verified
Limit?
Shared core ≠ identical ligands.
Source: Common activation mechanism of class A GPCRs · DOI · quote verified
Takeaway?
Diverse agonists converge on one allosteric path.
Source: Common activation mechanism of class A GPCRs · DOI · quote verified