Parameters defining the quaternary complex model of allosteric interaction at GPCRs (Fig. 6)
Parameter | Meaning |
---|---|
L | Receptor isomerization constant |
K a | Equilibrium association constant for orthosteric ligand [A] |
K b | Equilibrium association constant for allosteric modulator [B] |
K g | Equilibrium association constant for G protein [G] |
α | Activation cooperativity of [A] for the unliganded receptor |
β | Activation cooperativity of [G] for the unliganded receptor |
γ | Binding cooperativity between [A] and [G] |
δ | Activation cooperativity between [A] and [G] |
ε | Binding cooperativity between [B] and [G] |
ζ | Activation cooperativity of [B] for the unliganded receptor |
η | Activation cooperativity between [B] and [G] |
θ | Binding cooperativity between [A] and [B] |
ι | Activation cooperativity between [A] and [B] |
κ | Binding cooperativity between [A], [B], and [G] |
λ | Activation cooperativity between [A], [B], and [G] |