Structural basis for p38α MAP kinase quinazolinone and pyridol-pyrimidine inhibitor specificity

Structural basis for the high-affinity b

Structural basis for the high-affinity binding of pyrrolotriazine inhibitors of p38 MAP kinase

✍ Sack, John S. ;Kish, Kevin F. ;Pokross, Matthew ;Xie, Dianlin ;Duke, Gerald J. ; 📂 Article 📅 2008 🏛 International Union of Crystallography 🌐 English ⚖ 635 KB

The crystal structure of unphosphorylated p38 MAP kinase complexed with a representative pyrrolotriazine-based inhibitor led to the elucidation of the high-affinity binding mode of this class of compounds at the ATP-binding site. The ligand binds in an extended conformation, with one end interacting