Notch coregulator binding to CSL mutants. The figure graphically depicts the
results of rigorous isothermal titration calorimetry (ITC) experiments
involving series of CSL BTD mutants and their effects on binding between CSL
and established coregulators. The BTD residues selected for mutation—F261,
V263, A284, and Q333—were chosen to disrupt RAM binding without dramatically
altering CSL stability. They are shown with (a) and without (b) an overlay
of the FHL1 peptide; PDB: 4J2X. The colors highlighting the individual
residues reflect the binding retained after mutation, i.e. if a mutation
caused the Kd to increase more than 4-fold but less than 10-fold
(10–25% binding retained), the residue would be colored orange. (c) and (d)
Notch1 RAM and FHL1 were tested against the arginine mutants: F261R, V263R,
A284R, Q333R. Drastic decreases in binding were seen for both coregulators
with the F261 and A284 mutants, illustrating the importance of the platform
created by the phenylalanine sidechain, as well as the cleft afforded by the
compact alanine sidechain. (e) and (f) RITA and SHARP were tested against
the alanine/valine mutants: F261A, V263A, A284V, Q333A. Later experiments
moved to these mutants in order to avoid introducing artifacts due to the
lengthy and charged arginine sidechains.