Table 3

Parameters defining the quaternary complex model of allosteric interaction at GPCRs (Fig. 6)

ParameterMeaning
LReceptor 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]
αActivation cooperativity of [A] for the unliganded receptor
βActivation cooperativity of [G] for the unliganded receptor
γBinding cooperativity between [A] and [G]
δActivation cooperativity between [A] and [G]
εBinding cooperativity between [B] and [G]
ζActivation cooperativity of [B] for the unliganded receptor
ηActivation cooperativity between [B] and [G]
θBinding cooperativity between [A] and [B]
ιActivation cooperativity between [A] and [B]
κBinding cooperativity between [A], [B], and [G]
λActivation cooperativity between [A], [B], and [G]