Figure 23-45. How Gleevec (STI-571) blocks the activity of Bcr-Abl protein and halts chronic myeloid leukemia.

Figure 23-45How Gleevec (STI-571) blocks the activity of Bcr-Abl protein and halts chronic myeloid leukemia

(A) The chemical structure of Gleevec. The drug can be given by mouth; it has side effects but they are usually quite tolerable. (B) The structure of the complex of Gleevec (solid green object) with the tyrosine kinase domain of the Abl protein (ribbon diagram), as determined by X-ray crystallography. (C) Gleevec sits in the ATP-binding pocket of the tyrosine kinase domain of Bcr-Abl and thereby prevents Bcr-Abl from transferring a phosphate group from ATP onto a tyrosine residue in a substrate protein. This blocks onward transmission of a signal for cell proliferation and survival. (B, from T. Schindler et al., Science 289:1938–1942, 2000. © AAAS.)

From: Cancer Treatment: Present and Future

Cover of Molecular Biology of the Cell
Molecular Biology of the Cell. 4th edition.
Alberts B, Johnson A, Lewis J, et al.
New York: Garland Science; 2002.
Copyright © 2002, Bruce Alberts, Alexander Johnson, Julian Lewis, Martin Raff, Keith Roberts, and Peter Walter; Copyright © 1983, 1989, 1994, Bruce Alberts, Dennis Bray, Julian Lewis, Martin Raff, Keith Roberts, and James D. Watson .

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