Research Paper Volume 13, Issue 1 pp 163—180

Identification of a novel and potent small molecule inhibitor of SRPK1: mechanism of dual inhibition of SRPK1 for the inhibition of cancer progression

Structure of SRPK1-compund C02 complex is superimposed with SRPK1-ASF/SF2 complex. It is clearly seen that C02 has interrupted the complex formation by engaging Lys174 which forms critical attractive interaction with Glu170 of ASF/SF2. Lys174 is rotated almost 2-folds towards ATP binding site and is unavailable to form salt bridge interactions with Glu170 of ASF/SF2.

Figure 5. Structure of SRPK1-compund C02 complex is superimposed with SRPK1-ASF/SF2 complex. It is clearly seen that C02 has interrupted the complex formation by engaging Lys174 which forms critical attractive interaction with Glu170 of ASF/SF2. Lys174 is rotated almost 2-folds towards ATP binding site and is unavailable to form salt bridge interactions with Glu170 of ASF/SF2.