PCA of pocket
conformation using MD trajectories of apo-TNKS2,
TNKS2–XAV complex, and TNKS2–OLA complex. For the PCA,
the first 250 ns of the MD trajectory of apo-TNKS2 and 800 ns trajectories
of the TNKS2–XAV complex and the TNKS2–OLA complex were
used. The left panel shows the MD trajectories projected onto the
plane of the first two components (PC1 and PC2). The contribution
ratios of PC1 and PC2 were 44 and 7%, respectively. The black circles
represent the projections of the representative conformations of the
ligand binding pocket. (A–F) were determined based on the PC1
value histogram shown in Figure 5, and these correspond to conformations of (A–F)
of Figure 6. The black
circles of 3KR7, 3KR8, and 3U9Y correspond to the ligand-binding pockets
of X-ray crystallographic structures of apo-TNKS2, the TNKS2–XAV
complex, and the TNKS2–OLA complex. The right panel shows the
motions corresponding to the two eigenvectors, respectively. The red
regions indicate the position of the 21 amino acid residues used for
PCA (see the Methods section). The blue and
green arrows represent the motions of PC1 and PC2, respectively.