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Comparative analysis of two clinically active BCR-ABL kinase inhibitors reveals the role of conformation-specific binding in resistance

Structural studies suggest that most point mutations in the BCR-ABL kinase domain cause resistance to the ABL kinase inhibitor imatinib by impairing the flexibility of the kinase domain, restricting its ability to adopt the inactive conformation required for optimal imatinib binding, rather than by...

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Hlavní autoři: Burgess, Michael R., Skaggs, Brian J., Shah, Neil P., Lee, Francis Y., Sawyers, Charles L.
Médium: Artigo
Jazyk:Inglês
Vydáno: National Academy of Sciences 2005
Témata:
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC552942/
https://ncbi.nlm.nih.gov/pubmed/15705718
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1073/pnas.0409770102
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