•KDM5A/B
histone demethylases are amplified and overexpression in multiple solid tumors,
making these enzymes ideal targets for cancer therapy
•KDM5B
loss/inhibition induced robust antitumor immune response, leading to prolong
survival of tumor bearing mice in multiple models (Figure below)
•Specific
inhibitors of KDM5 inhibitors (IC50s of ~20 nM)
have been identified. 35 high-resolution crystal structures (1.22-2.29 Å) of
KDM5A with various inhibitors are available to support further medicinal
chemistry optimization
