Bcr-Abl Inhibited by STI571 (Imatinib)
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The groundbreaking development of STI571 has transformed treatment options for chronic myelogenous leukemia (CML), offering a beacon of hope for highly targeted and effective drug interventions. Bcr-Abl is an abnormally activated, mutated version of Abl, which would normally operate with tightly regulated activity. STI571 or Imatinib exhibits remarkably precise binding to the inactive conformation of the affected enzyme, and has been proven successful in halting disease progression in up to 93% of cases (Druker, 2008). Druker, BJ 2008, 'Translation of the Philadelphia chromosome into therapy for CML', Blood, vol. 112, no. 13, pp. 4808-4817. Structural Information: Schindler, T, Bornmann, W, Pellicena, P, Miller, WT, Clarkson, B & Kuriyan, J 2000, 'Structural mechanism for STI-571 inhibition of abelson tyrosine kinase', Science, vol. 289, no. 5486, pp. 1938-1942.
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