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Lessons learned from the development of an Abl tyrosine kinase inhibitor for chronic myelogenous leukemia
Brian J. Druker, Nicholas B. Lydon
Brian J. Druker, Nicholas B. Lydon
Published January 1, 2000
Citation Information: J Clin Invest. 2000;105(1):3-7. https://doi.org/10.1172/JCI9083.
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Perspective

Lessons learned from the development of an Abl tyrosine kinase inhibitor for chronic myelogenous leukemia

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Authors

Brian J. Druker, Nicholas B. Lydon

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Figure 2

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The crystal structure of AMP-PNP bound to Lck was used to made a model o...
The crystal structure of AMP-PNP bound to Lck was used to made a model of the Abl kinase domain. (a) The general architecture of the Abl kinase domain. The NH2-terminal domain has a 5-strand β-sheet (blue) and 1 α-helix (red). The COOH-terminal domain is made up of several α-helices. ATP is shown in the ATP-binding cleft. (b) Topology of the ATP-binding cleft of the Abl protein kinase. The ATP-binding cleft can be subdivided into 6 regions: adenine-binding region (yellow), hydrophobic region I (blue), hydrophobic region II (aqua), phosphate-binding region (red-orange), the ribose pocket (purple), and the linker region (pink). The ligated ATP is shown in green-blue. (c) Amino acid side chains lining the ATP-binding cleft.

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