STI-571 Inhibition of Abelson Tyrosine Kinase

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Inadvertent activation of the Abelson Tyrosine Kinase, or Abl, leads to chronic myelogenous leukemia, CML. This results in excessive production of white cells within the bone marrow, overcrowding the bone marrow and disrupting normal blood cell development. A small molecule inhibitor, STI-571, proves effective in treating CML. This model illustrates various interactions between residues and the inhibitor, including numerous hydrogen bonds and Van Der Waals interactions that boost stability and increase binding affinity. The native structure of Abl plays a crucial role in specific binding to STI-571. The binding of STI-571 involves the adoption by the kinase of an inactive conformation, where a centrally located "activation loop" remains unphosphorylated.