Ligand Binding and Activation of CAR

FIGURE 5.6 Ligand-induced AF-2 conformational change and coactivator recruitment. 

PXR pocket, thus providing overall stability of the LBD for packing of the AF-2 helix in the active conformation. The second feature is the unique linker helix Hx its position greatly facilitates the AF-2 helix positioning. The role of helix Hx in CAR activation is highlighted by the mutation of L346 to phenylalanine, which dramatically increases CAR s ability to interact with coactivators [31,28], Residue L346 is located 

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