Representative conformation of apo-TNKS2 during the last
550 ns
(250–800 ns) of MD trajectory. (Left) The ligand binding pocket
is depicted using a ribbon model. Several key residues (Gly1032, Phe1035,
His1048, Tyr1050, Tyr1060, Ser1068, and Tyr1071) are shown using a
green stick model. The α3 helix, D-loop, and G-loop regions
are shown in magenta. The cyan dotted lines indicate the distance
between the geometric center of the Tyr1050 phenyl ring and that of
the Tyr1070 (the ring distance of Tyr1050–Tyr1071) (Å)
and the minimum distance between the Phe1035 and His1048 side chains
(heavy atoms; the minimum distance of Phe1035–His1048) (Å).
This conformation shows that the NI-closed/AD-closed formed because
the AD subsite remained in the closed conformation and the NI subsites
became narrow compared to those observed in the experimental structure
of apo-TNKS2 (Figure 1 and Table S1). (Right) The ligand binding
pocket is depicted using a molecular surface representation. The hydrophilic
and lipophilic regions are drawn in purple and green, respectively.
These figures are the same view of the structures depicted in Figure 1.